Agent for preventing and treating prostatitis and prostate adenoma

FIELD: medicine.

SUBSTANCE: invention represents an agent for preventing and treating prostatitis and prostate adenoma in the form of a capsule, which contains doxazosin, diisopropylammonium dichroloacetate, afobazol, copper glycinate, vitamin E (d-alpha tocopherol acetate), zinc glycinate; L-Glutamine; L-Alanine; L-Arginine and excipients: corn starch and talc.

EFFECT: extended range of products for treating and preventing prostatitis and prostate adenoma.

4 ex, 3 tbl


The drug relates to medicine, namely to urology, and can be used for the prevention and treatment of prostatitis (inflammation in the prostate) and benign prostatic hyperplasia BPH (benign prostatic hyperplasia).

Among the most common diseases in men in the second half of life is benign prostatic hyperplasia (BPH) or prostatic hypertrophy, which is preceded by acute or chronic prostatitis.

The prostate is a small, but very important organ. Urologists sometimes jokingly called "the heart of a real man". The prostate gland plays an important role in the development of special male secret and because of its location below the bladder, partially covering the urethra, affects the entire urinary system. The prostate gland is an organ that produces nutritious juice for sperm, which is the basis of the ejaculate (semen). Effect of anatomical features here especially progresses rapidly asymptomatic inflammation (prostatitis). According to statistics, prostatitis in one form or another gets sick every second man over the age of 40-45 years. There are factors that significantly increase the risk of developing this disease. Among them is transferred sexually transmitted diseases, stress is s, not strong enough immunity, bad habits, and especially alcohol abuse, sedentary lifestyle, lack of exercise and sedentary work, as well as prolonged sexual abstinence and malnutrition, and its consequence is frequent constipation. Sedentary work has become the norm, with few of the office staff devotes sufficient time to the sport. Even the journey to work the most is doing sitting of the people in the bus or in the subway, who on the private car. Immunodeficiency is the result of other causes: poor in vitamins, but rich in fats, meals, stay in the polluted air of the big city, and, again, lack of physical activity. Well, the stress has long been the constant companion of almost everyone, especially in our country.

The main symptoms of prostatitis: difficult, painful urination, frequent urination, feeling of incomplete emptying of the bladder, the need to urinate at night, decreased libido, impairment of erection, premature ejaculation, smudged or painful orgasm, pain in the perineum, scrotum, penis, weakness, fatigue, drowsiness, constipation, unstable stool, discharge from the urethra.

Nonspecific symptoms - back pain, spine, reduced efficiency, concentration, attention to detail is I, initiative, irritability, tinnitus, ringing in the head, insomnia, fatigue in the morning after sleep, inappropriate aggression. The prostate begins to appear only in the later stages, when it's already passed in the prostate adenoma. Adenoma is a benign tumor, which is day by day increasing in size, squeezing the bladder and urethra. She insistently declares itself a weak jet of urine, feeling of incomplete emptying of the bladder, frequent night urination, and a sharp decline in potency. Often adenoma reborn in severe cancer - prostate cancer. Problems such patients known since Gerofila, Hippocrates, Seneca. The disease has a negative impact not only on health but also on the quality of life of patients. That's why it's urgent to develop less traumatic and effective methods of treatment, particularly drug therapy.

Similar to the proposed means is the drug SEISIN® (SONIZIN) International name: tamsulosin (tamsulosin)

Codes ATC: G04CA02

CFG: Drug, used for disorders of the urinary symptoms associated with benign prostatic hyperplasia. Alpha-blocker. Owner reg. ID: GEDEON RICHTER Plc. (Hungary). Register the ion number: LSR-002155/07 Capsules with modified-release hard gelatin, size # 2, opaque, with a brown cap and brown-yellow body. The contents of the capsules tamsulosin hydrochloride (5-2-2-O ethoxybenzothiazole-2-methoxybenzenesulfonamide hydrochloride) - 400 mg excipients: calcium stearate, triethylcitrate, talc, copolymer of methacrylic acid and ethyl acrylate (1:1) (also contains Polysorbate 80, sodium laurylsulfate), microcrystalline cellulose. The composition of the body and cap of the capsule: iron oxide yellow (C. I. 77492 E172), iron oxide black (C. I. 77499 E172), iron oxide red (C. I. 77491 E172), titanium dioxide (C. I. 77891 E171), gelatin. Seisin selectively and competitively blocks postsynaptic α1A-adrenergic receptors located in the smooth muscle of the prostate, bladder neck and prostatic part of the urethra, and α1D-adrenergic receptors, located primarily in the body of the bladder. This leads to a decrease of tonus of smooth muscles of the prostate, bladder neck and prostatic part of the urethra and improves the function of the detrusor. This reduces the symptoms of obstruction and irritation associated with benign prostatic hyperplasia. Typically, therapeutic effect develops within 2 weeks after you start taking the drug, although in some patients the decrease in the severity of symptoms is observed after which the Riem first dose (Kamalov, A. A., Dorofeev S. D. "Modern views on the problem of chronic prostatitis". Eng. the honey. journal., 2003; 11(№4): 229-233; Tkachuk Century. N. "Chronic prostatitis". - M.: Medicine for all, 2006 - 112 S.; Kudryavtsev Y. C., L. Romanova M. "Morphological changes in the tissue of the prostate in benign hyperplasia"; "Benign prostatic hyperplasia". M. 1999; 37-45 C.; Russian journal of medicine, December 25, 2008, volume 16, No. 29, "Clinical guidelines and algorithms for medical practitioners. Selected lectures for family physicians. Surgery and urology").

The disadvantages of this drug are its side effects:

- CNS: headache, dizziness, fatigue, sleep disorders (hypersomnia or insomnia);

- part of the reproductive system: retrograde ejaculation, reduced libido;

- cardio-vascular system: in rare cases

- orthostatic hypotension, tachycardia, palpitations;

- from the digestive system: nausea, vomiting, constipation or diarrhea, allergic reactions: skin rashes, pruritus, angioedema;

- other: rarely, back pain, rhinitis; in a few cases, pain in the chest;

- used with caution in patients older than 75 years.

The closest analogue to the proposed means is the drug Xatral".

The active ingredient of the drug - doxazosin. Chemical name: (±)-1-(4-Amino-6,7-dimethoxy-2-hintline)-4-[(2,3-dihydro-1,4-benzodioxin-2-yl)carbonyl]piperazine (and monoethanolamine).

Chemical formula C23H25N5O5. Mol. weight - 451.475 g/mol.

Tablets contains salt doxazosin nelfinavir in doses equivalent to 1, 2, 4 and 8 mg doxazosin. Other ingredients: sodium starch glycolate, microcrystalline cellulose, lactose, magnesium stearate, sodium laurylsulfate. Release form tablets. 1 mg, 2 mg, 4 mg: 30 pcs. Registration No.: - P # 011944/01-2000 23.05.05 Proizvoditel: PFIZER GmbH. HEINRICH MACKNACHF. GmbH&Co. KG. Code ATX: C02CA04 (Doxazosin). MHM: Doxazosin.

Pharm. group: Antihypertensive drugs.

Pharmacological action. Doxazosin is an active component of the drug Xatral, has a vasodilating effect through selective competitive blockade of postsynaptic alpha-adrenergic receptors.

The purpose of doxazosin patients with symptoms of benign prostatic hyperplasia (BPH) leads to a significant improvement of urodynamics and reduce the appearance of disease symptoms. This action of the drug is associated with selective blockade alpha-adrenergic receptors located in the stroma and capsule of the prostate and bladder neck.

It is proved that doxazosin is a blocker alpha-adrenoreceptor subtype 1A, which amount is approximately 70% of all subtypes, presented in the prostate. This explains its effect in patients with BPH. Xatral is used in the treatment of benign prostatic hyperplasia (BPH), for symptomatic treatment delays the outflow of urine and other symptoms associated with BPH. In patients with BPH the drug can be administered as presence of hypertension, and normal AD. When prescribing the drug to patients with BPH with normal blood pressure change last insignificant. (Lopatkin N.A. (as amended). "Benign prostatic hyperplasia"), 1999; 216; Tkachuk C. N., Al-Shukri, S. H., A. Lukyanov, E. "Medical treatment of patients with benign prostatic hyperplasia". - SPb., 2000; 104).

The disadvantages. The drug Xatral a large number of side effects: orthostatic reactions (in rare cases fainting), dizziness (including those associated with change of body position), headache, fatigue, malaise, edema, asthenia, drowsiness, nausea, rhinitis; abdominal pain, diarrhea, vomiting, agitation, tremor; incontinence of urine (this effect may be due to the pharmacological activity of Xatral), isolated cases of pianism and impotence. It was also noted cases of skin rash, thrombocytopenia, purpura, nasal bleeding, leukopenia, hematuria, cholestasis, hepatitis, jaundice, disorders of the indicator of the liver and hazy vision, other side effects that were reported during postmarketing studies of the drug in patients with arterial hypertension - tachycardia, palpitations, chest pain, angina, myocardial infarction, ischemic, and arrhythmias.

Objectives the proposed tools:

- organotropism; reduction of the clinical manifestations of the disease (average score of symptoms according to the International scale IPSS) and quality of life improvement;

positive dynamics of uroflowmetry (maximum urine flow rate, reducing the amount of residual urine, elimination of dysuria;

the decrease in the average volume of the prostate;

- decrease inflammation and reduce the activity of the inflammatory process in the prostate gland by improving the microcirculation;

- decrease side effects.

The essence of the proposed remedies for the prevention and treatment of prostatitis and benign prostatic hyperplasia is that it is a composition active substances, including the target of the ingredients the following ingredients, in mg:

Diisopropylamine dichloroacetate10-100
afobazolea 9.7-10,0
glycinate copper200-200,1
Vit E (d-alpha tocopherol acetate)36,70-of 36.76
glycinate zinc30,0-30,1


corn starch22,91-22,93

The proposed combination drug has a broad spectrum of pharmacological activity. It normalizes metabolic processes in the prostate gland, has detoxification, membrane stabilizing, antioxidant and organotropic action. Reduces edema, leukocyte infiltration of the prostate gland and normalizes secretion of epithelial cells, increases the amount of lecithin grains secret acini, stimulates muscle tone of the bladder. Reduces thrombus formation, has antiplatelet what aktivnosti, prevents the development of thrombosis of venules in the prostate gland. In comparison with drugs of the same pharmacological groups (diseases of the urogenital organs) are not toxic.

The applicants plan to call the proposed drug "Apostol-400". The technical result from the use of "Apostola-400" is determined by the action of substances in its composition:

- Doxazosin - chemical name: 1-(4-Amino-6,7-dimethoxy-2-hintline)-4-(2,3-dihydro-1,4-benzodioxin-2-yl)carbapenemases (monoethanolamine). Pharmacological group - selective alpha-blocker; a means of influencing the metabolism in the prostate gland, and correctors of urodynamics. This substance has a significant impact on the vessels of the prostate, normalizing their status, thereby improving blood flow in the prostate gland. Feature doxazosin is its selective effect on vascular postsynaptic alpha 1-adrenergic receptors, which distinguishes it from conventional alpha-blockers, at the same time blocking alpha and alpha 2-adrenergic receptors of the blood vessels, consequently doxazosingeneric the vasoconstrictor effect of neurotransmitter (norepinephrine) without affecting other types of activity. Typical actions doxazosin is mainly peripheral of vasodilate the Oia. He has simultaneously arterio - and wearaccentuate action. Selective alpha-blockers is the most popular and numerous group of drugs for the treatment of BPH in all countries of the world, due to the high efficiency, speed manifestations of positive change and availability. It is proved that in the body of the bladder revealed predominantly cholinergic and beta-adrenergic nerve endings, while the posterior urethra and the prostate gland contain mostly alpha-adrenergic receptors. This distribution of receptors plays an important role in coordinating the activities of the muscles of the bladder and prostate. Recent studies have shown that BPH leads to increased activity of the sympathetic nerve fibers, which causes an increase in the tone of smooth muscle structures of the base of the bladder, posterior urethra and prostate gland. The process of hyperplasia is mainly due to the stromal component of the prostate gland, which contains up to 60% of smooth muscle fibers, which is the point of application of alpha-blockers. The mechanism of action of alpha-blockers is the relaxation of smooth muscles of the bladder neck and posterior urethra due to the blockade of alpha 1-adrenergic receptors. The decreased activity of si is piticescu nervous system, in addition to addressing dynamiccode component infravesical obstruction, improves blood circulation in the pelvic organs and, in particular, of the bladder. Improved blood flow leads to a decrease in the intensity of hypoxia, improvement of bioenergy and contractility of the detrusor. Thus, alpha-blockers are the only group of drugs that have effects on two of the three pathogenic mechanisms of disorders of urination in BPH - increased maximum urinary flow rates, reducing the amount of residual urine. Weak flow of urine in patients with prostatitis is usually associated with incomplete relaxation of the bladder neck and spastic constriction of the urethra at the level of its external sphincter, which causes low pressure in the bladder and slow urination during excretion. In spastic syndrome sphincter of the bladder neck and urethra alphablocker give a quick and positive effect. After just one or two days after starting the drug, many men have reported the enhancement of the urine stream and do not experience such frequent urination, especially at night. This occurs at the expense of reducing the maximum detrusor pressure and opening pressure. Changes in these urodynamic indices indicates the object is active reduction intravesically obstructive and irritative symptoms in the treatment of alpha 1-blockers. Doxazosin may also favorably affect the performance of serum lipids, reduces the aggregation of erythrocytes.

- Afobazole. Pharmacotherapeutic group: Tranquilizer (selective anxiolytic). The derived 2-mercaptobenzimidazole not classified as agonists of benzodiazepine receptors. Prevents the development membranes.obesity changes in GABA-a receptor. The drug has anxiolytic (anti-anxiety) effect and a light stimulus (activating) effect. Has no gipnosedativnogo effect, reduces or eliminates anxiety (concern, misgivings, fears, irritability), tension (fearfulness, tearfulness, anxiety, inability to relax, insomnia, fear). Somatic (muscular, sensory, cardiovascular, respiratory, and gastrointestinal symptoms), vegetative (dry mouth, sweating, dizziness), cognitive (difficulty concentrating, impaired memory) violations disappear in 5-7 day treatment Effects. The maximum effect is reached by the end of 4 weeks of treatment and maintained in polyarimetricheskim period on average 1-2 weeks. At drug no miorelaksantnoe properties, a negative effect on memory and attention. If the drug is not formed drug dependency and nerazvijena syndrome. Afobazole has a special mechanism of action different from other anti-anxiety and sedative drugs. Afobazole affects the so-called Sigma-receptors and triggers our inner, natural protection mechanism against stress, revitalizing destabilized membranes of nerve cells. Thanks to a special mechanism of action, he has no inhibitory action on the Central nervous system, this allows you to avoid the development of side effects that affect our physical health. Many drugs for the treatment of anxiety and stress cause Central nervous system depression and related drowsiness, impaired concentration, which complicates the use of these drugs in everyday life. Afobazole such effects is not. It does not cause drowsiness or addiction or habituation, therefore, justified its use in prostatitis and prostate cancer with the development of symptom-nocturia. Nocturia (urination at night, for which you want to interrupt sleep; nocturia - nocturnal polyuria) is one of the most painful disorders of urination. Every time the night-time urination, frequency of which is up to 5 times or more, preceded by the interruption of sleep. Chronic sleep deprivation causes patients solivas the ü day mood swings, depression, trouble falling asleep at night and eventually deterioration of the quality of life. Nocturia included in the list of so-called prostatic symptoms that admits the existence of a causal relationship between benign prostatic hyperplasia (BPH) and need to empty your bladder during the night.

- Diisopropylamine dichloroacetate. International non-proprietary name - Diisopropylamine. Pharmaceutical group - stimulants metabolism of different chemical groups. Empirical formula C8H17Cl2NO2. Molecular weight: 230.13. White crystalline powder bitter taste. Easily soluble in water and alcohol. Obtained by hydrolysis of ethyl ether dichloracetic acid. Production technology developed by LLC "Polivet" (, Ufa). Metabolic impact of Diisopropylamine of dichloracetate due to the improvement of the functional state of the prostate, the restoration of homeostasis in the body, the normalization of functional activity and the stimulation of tissue regeneration processes gland, normalization of redox processes and the microcirculation in the syndrome of peripheral ischemia. The mechanism of action of Diisopropylamine of dichloracetate due to its antioxidant and membrane-stabilizing action. It inhibits the peroxidation processes, avishay activity superoxidized, reduces the viscosity of the membrane increases its fluidity. Modulates the activity of membrane-bound enzymes that enhances their ability to associate contributes to the preservation of structural and functional organization of biomembranes. Causes activation energosintezirutuyu of mitochondrial function, stabilization of cell membranes, improves the rheological properties of blood. All of the above processes reduce swelling and inflammation in the prostate gland.

Diisopropylamine dichloroacetate allows you to resolve the following symptoms seen in chronic prostatitis and prostate adenoma: disorders of urination; erectile dysfunction; decreased sexual desire; feeling of incomplete emptying of the bladder; the difficulty and the reduction of the jet of urine; straining to urinate; the imperative urge to urinate.

Depending on the phase of the disease, the authors propose to use the drug "Apostol-400" with different content of Diisopropylamine of dichloracetate. Minimum single dose of 10 mg for the prevention of prostatitis, benign prostatic hyperplasia and in remission chronic prostatitis. The maximum single dose 100 mg used to treat prostatitis and benign prostatic hyperplasia. Other concentrations of Diisopropylamine dichloroacetate determines l is casi doctor.

- Glycinate copper - biocoordination connection, biogenic metals. Glycine metabolic means, nonessential amino acid, a Central neurotransmitter braking action type. Amino acids are white crystalline substances, soluble (with some exceptions) in water, ammonia and other polar solvents; non-polar and slightly polar solvents (methanol, ethanol, acetone) dissolved bad. In aqueous solutions of all amino acids exist in the form of bipolar ions (zwitter-ions) with dissociated carboxyl group and a protonated amino group. Depending on the pH of the medium amino acids can be in the form of cations, anions, neutral in charge of bipolar ions or mixtures of these forms, one of which usually dominates. Amino acids are amphoteric compounds, in strongly acidic solvents have a positive charge, alkaline - negative charge. Due to the amphoteric character of the amino acids are buffer substances, performs an important function in the regulation of pH in the body. Glycine improves metabolic processes in tissues, has antidepressant and sedative effect. Has a glycine and the GABAergic, alpha-adrenoceptor blocking, antioxidant and antitoxic action; regulates the activity of glutamate (NMDA) receptors, which reduces the psycho who emotional tension, aggression and conflict; improves social adjustment and mood, AIDS sleep and normalizes sleep; improves mental performance; reduces the severity of vegetative-vascular disorders and cerebral disorders. Sedative (calming), mild anxiolytic (anti-anxiety) and weak antidepressant effect, reduces anxiety, fear, emotional tension, enhances the action of antidepressants. Has some neuroprotective properties, improves memory and associative processes. Glycine is a component of many proteins and biologically active compounds. Of glycine in living cells synthesized porphyrins and purine bases. Glycine is also a neurotransmitter amino acid. The receptors for glycine are found in many parts of the brain and spinal cord and have a "braking" effect on neurons, reduce the allocation of neurons excitatory amino acids. Easily penetrates most body fluids and tissues of the body, metabolized to water and carbon dioxide, its accumulation in the tissues does not occur. Currently increased interest in complex preparations, obtained by the synthesis of minerals with amino acids, forming the so-called biocoordination connection - glycine chelates, this is the best - glycinate copper. As such, the trace element and amino acid are easily absorbed in the gastrointestinal tract and enhance the action of each other (C. I. Dorozhkin, 2000). Their functional feature is the ability to form a chelate structure and participate in metabolic reactions. Coordinated group significantly change the chemical properties of the metal. Metabolic pathway for trace elements in the human body is strictly deterministic. The flow of information that defines the metabolism of proteins and amino acids, is correlated with the flow of information for mineral metabolism. Essential role of biogenic metals play for the normal function of the endocrine system, as well as a number of hormones prostate cancer (RJ. Henkin, 1976; K. Burger, 1979). Glycinate copper has anti-proliferative, anti-inflammatory, reduces prostatic hyperplasia, normalizes its functions, participates in the regulation of hormonal balance in the body.

- Vitamin E was isolated from the oil of germs of wheat and was named tocopherol. The most biological active α-tocopherol. Vitamin E natural (d-alpha Tocopheryl acetate). The proposed product contains 50 IU (IU) that the Converter International Units corresponds to at 36.76 mg (mg). The mechanism of action of tocopherol is the biological EN what oxidants. It inhibits, free radical reactions in cells and thus prevents the development of a chain reaction of peroxidation of unsaturated fatty acids in the lipids of biological membranes and other molecules, such as DNA. Tocopherol increases the biological activity of vitamin a, protecting it from oxidation of unsaturated side chain. Vitamin E acts as an antioxidant, preventing the formation in the cells of toxic products of lipid peroxidation, is involved in the biosynthesis of heme and proteins, cell proliferation, and other critical processes of cellular metabolism. Vitamin E improves oxygen consumption by the tissues of the body. Has angioprotective action affects the tone and permeability of blood vessels, stimulates the formation of new capillaries. Tocopherol is required for normal reproductive processes: fertilization, fetal development, formation and functioning of the reproductive system. Vitamin E - antioxidant supports hormonal balance. At deficiency of vitamin E increased permeability and capillary fragility in men is decreasing sexual function. After absorption in the intestine most tocopherol enters the lymph and blood, rapidly distributed in the body tissues, with preferential accumulation in the liver, muscles, adipose tissue. The maximum concentration of the Reparata is defined in the adrenal glands, the pituitary gland, sex glands, myocardium. Indications: dysfunction of the male reproductive system, severe physical illness, a period of increased physical activity, diseases in which the necessary antioxidant therapy.

- Glycinate zinc - biocoordination connection, biogenic metal. Zinc is part of enzymes, is a necessary element for the development of the reproductive organs. Helps to maintain the immune response. Plays an important role in the normalization of the metabolism of the pancreas and prostate. Zinc supports the activity of over 100 enzymes associated with energy metabolism, protein synthesis, heme biosynthesis, transport of carbon dioxide and many other biochemical reactions. Helps normalize the function of the prostate by blocking aromatase enzyme. 50-67% of men suffer from zinc deficiency. Zinc is involved in virtually all stages of cell growth. It is necessary to work more than 300 different enzymes. In the adult human body contains a rather large amount (2-3 g) of zinc. Most of it is concentrated in the bones and skin. The level of zinc is highest in semen and prostate gland. Zinc is found in organs and tissues mainly in organically bound form in the form of easily dissociable compounds with amino acids (in this case with what licina, glycinate zinc and protein. Great biological role of glycinate zinc in growth, development, sexual maturation and maintenance of reproductive function. It is essential for normal functioning of the pituitary, thyroid, pancreas and prostate glands. Under the influence of its compounds increases the activity gonadotropic pituitary hormones. The barrier function of the prostate is associated with the content of zinc. Glycinate zinc has in vitro antibacterial effect on gram-positive and gram-negative bacteria. It is known that the prostate is the most rich in zinc accumulates zinc and its antibacterial activity is associated with the presence of free zinc. In addition, the gland is formed zinc-peptide complex, which plays the role of prostatic antibacterial factor (Stamey 1968, Marmar 1975, Fair&Wehner 1976, Fair&Parrish 1981). The prostate is the level of zinc is recovered when it is received.

- L-glutamine is a substrate amino acids - glutamine. Glutamine is more than 50 percent of the amino acid composition of the body and is critical of the "interchangeable" (synthesized in the body) amino acids. Cells of the immune system, sex glands, the pancreas, the kidneys need the intake of this substance. Glutamine is a potent immunostimulant, actively participates in the processes of regenera the AI tissues. High concentration in the plasma necessary for the successful functioning of the immune system (as a substrate in the form of L-glutamine). However, almost all of glutamine from food, is used by the cells of the small intestine. Glutamine improves brain function and mental activity. Promotes protein synthesis in the body. Strengthens the immune system. Has a detoxifying effect. Is an anti-stress factor. Glutamine is the most common amino acid in the human body: it is 25% of the total number of amino acids and up to 60% of the free amino acid pool. Glutamine is conditionally essential amino acid because under intensive exercise, in conditions of stress, illness, diet, hospitalization, surgery, chemotherapy, muscle and immune system need such large quantities of glutamine (up to 20-40 g / day), which the body cannot produce by itself, require additional dietary. Functions of glutamine diverse. Glutamine is the major building material for cells of the immune system; it increases the immune system's response in case of severe infections, cleanses the body of ammonia, a toxic product of protein metabolism. Glutamine is involved in the formation of a number of vitamins, neurotransmitters and other substances involved in biochemi the mini-processes, serves as a source of energy for brain activity, has a strong anti-stress action. Glutamine is one of the few amino acids that increase the synthesis of hormones in the prostate gland.

L - Arginine is a form of existence in the human body from the amino acid Arginine. Arginine has excellent psychotropic effect, causing an increase in the concentration of somatotropic hormone (STH) - growth hormone. Growth hormone is secreted by the pituitary gland and improves resistance to disease, promotes tissue repair. In blood and lymph Arginine circulates in the form of L-Arginine. This amino acid helps to improve mood, making people more active, enterprising and hardy. Slows the growth of tumors, including malignant. In mechanisms of this phenomenon involved the ability of arginine to activate antitumor cytotoxicity of macrophages; to increase the number and functional activity of T-helper cells - the main component in the development of the immune response; to increase the number and activity of NK (natural killer) and LAK (lymphokine-activated killer cells) in their direct anti-aggression. Arginine is used for the prevention of atherosclerosis, improve the rheological properties of blood. It prevents the formation of blood clots and adhesion of the clot on the inner wall art is s - this reduces the risk of blood clots and atherosclerotic plaques. Arginine is used to increase the cleaning capacity of the kidneys for excretion of end products of nitrogen metabolism. Semen is very rich in Arginine, is effective in the stimulation of spermatogenesis, which is used to treat infertility in men. L-Arginine can increase the strength and duration of the blood supply of the penis in men, prolonging the time of sexual intercourse, increases the pleasurable sexual sensations and orgasm makes a long and deep.

- L-Alanine is a nonessential amino acid (L-levogyrate isomer) in this form circulates in the body. Reduces the risk of stone formation in the kidneys, regulates the functions of the immune system. Alanine is actively involved in the mechanism of regulation of the biosynthesis of amino acids: stable concentrations of alanine and glycine in the cell have a great influence on the synthesis and metabolism of glutamine. Alanine is glycogenic as a source of energy reserve of glucose. Alanine - aliphatic amino acid. Alanine is easily converted in the liver into glucose and Vice versa. This process is called glucose-alanine cycle and is one of the major pathways of gluconeogenesis in the liver. L-Alanine is a part of many proteins, easily incorporated into metabolic processes uglev the Dov and organic acids, in the body can be synthesized from pyruvic acid. Participates in the detoxification of ammonia generated in the process of inflammation, which reduces swelling of a sore and painful symptoms. Alanine is an important source of energy for the brain and Central nervous system; strengthens the immune system by producing antibodies; actively participates in the metabolism of sugars and organic acids. Synthesized from branched chain amino acids (leucine, isoleucine, valine). Alanine can be raw material for the synthesis of glucose in the body. This makes it an important energy source and regulator of blood sugar levels.

- Fillers. Corn starch is a natural substance, carbohydrate polymer, which consists of two structurally different fractions: amylose and amylopectin. Starch as a natural polymer, is one of the main organic sources of raw materials for the food, chemical and pharmaceutical industries. In the manufacture of starch genetically modified raw materials are not used. Corn starch highest grade has no room and declared as corn starch. Physico-chemical properties: moisture content,% not more than 13,0; mass fraction of total ash (calculated on the dry matter),% not more than 0.11; mass fraction of protein (in terms of dry matter), % - less than 0,40. Without kosny, amorphous white powder, insoluble in cold water. Under the microscope it is seen that this granular powder; compacting the powder of starch in his hand, he produces a characteristic "squeak", caused by the friction of the particles.

Medicinal properties: starch is a product of partial hydrolysis of linear polysaccharides improves digestion, stimulates the metabolism of bile acids and has a beneficial effect on the nervous system and cholesterol metabolism, helping to eliminate cholesterol from the body. Corn starch is needed to supply nerve cells and muscle fibers.

Corn starch is most appropriate as a means of transport (binding medium), and a filler in the pharmaceutical industry. Functional properties of corn starch as a filler encapsulated dosage forms: attached crumbling properties of the drug, hygroscopic properties, properties of baking powder; maintains viscosity and moisture content of the dosage form.

Talc is hydrochloricum. Talc is a natural mineral, and rock, formed by this mineral.

Chemical formula talc - Mg3(Si4O10) (OH)2. Occurs in nature in serpentine and olivine rocks with admixture of quartz, anthophyllite, tremolite. THE 5727-002-10733471-99. Used in pharmaceutical production as ispolnitel. The physical properties. Crystals or powder-like mass of white and light-green color. The particles have a different shape with a predominance of squamous. Advantages of talc are: facilitating ingestion of solid medicines, reduces friction, antibacterial, soft, inert filler, has a high absorbent properties.

The claimed means tested on 30 volunteers, BPH patients, and 30 healthy volunteers, patients with chronic prostatitis. The average age of the patients was 63.5±2.4 years. In 16 (53.3 percent) of the 30 patients of BPH were identified comorbidities, among which was dominated by diseases of the cardiovascular system (coronary heart disease, hypertension stage I-II). All patients of BPH was monitored as an outpatient and had before treatment moderately pronounced symptoms of the disease. All patients recorded symptoms of disorders of urination and reduced quality of life scale IPSS-QOL, was conducted and digital rectal transrectal ultrasound of the prostate, uroflowmetry and determination of residual urine volume. Performed sampling of biological materials for the General analysis of urine and determine the level of PSA in the serum.

Scale IPSS (International Prostate Score option) allows AEC to assess the severity of symptoms in patients with impaired urination. The number of points the doctor determines the severity of symptoms in the patient and selects one or the other type of treatment. As an additional method used definition of quality of life index. The results of the questionnaire scales IPSS can be fully interpreted only on the reception of doctor who before giving any evaluation will study the complaint and history of the disorder of a patient, shall examine him, will conduct other tests and studies aimed at identifying causes of disorders of urination. Application form international system total evaluation of diseases of the prostate in points (1-PSS) includes the following questions:

1. How often in the past month have You had a sensation of incomplete emptying of the bladder after urination?

2. How often in the past month have You had the need to urinate more frequently than 2 hours after the last urination?

3. How often in the past month You have had intermittent urination?

4. How often in the last month You have been hard to temporarily refrain from urinating?

5.How often in the past month have You had a weak stream of urine?

6. How often in the past month have You had to naturopathica to begin urination?

7. How often in the last IU is ACA You had to get up at night from the bed, to urinate? The answer for each question:

Less than 1 time of the five - 1 point.

Less than half of the cases - 2 points.

In about half of cases - 3 points.

More than half of the cases - 4 points.

Almost always 5 points.

8. Quality of life due to disorders of urination.

- How would you feel if You had to live with that You have problems with urination until the end of life? The index measuring the quality of life L=:

- perfectly - 0 points;

- well - 1 point;

- satisfactory - 2 points

- mixed feelings - 3 points;

- unsatisfactory - 4 points;

- poorly - 5 points;

- very badly - 6 points.

Total score no I-PSS=

from 0 to 7 speaks of minor violations,

from 8 to 19 - about potencial,

from 20 to 35 indicates severe symptoms.

Prior to the study was a comprehensive examination of each patient using combined urodynamic studies, electromyography of the pelvic floor and MRI of the lumbosacral spine, which allowed to set at 92% signs of pseudodictionary external urethral sphincter: increasing the maximum be pressure to 137 cm water.article (+23%), pressure closing the urethra up to 158 cm water.article (+17.7 percent). All this was observed by the increasing amplitudes of the EMG potential of the pelvic floor muscles in the phase of emptying up to 40 mV (+75%) and could contribute to the development uretroprostaticheskih reflux and pain. In 58% of patients when MRI revealed different changes of the spine in lumbo-sacral region, including spinal hernia, meningomyelocele, myelodysplasia. The study of the mental status of the patients has led to the understanding of the contribution of psychosomatic disorders in the pathogenesis of the disease. Among patients with chronic prostatitis frequent finding was the depression.

It has been proven that the drug "Apostol-400 provides an organotropic action, it also has anti-inflammatory and immunomodulatory effects, effect on hemostasis, improves microcirculation in the affected organ and effective in patients with chronic prostatitis, including the combination of chronic prostatitis with BPH the duration of treatment is 60 days. Observed patients received "Apostol-400 capsules continuously for 60 days. The drug was appointed with the following clinical indicators of the disease: 1) the sum of the scores of symptoms of the disease according to the International scale IPSS averaged a 13.9±2.1 for the fluctuations of this indicator from 10 to 17.2) index measuring the quality of life QOL was on average of 3.8±0,4; 3) the maximum speed of urine flow (Q max) according to uroflowmetry was equal to 9.3±0.9 ml/s in case of fluctuations of this indicator from 6 to 13 ml/s; 4) the amount of residual urine in the urinary bubble is in the middle was 65.5±12.9 ml in case of fluctuations of this indicator from 36 to 80 ml; 5) the volume of the prostate on average amounted to 48.5±5.5 cm3for variations of this index from 40 to 57 cm3; 6) the level of prostate specific antigen (PSA) on average was 3.1±0.2 ng/ml in case of fluctuations of this indicator from 0.4 to 4.0 ng/ml On the basis of medical history, tests, and transrectal ultrasound in 23 (76.7 percent) of the 30 patients of BPH was diagnosed with concomitant chronic prostatitis. In the study did not include patients with other urological diseases involving disorders of urination (e.g., overactive bladder, sclerosis of the prostate, bladder stones, prostate cancer, stricture of the urethra), as well as patients who needed surgical treatment of BPH, in patients with the expressed violations of function of kidneys and/or liver and/or other vital organs, accompanied by violation of their functions. The experience with the drug included 4 visit patients with BPH to the doctor. At the first visit after diagnosis, patients received Apostol-400 for 30 days. The second visit was conducted after 30 days from the start of study drug, and the patients received the drug for another 30 days. The third visit was held within 60 days from the beginning of the experience with the drug, which evaluated the effectiveness of the treatment. Che the fourth patient visits were conducted within 120 days from the start of treatment, i.e., after 60 days after its completion, which were evaluated long-term results of treatment of patients with BPH and chronic prostatitis drug "Apostol-400". As a result of the treatment was that all 30 patients with BPH and chronic prostatitis, receiving "Apostol-400" within 60 days after the completion of treatment noted a positive effect. This pronounced positive effect noted 8 (26,7%) patients, good effect - 12 (40%) patients, satisfactory - 10 (33.3%) patients. In table 1 the results of treatment of patients with BPH and XP. prostatitis drug "Apostol-400" according to the criteria recommended by the International Advisory Committee of BPH. By the end of the drug all the clinical indicators of the disease has improved.

Table No. 1
The results of drug treatment "Apostol-400".
Criteria for evaluation of treatment resultsSource data (first visit)After 30 days of treatment (second visit)After 60 days of treatment (third visit)60 days after completion of treatment (visit Thursday is rty)
1. The sum of the scores of symptoms on a scale IPSS13,9±2,111,8±2,39,7±1,99,7±1,7
2. Index quality assessment3,8±0,43,0±0,72,6±0,52,6±0,4

life QOL (points)
3. The maximum urine flow rate (Q max) (ml/sec9,3±0,910,5±0,612,9±0,414±0.7
4. The amount of residual urine in ml65,5±12,942,4±10,533,8±9,125,6±7,5
5. The volume of the prostate in cm348,5±5,547,8±6,144,2±3,742,2±3,8
6. The level of prostate specific antigen (PSA) in ng/ml3,1±0,23,0±0,12,9±0,2

So, the average score of the symptoms of the disease according to the International scale IPSS after 30 days of treatment decreased from 13.9±2,1 to 11.8±2.3 points, i.e. by 2.1 points, and 60 days of treatment is to 9.7±1.9 points, i.e. by 4.2 points. 60 days after completion of the treatment was the same (9,7±1,7) level score of symptoms, and by the end of treatment. In patients with BPH receiving "Brostol-400, which revealed a statistically significant improvement in quality of life. The average value of the indicator of quality of life to the 30-th day of treatment decreased from 3.8±0.4 to 3,0±0.7 points, and to the 60-th day of treatment to 2.6±0.5 points. The quality of life remained at the same level (2,6±0,4 points) and 60 days after completion of treatment.

The maximum urine flow rate after 30 days of drug treatment, "Apostol-400" increased from 9.3±0.9 to 10,5±0.6 ml/s, and after 60 days of therapy is to 12.9±0.4 ml/sec (i.e., 3.6 ml/s). This metric clinical course of the disease even more significantly improved after 60 days of treatment Apostol-400", making of 14.0±0.7 ml/s In patients with BPH receiving "Apostol-400, which decreased the amount of residual urine. If before treatment the mean value of the residual urine volume was 65.5±12.9 ml, then after 30 days of treatment - 42,4±10.5 ml after 60 days of treatment of 33.8±9.1 ml, and th is ez 2 months after discontinuation of the drug - 25,6±7,5 ml In patients receiving Apostol-400 volume of the prostate in patients with BPH decreased only after 60 days of treatment - from 48.5±5.5 to 44,2±3,7 cm3and remained at the same level within 60 days after the end of treatment.

The level of prostate specific antigen in patients with BPH in patients receiving "Apostol-400" was changed slightly.

None of the 30 we observe BPH patients in the treatment process "Apostol-400" no adverse events were observed, which indicates a good tolerability and safety of the drug.

When analyzing the study results proved that the drug "Apostol-400" appointed within 60 days, has a positive effect on subjective and objective symptoms of BPH. The drug significantly reduces clinical manifestations of the disease (average score of symptoms according to the International scale IPSS by the end of treatment was decreased by 4.2 points from 13.9±2,1 to 9.7±1.9 points) and improves the quality of life. There is a strong positive dynamics of uroflowmetry (maximum urine flow rate after treatment has increased by 3.6 ml/s from 9.3±0,9 to 12.9±0.4 ml/s). In patients with BPH on treatment "Apostol-400" significantly decreased the amount of residual urine (65,5±12.9 ml up to 33.8±9.1 ml by the end of treatment). On a background of reception of a preparation identified and moderately pronounced decrease in the average volume present the preliminary gland (48,5±5.3 cm 3before the start of therapy and 44,2±3,7 cm3by the end of treatment). Transabdominal ultrasound examination of the prostate performed on the machine company "Kontron" (France) and uroflowmetry apparatus DANTEC, Denmark). Determining the concentration of testosterone in serum and in the ejaculate and cortisone in serum of patients with chronic prostatitis was performed using enzyme immunoassay systems "Steroid ELISA testosterone" and company "Alkor BIO" (Russia, St. Petersburg). The content of prolactin, estradiol, LH, FSH was determined with fluorescent analysis of blood serum using sets "Amerlite prolactin-30", "Americacredit", "Amerlite LG-30", "Amerlite FSG company Amersham (UK). The activity of lactate dehydrogenase (LDH), acid phosphatase (EC) and alkaline phosphatase (alkaline phosphatase) in the ejaculate investigated biochemical analyzer FP-900 firm Labsystems (Finland) using sets: for LDH - firm "Cormey (Poland), for KF and alkaline phosphatase - "Lachema (Czech Republic). The content of fructose and citric acid in the ejaculate was determined by the colorimetric method. The influence of "Apostola-400" on the activity of the inflammatory process in chronic prostatitis is confirmed by normalization of leukocytes in the ejaculate in most patients, a reliable decrease in the concentration of IgG, IgA, sIgA and interleukin-8, as well as significant increase in the end of the ation of citric acid and KF in the ejaculate (table.2). It should be noted that after treatment was typical and significant decrease in the relative amount of immobile sperm, which also indicates the suppression of the activity of inflammation (table.2). Therefore, reducing the activity of inflammation in the prostate and restoring the activity of the cells of the prostate gland, "Apostol-400" and improves the performance of the ejaculate. Immunological screening of patients after treatment "Apostolos-400" revealed an increase in the absolute number of lymphocytes with the phenotype CD3+ and CD2+DR+, the change in the ratio of the content of the lymphocytes with the phenotype CD4+ and CD8+ in the direction of increasing the number of the first (PL.3). After treatment, found an increase in the content of b-lymphocytes and the normalization of relations subpopulations of b-cells by reducing the number of b-lymphocytes with receptors IgM+ and IgA+. The decrease in the migratory activity of monocytes and the absorption capacity of neutrophils after treatment "Apostolos-400" evidence of decreased activity of the inflammatory process (table.3). The influence of "Apostola-400" on indicators of humoral immunity was manifested in the reduction of the concentration of IgA.

Table 2
The impact of APR the table-400" macro microscopic, biochemical and immunological parameters of ejaculate in patients with chronic prostatitis (M±M).
IndexPatients with chronic prostatitisThe control group
before the treatmentafter the treatment
pH units7,39±0,167,49±0,077,51±0,05
Viscosity, cm0,36±0,190,19±0,090,15±0,05
The number of leukocytes, '106/l1,3±0,40,5±0,20,3±0,1
Concentration of spermatozoa, '106/lto 75.7±15,6116±7,1120,9±6,8
The relative amount of immobile sperm, %43,5±6,624,3±5,923,9±7,8
The relative number of pathological forms14,2±3,9 6,1±1,86,8±3,2

sperm, %
Citric acid, mmol/l18,6±1,925,5±2,627,3±2,5
Fructose, mmol/l26,2±1,027,4±1,328,3±1,5
Acid phosphatase, '105/l19,7±1,88,5±1,28,1±2,7
Alkaline phosphatase, U/l198,5±33,5184,5±27,1190,9±15,5
Lactate dehydrogenase, U/l2006±661742±1211514±268
Interleukin-8, PCG/ml4317±365973±213605±176
IgG, g/l0,76±0,220,36±0,090,37±0,08
IgA, g/l1,24±0,210,72±0,110,66±0,17
IgM, g/l0,93±0,150,81±0,170,74±0,19
IgsA, g/lof 2.26±0,111,36±0,211,48±0,38

Table 3
The influence of "Apostola-400" on immunological parameters in peripheral blood of patients with chronic prostatitis (M±M)
IndexPatients with chronic prostatitisThe control group
before the treatmentafter the treatment
Spontaneous migration of granulocytes,.E.4,65±2,09of 3.46±0,182,95±0,53
The index of inhibition of migration of granulocytes, %27,7±23,534,3±17,855,0±12,0
Spontaneous migration of MES is the nuclears, .E.of 8.28±2,683,47±0,564,15±0,68
The index of inhibition of migration of mononuclear cells, %31,7±17,633,8±9,441,0±7,5
Phagocytosis of neutrophils, %46,9±8,923,9±1,924,5±2,4
Complement, CH50 units21,3±1,3of 21.9±0,822,0±0,5
Circulating immune complexes.E.0,07±0,030,06±0,040,07±0,05
Lymphocytes, %34,8±1,236,8±2,839,0±1,3

Cells with the phenotype CD3+, %57,5±2,5of 56.4±2,155,1±2,5
Lymphocytes with the phenotype of CD2+DR+% 22,7±0,929,4±3,431,9±1,3
Lymphocytes with the phenotype of CD+, %27,1±2,230,6±3,033,8±3,3
Lymphocytes with the phenotype CD8+, %24,3±1,721,1±2,322,3±1,20
B-lymphocytes with Ig+ receptors %17,2±2,018,8±1,724,4±2,1
B cells from IgM+ receptors %8,2±1,27,0±1,46,9±0,7
In cells with IgG+ receptors %4,6±0,44,6±0,54,5±0,6
In cells with IgA+ receptors %3,5±0,42,8±0,32,3±0,3
IgA, g/l5,75±1,341,75±1,342,15±0,25
IgM, g/l1,31±0,521,23±0,471,63±0,16
IgG, g/l13,4±1,7111,7±2,3312,3±0,97
sIgA, g/l4,13±2,62,83±1,81,24±1,21

Detected in drug treatment "Apostol-400" positive dynamics in the clinical course of BPH should explain the specific direct and indirect organotropic action of this drug, etiopathogenetic mechanism of its action and reduced proliferative activity of the cells of the prostate, reduce swelling and decrease the activity of the inflammatory process in the prostate gland by improving the microcirculation.

It is important to note that 75-95% of patients of BPH takes place and concomitant chronic prostatitis, which aggravates the clinical course of the underlying disease. "Apostol-400 contributes to reduction activity accompanying inflammatory process in the prostate gland and thereby increases the effectiveness of treatment. Positive changes in the clinical course of the disease remain within 2-6 months after taking the drug, which confirms the high effectiveness evaluation "Apostol-400" in patients with BPH.

Conclusion. Obtained in the course of this study, the result of which allow us to recommend the drug "Apostol-400", for use in patients with BPH. The drug is more effective in patients with concomitant BPH and chronic prostatitis. In the treatment of patients with BPH "Apostol-400" it is advisable to appoint at least 2 months continuously. This term treatment can significantly improve the effectiveness of treatment, to improve the quality of life and reduce the volume of the prostate gland. In addition, "Apostol-400" a beneficial effect on the nervous and cardiovascular system, not identified in the testing side effects.

"Apostol-400 was tested on volunteers in a placebo-controlled study, which was attended by a total of 40 people. Patients who "Apostol-400 and placebo, were divided into two almost equal groups. 40 35 diagnosed with BPH. In these studies lasting 1 to 3 months was significantly demonstrated the clinical efficacy of the drug compared with placebo. The frequency of nocturnal urination decreased by 33-46%, day pollakiuria - 11-20%, a Qmax increased by 29-50%, which was significantly higher than in the placebo group, where these indicators were 15-18%, 1-3% and 5-9%, respectively.

"Apostol-400 acted as an effective means of eliminating dysuria. The study showed that within 1 month dysuria decreased in 31% of the treated "And is rostol-400" compared with 16% in the placebo group. On the background of the drug residual urine volume decreased relative to the initial values up to 50%, and was statistically significant compared with the placebo group, which saw not only decrease, but also the increase in this index.

Of great interest are the results of self-assessment by patients efficacy "Apostola-400" in comparison with placebo.

According to patients, 88% of them on the background of the drug showed improvement of symptoms, while only 12 percent cited a lack of response or deterioration. In the placebo group, these values amounted to 68% and 32%, respectively. Similar statistically significant results were obtained when assessing the condition of patients attending physicians. Up to 90% of patients receiving "Apostol-400", were regarded by them as having improvement or significant improvement, compared with 36% in the placebo group. Thus, the placebo-controlled studies "Apostola-400 has demonstrated clinical efficacy, which is a marked reduction of symptoms and improvement in urodynamic parameters.

Get the tool in encapsulated dosage form. Manufacturing process flow mass for encapsulation involves several steps and is carried out automatically one after the another by means of corresponding actuators.

The stage of preparation of raw materials. At this stage, crushed and sieved all the ingredients that are included in a capsulated form means: prazosin, Diisopropylamine dichloroacetate, afobazole, glycinate copper. Vit E (d-alpha tocopherol acetate), glycinate zinc, L-Glutamine, L-Alanine, L-Argin. The raw material is ground in a rotary mill and sieved by the vibrating screen. Seek substance crystals set in flowability and humidity. The result is a crystalline drug substance with crystals sociometrically forms, freely poured from a funnel and as a consequence easily subjected to volumetric dosing. The crushed raw materials are weighed based on 1 capsule in mg doxazosin, Diisopropylamine dichloroacetate, afobazole, glycinate copper, Vit E (d-alpha tocopherol acetate), glycinate zinc, L-Glutamine, L-Alanine, L-Arginine and excipients: corn starch, talc.

The weight of the raw materials produced in the weight rooms using weights, all data is logged. The stage of obtaining the mass of capsules. The mixture of powders is carried out in a mixer, using a vacuum system boot into the installation. The step of filling hard gelatin capsules with powder; packing capsules in blister packaging (blister) with the subsequent packing blisters in a cardboard box. Hard gelatin capsules are designed for dosiro is of free-flowing powdery substances. They have the shape of a cylinder with hemispherical ends and consist of two parts: body and lid; both parts must be free to enter one another without forming gaps. Hard capsules are two-piece structure made in advance, and filling their medicinal substances carry out as necessary. Encapsulated drugs have a number of advantages and positive characteristics. These include, in particular, include:

- High accuracy of dosing placed in them drugs.

- High bioavailability. Capsules disintegrate faster in the body than tablets, and their nespracovane solid content faster and easier absorbed. Pharmacological action of medicinal substance is manifested through 4-5 minutes

- High stability. Medicinal substance in the capsules are protected from various adverse environmental factors - exposure to light, air, moisture, mechanical effects - thanks to the shell, which provides a relatively high air-tightness and insulation components. Therefore, in the manufacture of capsules, you can avoid the use of antioxidants or stabilizers, or to reduce their number.

- Corrective capacity - eliminates unpleasant taste and odor of drugs, which is especially important in Pediatrics.

- Use fewer excipients in the manufacture of capsules than, for example, in the manufacture of tablets.

Example 1. According to the composition of the proposed tools, source the ingredients to grind on a rotary mill, screened by vibrating screen. Measured in bulk seen mg.:

Diisopropylamine dichloroacetate10,0
afobazolethe 9.7
glycinate copper200,0
Vit E (d-alpha tocopherol acetate)36,70
glycinate zinc30,0


corn starch22,91

The powders were mixed in a mixer, using a vacuum is the recalls. From the mass of the software received capsules.

Example 2. In this way received capsules of a mixture of powders of mg:

Diisopropylamine dichloroacetate100
glycinate copper200,1
Vit E (d-alpha tocopherol acetate)of 36.76
glycinate zinc30,1
L - Glutamine40,1


corn starch22,93

Example 3. The medical history of the patient X, 58 y.o.

The clinical diagnosis: prostate cancer, stage II.

Of the patient's complaint: Filed complaints about the frequent urge to urinate, especially at night up to 4 times, adnene urination, most of its length, reducing the width and the lethargy of jet remains a feeling of residual urine after urination. Also filed complaints appeared irritability, fatigue, sleep disorders as insomnia and nightmares, increased sweating. Considers himself ill in the course of the year, when first appeared the above complaints, but were less pronounced. Has addressed to the urologist at the place of residence, was diagnosed with prostate cancer, stage II. The proposed hospitalization in the urology Department with the aim of further diagnosis and treatment. At objective examination from the lungs and cardiovascular system revealed no pathology. Status localis. When rectal finger study determined the enlargement of the prostate (prostate size - 4 cm × 4 cm × 5 cm and a volume of 30 ml). The bladder is determined percutere in the form of dullness and by palpation in the form fugolastic spherical formation above the pubis, full, marked bulging of the suprapubic region. Laboratory tests: blood tests clinical, clinical urine analysis, biochemical blood analysis - conclusion: no changes. Ultrasound: the bladder is deformed, knotty. The prostate gland with smooth, clear contours, the size of the prostate and 4 cm × 4.4 cm × 5.2 cm, and the volume of 34 ml of Seminal vesicles of the usual dimensions are not changed. The bladder is filled satisfactorily. Prostatorrhea. Excretory urography showed the volume of the bladder 365 ml, after an arbitrary bladder emptying in addition is made to the descending cystogram - the amount of residual urine 65 ml Prostate specific antigen (PSA)for admission to 15 ng/ml Patient received within 60 days of the drug "Apostol-400". After 60 days of treatment with rectal finger study of prostate size 3 cm × 3 cm × 4 cm and a volume of 25 ml. Consistency gland uniform, photoelasticity; the mucous membrane of the intestine above the prostate gland mobile palpation painless. Laboratory tests: blood tests clinical, clinical urine analysis, biochemical blood analysis - without a pathology. Prostate specific antigen 10 ng/ml Ultrasound: the bladder without features. The prostate gland with smooth, clear contours, the size of the prostate - 3.5 cm × 3.0 cm × 4.4 cm, and the volume of 27 ml of Seminal vesicles of normal size are not changed. Prostatorrhea. Excretory urography showed a bladder volume of 300 ml, after an arbitrary bladder emptying in addition is made to the descending cystogram - the amount of residual the eyes 35 ml. After examination exhibited clinical diagnosis: prostate cancer, stage I.

Example 4. The medical history of the patient U. 43 years. Diagnosis clinical: Chronic abacterial prostatitis.

The patient complains of pain that is dull, aching character, is localized in the projection of the perineum, scrotum, testicles, penis, lower abdomen. The pain is crushing in nature. The patient notes frequent urination especially at night, feeling of incomplete emptying of the bladder, pain during urination, fever up to subfebrile figures. In the last days feels causeless anxiety and depression. Considers himself ill for 3 months, during this period was twice observed exacerbation of this disease. Surveyed, treatment received as an outpatient. Is registered with a urologist. When rectal finger examination of the patient is determined by the enlargement of the prostate 4.5 cm × 4 cm × 5.5 cm, with a convex, smooth surface. Consistency soft, testovaty, smooth accurate contours, mobility of the rectal wall above it saved. Palpation of the prostate is painful. Ultrasound of the prostate gland through the rectal sensor (prostate transrectal us):heterogeneous echostructure, hyperechoic areas in periurethral region, a diffuse decrease in echogenicity prostate VC is PS. Length - 4.5 cm, width 4.5 cm, thickness - 5.5 cm, the volume of the prostate 30-35 ml Average volume of residual urine - 20,5 (in the norm of 6.1±1.9 ml). Uroflowmetry. The maximum volumetric rate of urination, duration and volume of urination - 10 ml/sec (normally no less than 15 ml/sec). The acid level of the blood - 19,7 U/l (norm - 8,1±2,7 U/l); alkaline phosphatase blood - 198,5 U/l (normal is 180±2.5 U/l). Prostate specific antigen (PSA), 20 ng/ml for All other clinical and biochemical analyses without pathology.

The patient within 60 days of taking the drug, "Apostol-400". After taking the drug stopped the pain, night urination, feeling of incomplete emptying of the bladder, pain during urination, became less frequent daytime urination, normal body temperature, improved mood and well-being. The patient leads an active life. After 60 days of treatment with rectal finger study of prostate size - 3.5 cm × 3.5 cm × 4.5 cm, and a volume of 25 ml. Consistency gland uniform, photoelasticity; the mucous membrane of the intestine above the prostate gland mobile palpation painless. Laboratory tests: blood tests clinical, clinical urine analysis, biochemical blood analysis - without a pathology. The acid level of the blood is 11.0 U/l (norm - 8,1±2,7 U/l); alkaline phosphatase CROs and - 183,5 U/l (normal is 180±2.5 U/l).

Prostate specific antigen - 14 ng/ml.

Ultrasound: the bladder without features. The prostate gland with smooth, clear contours, the size of the prostate - 3.5 cm × 3.0 cm × 4.4 cm, and the volume of 27 ml of Seminal vesicles of normal size are not changed. Prostatorrhea. Excretory urography showed the volume of the bladder 275,0 ml, after an arbitrary bladder emptying in addition is made to the descending cystogram - the amount of residual urine and 10.5 ml. of Uroflowmetry. The maximum volumetric rate of urination, duration and volume of urination - 18 ml/sec.

After treatment achieved a significant reduction of the inflammatory process in the prostate gland, exacerbation translated to remission.

The remedy for the prevention and treatment of prostatitis and benign prostatic hyperplasia, characterized in that it is a composition active substances, including the target of the ingredients in the powder, the following ingredients, in mg/capsule:

dichloracetate 10-100
afobazolea 9.7-10,0
glycinate copper200-200,1
Vit E(d-alpha
tocopherol acetate)36,70-of 36.76
glycinate zinc30,0-30,1
Excipients: corn
starch -22,91-22,93


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FIELD: medicine, pharmaceutics.

SUBSTANCE: what is presented is using at least one protease for producing a drug preparation for treating and/or preventing benign prostatic hypertrophy/hyperplasia wherein the drug preparation is acceptable for the oral administration with at least one protease being specified in a group consisting of plant and microorganism proteases, and with at least one protease being administered in the amount of 1 to 100 mg/kg of body weight, and a respective pharmaceutical preparation.

EFFECT: what is shown is reducing high vascular endothelial growth factor in patient's blood under the action of a mixture of enzymes that makes it possible to inhibit angiogenic growth factors (VEGF), thereby leading to lower vascularisation, and reducing benign prostatic hypertrophy/hyperplasia, with the enzymatic therapy under the present invention having no effect on the normal VEGF level.

13 cl, 7 dwg

FIELD: medicine.

SUBSTANCE: invention refers to medicine, namely urology, and may be used for treating suppurative septic complications of prostate adenoma. For this purpose, with underlying administering antibiotics, ozonised saline solution in the concentration of 3 to 6 mg/l in the amount of 200 to 400 ml is additionally intravenously administered; the therapeutic course is 3-5 injections depending on the patient's state. Besides, ozonised saline solution in the concentration of 5 to 8 mg/l is injected into the bladder in the preoperative preparation period, and from the second postoperative day, saline solution is introduced drop-by-drop in the amount of 400.0 ml daily five times with a two-way flushing system.

EFFECT: method enables reducing the risk of urosepsis, eliminating intoxication and accelerating postoperative wound healing of a BPH bed by anti-inflammatory, detoxification, analgesic action, improved blood rheology and microcirculation, increased local immunity with activated regenerative and reparative processes.

2 tbl, 1 ex

FIELD: chemistry.

SUBSTANCE: invention relates to a compound of formula (1), in which Ar is a group of formula (Ar-1) or (Ar-2), in which R1 is a halogen, R2 is hydrogen, R3 is hydrogen, R4 is hydrogen, alkyl or alkenyl, X is a nitrogen atom or CH, R5 and R6 are each hydrogen and h equals 1; 1 equals 1 or 2; m equals 1 or 2; n equals 0, 1 or 2; o equals an integer from 0 to 3, under the condition that n and o are equal to 0 at the same time. Values of group A are as given in claim 1 of the invention. Described also is a pharmaceutical composition having agonistic activity with respect to 7 serotonin (5-HT4-receptors), which contains a compound of formula (1) and an agent which stimulates enterokinesis or improves functioning of the alimentary canal, which contains a compound of formula (1) as an active ingredient.

EFFECT: novel compounds are obtained and described, which have strong affinity towards 4 serotonin receptors, which are useful as an agent which stimulates enterokinesis or an agent which improves functioning of the alimentary canal.

28 cl, 233 ex, 29 tbl

FIELD: medicine.

SUBSTANCE: invention relates to medicine, namely to urology, and can be used for treatment of chronic abacterial prostatitis in men, which is not connected with dysfunction of urethral sphincter. For this purpose, efficient amount of fispemiphene is introduced to patient who needs it. Introduction of fispemiphene is performed in amount in the range from 0.1 to approximately 100 mg/kg of body weight.

EFFECT: invention ensures efficient treatment of abacterial prostatitis at the early stage of disease where only histological changes of prostate gland are present without presence of urethral sphincter dysfunction, with drug fispemiphene, which demonstrates antagonistic activity to estrogen receptors in particular with respect to prostate tissue.

2 cl

FIELD: medicine.

SUBSTANCE: therapeutically effective amount of ethyl methyl hydroxypyridine succinate and calcium atorvastatin, as well as additives in the form of lactose and magnesium stearate are encapsulated in gelatine. Ethyl methyl hydroxypyridine succinate and magnesium stearate is placed into an inner smaller gelatine capsule inside a main outer gelatine capsule containing atorvastatin, lactose and magnesium strearate. The ingredient ratio in the inner capsule makes, wt %: Ethyl methyl hydroxypyridine succinate 96.2-98.6; magnesium stearate 1.4-3.8, and the ingredient ratio in the outer capsule makes, wt %: calcium atorvastatin 10.0-45.0; lactose 52.0-89.0; magnesium stearate 1.0-3.8.

EFFECT: method enables providing the higher pharmaceutical effectiveness of the preparation and prolonging the shelf-life by preventing atorvastatin degradation.

3 cl, 3 tbl

FIELD: chemistry.

SUBSTANCE: invention represents pharmaceutical composition for correction and therapy of manifestations of amyloid intoxication in patients with brain pathologies, which are characterised by the fact that it contains melatonin 3-10 mg and memantine 5-300 mg.

EFFECT: effective treatment of patients, including cases of moderate cognitive disorders.

4 cl, 2 ex, 6 tbl, 7 dwg

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to the pharmaceutical industry, particularly to a method for preparing an agent possessing an antiulcerogenic action. A method for preparing the agent possessing the antiulcerogenic action by extracting the aspen bark in 40% ethanol by the multi-step reverse-flow extraction followed by purification, vacuum concentration and drying in a vacuum chamber; the prepared dry extract is added with the Ludipress extract in the specific environment and used to fill solid gelatine capsules.

EFFECT: preparing the agent possessing the antiulcerogenic action.

15 dwg

FIELD: medicine.

SUBSTANCE: composition containing curcumine, an acid specified in a group consisting of citric acid, malic acid, acetic acid, tartaric acid, lactic acid, alginic acid or a mixture thereof, and an edible emulsifying agent with specific characteristics and taken in a certain amount wherein the above composition is applicable as a therapeutic agent. The composition containing curcumine, the edible emulsifying agent or a mixture thereof, the acid specified in a group consisting of citric acid, malic acid, acetic acid, tartaric acid, lactic acid, alginic acid or a mixture thereof taken in certain proportions, and additionally encapsulated into a gelatine capsule, wherein the above composition is applicable for treating or preventing an inflammation and/or diseases caused by the inflammation.

EFFECT: compositions improve the curcumine bioavailability effectively.

13 cl, 1 tbl, 6 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: perorally delivered pharmaceutical composition contains a compound, which inhibits a protein of family Bcl-2, in particular ABT-263, a slightly soluble in lipids antioxidant, selected from the group, which consists of sulphites, bisulphites, metabisulphites, thiosulphates and their mixtures, and an in fact non-aqueous lipid carrier, which includes a phospholipid, a non-phospholipid surface-active substance and a solubilising component, which includes one or more glycols, glycolides and/or glyceride compounds, where the said compound ABT-263 and the said antioxidant are in a solution in the lipid carrier.

EFFECT: composition is suitable for peroral introduction to an individual who requires it for treatment of a disease, characterised by superexpression of one or some antiapoptotic proteins of family Bcl-2, for example cancer.

28 cl, 2 dwg, 17 tbl, 12 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: present invention refers to a solid pharmaceutical product for oral administration which contains a photosensitiser representing a compound of general formula I:

wherein R1 represents a substituted or unsubstituted unbranched, branched or cyclic alkyl group, and each R2 independently represents a hydrogen atom or optionally a substituted alkyl group or its pharmaceutically acceptable salt, and at least one pharmaceutically acceptable carrier or excipient. The above pharmaceutical product is presented in the form of a tablet, a pill or a capsule having an enteric and gastroresistant coating, or in the form of the tablet or the capsule containing a number of balls, drops, granules or mini-pills with an enteric and gastroresistant coating. The above coating disintegrates in the lower gastrointestinal tract. The invention also refers to using the above photosensitiser in preparing the solid pharmaceutical product applicable in photodynamic treatment or diagnostics of a cancer condition in the lower gastrointestinal tract. What is also described is a photodynamic method of treating or diagnosing the cancer condition in the lower gastrointestinal tract by administering the solid pharmaceutical product containing the photosensitiser.

EFFECT: invention provides photosensitiser delivery to the lower gastrointestinal tract, and homogenous distribution of the photosensitiser in the target region, thereby improving the response to photodynamic treatment or diagnostics.

20 cl, 2 dwg, 2 tbl, 54 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to the field of cosmetology, namely to a cosmetic composition for peroral introduction, which contains a combination of lycopene, vitamin C, vitamin E and at least one polyphenol compound, obtained from pine bark, in which the ratio of weight content of polyphenol compound to the sum of weight contents of lycopene, vitamin C and vitamin E constitutes from 0.3 to 0.7, as s single active ingredient.

EFFECT: invention is intended for prevention and/or treatment of wrinkles in the area of eyes and mouth angles, small wrinkles, eye bags and dark circles under eyes.

22 cl, 2 ex, 11 tbl

FIELD: chemistry.

SUBSTANCE: invention relates to preparation of encapsulated protein-containing products. The method producing protein-containing products involves preparing internal contents with a protein component, followed by encapsulation of the internal contents to obtain a protein-containing product with a shell. Said internal contents have a ratio of protein to salt mixture of (1-11):(1.0-4); the salts used are soluble calcium salts, barium salts or mixtures thereof and pH corrector salts with the ratio (1.0-3.0):(1-2). The internal contents are encapsulated through a sodium alginate solution 0.5…3.0%. Also disclosed is an encapsulated protein-containing product. The product has an alginic shell based on calcium, barium or mixture thereof with the ratio of internal contents to the shell of 100:(20-50), wherein the internal contents have pH 7.5…8.5.

EFFECT: invention enables to obtain an encapsulated protein-containing product which is resistant to breakdown at low pH values and is impervious to pepsinolysis enzymes.

3 cl, 1 tbl, 6 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to chemical-pharmaceutical industry, particularly to a method for preparing a powder. The method involves the stages of providing at least one first ingredient that has a consistence of viscous fluid and that has an initial melting point within the temperature range of 15°C to 40°C, providing at least one second ingredient that has a melting point, particularly within the range above an ambient temperature up to 120°C, preparing a homogenous liquid mixture containing one first ingredient and one second ingredient by mixing and heating the mixture to a temperature or maintaining a temperature of the mixture within the range above the melting point. Supplying the liquid mixture to an irrigation hardening unit and extracting the powder prepared by irrigation hardening. In addition, the present invention refers to the method for preparing the solid dosage form containing the powder prepared by the method described above.

EFFECT: improvement of the method.

17 cl, 6 ex, 2 tbl

FIELD: chemistry.

SUBSTANCE: invention relates to novel omega-3 lipid compounds of general formula (I) or to their pharmaceutically acceptable salt, where in formula (I): R1 and R2 are similar or different and can be selected from group of substitutes, consisting of hydrogen atom, hydroxy group, C1-C7alkyl group, halogen atom, C1-C7alkoxy group, C1-C7alkylthio group, C1-C7alkoxycarbonyl group, carboxy group, aminogroup and C1-C7alkylamino group; X represents carboxylic acid or its carbonate, selected from ethylcarboxylate, methylcarboxylate, n-propylcarboxylate, isopropylcarboxylate, n-butylcarboxylate, sec-butylcarboxylate or n-hexylcarboxylate, carboxylic acid in form of triglyceride, diglyceride, 1-monoglyceride or 2-monoglyceride, or carboxamide, selected from primary carboxamide, N-methylcarboxamide, N,N-dimethylcarboxamide, N-ethylcarboxamide or N,N-diethylcarboxamide; and Y stands for C16-C22 alkene with two or more double bonds, which have E- and/or Z-configuration.

EFFECT: described are pharmaceutical and lipid compositions, which contain said compounds, for application as medications, in particular, for treatment and/or prevention of peripheral insulin resistance and/or condition of diabetes, for instance, type 2 diabetes, increased levels of triglycerides and/or levels of non-HDL cholesterol, LDL cholesterol and VLDL cholesterol, hyperlipidemic condition, for instance, hypertriglyceridemia (HTG), obesity or condition of excessive body weight, fatty liver disease, for instance, non-alcoholic fatty liver disease (NAFLD) or inflammatory disease or condition.

60 cl, 3 tbl, 65 ex

FIELD: chemistry.

SUBSTANCE: invention relates to bio-compatible conjugated polymer nanoparticle, dicarbonyl-lipid compound, compound in form of vesicles, micelles or liposomes, containing multitude of nanoparticles, including said dicarbonyl-lipid compound, method of treating cancer or metastases, biocompatible polymer, as well as to conjugate. Biocompatible conjugated polymer nanoparticle includes main chain of copolymer, with at least one polymer monomer containing two side chains, selected from the group, consisting of carboxylic acid, amide and ester, and sad side chains are separated from each other by 1-1- carbon atoms, oxygen atoms or sulphur atoms, or their any combinations. Said nanoparticle further contains multitude of side chains, covalently bound with said main chain, with said side chains being selected from the group, consisting of monosaccharides, dicarboxylic acids, polyethyleneglycol and their combinations; and multitude of platinum compounds, dissociatedly bound with said main chain. Multiple platinum compounds are connected with said main chain via at least one coordination bond between carbonyl oxygen of carbonyl or amide group of main chain and platinum atom of platinum compound. Said platinum compound is selected from Pt(II) compounds, Pt(IV) compounds and any their combinations. Invention is also aimed at dicarbonyl-lipid compounds, in which platinum compound is dissociatedly bound with dicarbonyl compound. Invention is also aimed at method of treating cancer and metastases. Methods include selection of subject, requiring treatment of cancer or metastases, and introduction to subject of effective amount of nanoparticles, compounds or compositions of the invention.

EFFECT: obtaining biocompatible conjugated polymer nanoparticles for chemotherapeutic platinum-based preparation.

40 cl, 1 tbl, 29 dwg, 12 ex