Xydiphone-containing rectal suppositories

FIELD: medicine, pharmaceutics.

SUBSTANCE: the present innovation deals with rectal suppositories that contain biphosphonic acids and their pharmacologically acceptable salts applied for preventing and treating diseases caused by affected calcium and magnesium balance in the body. The suggested new suppositories contain 0.1-10 weight% xydiphone and 0.5-10 weight emulsifiers, the rest - the foundation for one suppository of 1.125-2.5 g weight. Rectal xydiphone-containing suppositories could additionally contain medicinal and/or biologically active supplements, for example 0.1-1.0 weight% trisodium salt of phosphonoformic acid as medicinal additive, and, also, biologically active additive chosen out of the group of vitamin B6, B12 or carbon dioxide solution of common camomile, olive oil. The innovation provides the chance to avoid some complications occurred at applying this preparation in known forms and, also, in some cases leads to its increased efficiency.

EFFECT: higher efficiency of application.

4 cl, 4 ex, 1 tbl

 

The invention relates to medicine, namely to pharmaceutical preparations made in the form of suppositories for rectal administration, containing the drug Califon and used for the prevention and treatment of several diseases, for which effective Califon, for example, when the metabolism of calcium in adults and children with urolithiasis, ismetabolites nefropatia, the immobilization osteoporosis, and chronic intoxication with heavy metals.

Known for the ability of pharmaceutical drug Xidian (monosodium, monogalia salt 1-hydroxyethylidene-1,1-bisphosphonate acid) to regulate the metabolism of calcium in the body, which made it possible to use it widely in various fields of medicine, for example in the treatment of bone diseases such as osteoporosis immobilization disorders of calcium metabolism in adults and children with kidney stones, asthma, ismetabolites nefropatia, diseases of the nervous system, pathology of the teeth, and chronic intoxication with heavy metals (Tagatausta, Keepopen, Ayurdeva. Bisphosphonates, properties, structure and application in medicine. M.: Chemistry, 2001). In Russia commercially release of the drug xidian in the form of a 20%aqueous solution according to the technology described in the patent (RU, 1741801, a 61 K 31/00, 1992). This drug in the medical the th practice is applied usually in the form of a 2%aqueous solution and introduced into the body orally or parenterally, and by electrophoresis (Horenko E.V., Magdalou Ressourcement issue of neurology. Dnepropetrovsk, 1994, p.1-5) or a method of applying applications in the composition of ointments or creams (EN, 2101015, a 61 K 31/66, 1998).

A single dose of this drug is injected at the rate of 10 mg/kg weight of the patient depending on the patient's age, weight and type of the disease. However, the known methods of taking the drug often cause unwanted side effects or are characterized by sustained pharmacological effect. This is particularly evident in oral administration of the drug in patients with diseases of the gastrointestinal tract. Oral introduction of califona maximum therapeutic effect is achieved only after 10-14 days. Parenteral and oral administration of the drug is particularly complicated in the case of untreated patients vomiting side and pain effects that often manifests itself in children, as well as the violation of absorption in the gastrointestinal tract.

To eliminate the above disadvantages of califona in the form of liquid funds developed dosage form of rectal suppositories containing 0.1-10 wt.% califona as an active ingredient, and containing 1.0 to 10 wt.% the emulsifier and the rest up to 100 wt.% suppozitornoj basis for the weight of one suppository of 1.0 to 2.5, Preferably the application of the composition californiadreamin suppositories as emulsifiers substances from the group of monoglycerides, ethoxylated lanolin, hydrophobic silicon dioxide, and as the basis for the cocoa butter. Rectal californiadreamin suppositories may further comprise a biologically active and/or medicinal substance in an effective amount of vegetable oil from 1-5 wt.% the total weight of the mixture, preservatives in an amount of 0.01-0.1 wt.% the total weight of the mixture. As a medicinal additive suppositories can contain, for example, chinatravel salt postemergency acid (foscarnet) an effective amount of 0.1 to 3.0 wt.% the total weight of the mixture.

The choice suppozitornoj forms for drug xidian explains the benefits suppozitornoj form as such. As is well known in medical practice, this dosage form has recently become one of the most widely used dosage form because of its high bioavailability, ease of use and more painless form of its introduction into the body than other dosage forms such as solutions. Xidian as other bisphosphonates drugs, as suppozitornoj form up to the present time has not been applied. In General, suppositories as dosage forms are more often used as analgesic, anti-inflammatory, laxative, as a means for treatment of proctologic, acute intestinal, Gris is the same diseases. However, known prior art and suppositories containing medicines on the basis of 1,1-biphenyl-4-acetic acid and its salts, is effective in the treatment of rheumatoid arthritis, osteoarthritis, there are diseases for which treatment including applied and bisphosphonates (EP 0339176, a 61 K 31/19, 1989).

To increase the effectiveness of califona in various diseases developed a new dosage form - rectal californiadreamin suppositories. The scope of califona in the form of a new dosage form of suppositories is the same as for known use of this drug in the form of solutions, in the composition of ointments. However, the use of califona in a new dosage form not only allows you to avoid some of the complications caused when using this drug in known forms, and in some cases leads to higher efficiency and extends the possibility of its application, in particular in pediatric and veterinary medicine. A significant role in the new medicinal product plays concentration of active ingredient in each suppositories. Xidian part suppositories entered as produced by industry 20%aqueous solution in a quantity of 0.1-10 wt.%, that was chosen experimentally based on the drug's effectiveness and structure with the properties of the form. Studies have shown, when the content of califona exceeding 10 wt.%, complicated fabrication process suppozitornoj form stable during storage. Understating the same content of the main component leads to the disappearance of therapeutic effect. Weight of one suppository may vary in the range of from 1.0 g to 2.5 g, which depends on the age and weight of the patient. While suppositories weighing 1.0 g can be used for newborns and infants, for children zapotockogo age, suppositories weighing 1.0-2.0 g - for teenagers and suppositories weighing 2.0 to 2.5 g for adults. In addition califona as main components in the composition rectal suppositories include emulsifiers and suppozitornyj basis. Experimentally it was found that the best compatibility califona based is achieved by using as the basis of cocoa butter. However, as the framework can be applied and Witepsol and solid fat type and compatible with califona basis. Cocoa butter is a long time and are widely used in medical practice suppozitornyj basis and was selected as the optimal basis for califona in the process of studying the impact of substance with preliminary identification of compatibility califona with the proposed basis. As you know, the cocoa butter is p is ironim product with a slightly aromatic odor, melting at 30-34°With an acid number of not more than 2.25 and iodine number 32-38 that meets all the requirements of suppozitornyj the basics. Each suppository given the size and age of the patient includes a base in a quantity sufficient to obtain the suppository mass of 1.0 to 2.5, As shown in clinical studies, the overestimation of the number of bases above the claimed slows the release of the active ingredient and, thus, slows down the healing effect, and reducing the number of bases in suppositories below the claimed causes difficulty in manufacturing suppozitornoj mass and makes it unstable during storage, and may also lead to side effects from excessive content of califona. As another essential component in the composition of new suppositories enter the emulsifier or mixture of emulsifiers. The emulsifier in the composition of the suppositories are needed to increase their viscosity, which contributes to the creation of a stable homogeneous suppozitornoj form. Optimal combination of emulsifiers, in particular monoglycerides, ethoxylated lanolin and hydrophobic colloidal silicon dioxide, often produced under the name "Aerosil". Introduction to new suppositories emulsifiers, in addition, contributes to the increase of bioavailability XI is iPhone due to its lightweight release of suppozitornoj form when introducing it into the body. The list of these emulsifiers does not limit the applicability and the other compatible with califona physiologically acceptable emulsifiers. Emulsifiers are entered in californiaread suppozitornyj form in number, comprising 1-10 wt.% the total weight of the composition. The increase in the content of the emulsifier stated above leads to the increase of viscosity suppozitornoj mass that changes the melting point of the suppository and thus leads to poor efficiency califona in the body by the introduction of a suppository. The reduction or absence in the composition of the emulsifier leads to deterioration of structure-forming properties of the composition. In addition to the main components in the composition of new suppositories can be entered various additives, in particular biologically active additives, such as vitamins, for example vitamins, herbal extracts, such as chamomile, contained, for example carbon dioxide solutions of medicinal plants such as chamomile and drug additives that are compatible with califona for example trinational the salt postemergency acid, known under the trade name foscarnet. The effective number of input foscarnet in new suppozitornyj mass is 0.1-3 wt.% the total weight suppozitornoj mass. The introduction of this drug extends the application but who's suppositories, allow comprehensive treatment of several diseases, including the treatment of viral infections, for example herpes, along with the above diseases, the treatment of which effective Califon. As an additive in the composition of the suppository can also be put vegetable oil in the amount of 1-5 wt.% the total weight of the mixture, for example olive oil, rosehip oil, vaseline oil. The role of such additives is to improve the lubricating properties of the suppository, to prevent irritation, reduce inflammation. With the introduction of the new suppositories vitamins of group In (B6, B12), which is biologically active additives, enhanced by a comprehensive positive impact of califona and vitamins to tissue metabolism and membrane structure of the cells. Vitamins are introduced into the composition in effective amounts, regulated for this group of vitamins. As an additive in suppozitornyj mass may be a preservative from the group of pharmaceutically acceptable, compatible with califona and based preservatives, such as nipazol or nipagin in effective amounts as low as 0.01 to 0.3 wt.% the total weight suppozitornoj mass.

In preclinical practice bioavailability and therapeutic effect californiadreamin suppositories tested on white rats weighing 130-160 g In animals took blood every 45 minutes pokerenlinea the introduction of a suppository. The study of pharmokinetic and biological availability of califona confirmed the presence of high concentrations of the drug throughout the experiment and the high bioavailability of bisphosphonates in suppositories. Conducted pathological studies showed no signs of irritation after using the analyzed suppositories.

The pharmaceutical preparations of the present invention - suppositories containing xidian suitable for therapy or prevention of disorders of calcium and phosphate metabolism and associated diseases diseases, such as osteoporosis, Paget's disease, references for additional information myositis, Bechterew's disease, malignant hypercalcemia, periodontal disease, nephrolithiasis, urolithiasis, urinary concrement, arthritis, neuritis, etc.

Bioavailability and therapeutic effect californiadreamin suppositories with a base of cocoa butter was tested on patients aged 40-65 years. To control pharmokinetics drug investigated excretion with urine collected 2 days/ every once in 2 portions: day, night. After a single injection of suppository (for example, suppositories 1 and 2, the compositions of which are given below), it is shown that with this method of introducing califona the drug remains in the body 1.5-2 days. The number of specified drug sostavljaet,5-2,5 wt.% (45-70 mg) from the input dose slightly more than when administered orally (0.5-1 wt.%), and corresponds to the current therapeutic concentrations of the drug over a long period of time (up to 1.5-2 days), whereas when administered orally, the drug is injected at 95-99% for 10-12 hours. Excretion of califona urine occurs according to the scheme: 1st day: day-20-25 mg, night-15-20 mg, 2nd day 10-15 mg overnight 0-10 mg

During the research of pharmokinetic drug there has been no unpleasant sensations in the subject.

For new members suppositories given the nature of the properties of their constituent ingredients developed technology of preparation of suppositories, which consists in mixing at an elevated temperature of about 50-60°With melt basics, including cocoa butter and emulsifying additives, prepared californiadreamin composition containing compatible emulsifiers (simulatory), for example molten hydrophobic dioxide Aerosil. The resulting mixture is stirred at elevated temperature, about 60°With, before the formation of a homogeneous composition is poured into a special suppozitornoj shaped and molded suppositories keep the temperature in the range of 36-38°, then cooled to 5-10°C. the Additive is injected in a particular phase, depending on their physico-chemical properties. For example, when rst the situation in the composition of the water-soluble suppositories drugs for example, foscarnet, they are mixed with califona, and then with other components of the composition. With the introduction of biologically active additives, such as vitamins or carbon dioxide plant extracts medicinal plants add them to the base, such as cocoa butter.

Thus obtained suppositories new members have the following physicochemical characteristics: full time deformation 10 minutes, melting point 33,0-34,5°C, an acid number of 2.0 to 2.25, iodine number 33,0-36,0, peroxide value of 0.25 and 0.28.

Get the new composition of suppositories is illustrated by the following examples.

Part 1: suppository weighing 2.5 g, temperature plasma 34,0-34,5°C, an acid number of 2.2, iodine number is 34.0, peroxide value - of 0.26. Under the above scheme gives a blend of califona (0.25 g, 10 wt.%) with Aerosil (0.075 g, 3.0 wt.%) and molten ethoxylated lanolin (0.1 g, 4.0 wt.%), which is mixed with an oil phase containing monoglycerides (0.075 g, 3.0 wt.%), olive oil (0.125 g, 5.0 wt.%), propyl ester of para-oksibenzoynoy acid (0.0075 g, 0.3 wt.%) and the rest (1,87) - cocoa butter.

Part 2: suppository weighing 1.0 g, temperature plasma 34,5-34,8°C, an acid number of 2.25, iodine number 36,0, peroxide value of 0.28. Under the above scheme gives a blend of califona (0.01 g, 1 wt.%) with foscarnet (0.001 g, 0.1 wt.%), molten ethoxylated Lanal the nom (0.005 g, 0.5 wt.%), cocoa butter - the rest, 0,988 g).

Part 3: suppository weighing 2.0 g, temperature plasma 35,0-35,2°C, an acid number of 2.0, iodine number - 33, peroxide value of 0.26. Under the above scheme gives a blend of califona (0.4 g, 5 wt.%), foscarnet (0.25 g, 3.0 wt.%.) with Aerosil (0.25 g, 3 wt.%) and with a basis containing carbon dioxide a solution of chamomile (0.1 g, 1.2 wt.%), olive oil (0.02 g, 1 wt.%), nipazol (0.0002 g, 0.01 wt.%), the rest is cocoa butter (up to 2 g).

Part 4: suppository weighing 2.0 g, an acid number of 2.2, the temperature of the plasma 34,5°C, iodine number 34,0, peroxide value of 0.25. Under the above scheme gives a blend of califona (0.4 g, 5 wt.%), with Aerosil (0.25 g, 3 wt.%) and with a base containing vitamins 6 and 12 (0.01 g, 0.2 wt.%) and Witepsol (the rest up to 100 wt.%).

The following are examples of clinical studies experienced parties suppositories for example, suppositories composition 1 and composition 2. There was an open randomized study the efficacy of suppositories with califona when dysmetabolic nephropathy oxaluria in 10 adolescents aged 12-17 years and 10 adults. Teenagers some were on the examination in the hospital, partly in outpatient treatment. Dose califona each suppositories ranged from 0.01 to 0.25, depending on the age and weight of the patient and inserted through the rectum 1 every 2 days after defecation, preferably is at night, the total dose of drug was 3 g for 20 days (intermittent treatment). Treatment effectiveness was evaluated for its effect on oxalate-calcium crystalluria, the total excretion of oxalates per day with urine and index = the ratio of oxalate to creatinine in the urine. Before treatment, all the patients noted improvement of excretia oxalates in urine from 160 to 330 µmol/day at normal 90-135 units and/or permanent oxalate-calcium crystalluria. In the examined patients before treatment was not observed the presence of active infection of the urinary tract (pyelonephritis, cystitis, diarrhea, and which at the same time for 20 days of observation were not receiving other drugs that affect the metabolism of oxalic acid, the observation time is not marked renal dysfunction (pH, titratable acidity, osmolarity, excretion of ammonia, electrolytes), and no marked adverse reactions and subjective complaints. As a result of treatment during the examination at 20-22 days from the beginning of the use of suppositories with califona excretia of oxalates per day all observed decreased to 50-200 μmol/day, for an average of 145 mmol/day, and 12 patients it was normal values (50-130 µmol/day). Index oxalate/creatinine returned to normal in 15 observed and averaged 0,1 (before treatment this index was 0.58), and the OST is selected, this indicator did not exceed 0.3% We all observed, starting from the 6th day from the beginning of treatment, have not been determined in urine oxalate-calcium crystalluria and there have been no changes in the kidneys. Tolerability of the drug in all observed was satisfactory. These studies confirmed that the use of suppositories with califona is in the medical plan as effective as when taking it orally or transdermal (in the form of 2%solution or cream such as cream XYREM manufactured by REFORM containing 2% califona). In the case of the use of suppositories positive effect is and simplifying the delivery of califona in the body intermittent rate of 1 time per day every other day. In the case of patients additional viral infections, for example herpes, was used suppositories, optionally containing foscarnet. Table 1 presents results of the effects of treatment with suppositories with califona on the exchange of oxalic acid at dysmetabolic nephropathy.

Table 1
In the group of patientsExcretion of oxalates µmol/dayOxalate-creatine indexOxalate-calcium crystalluria
patients before treatment280-20of 0.58-0.06+++
after the treatment145-120,13-0,01-
Norma90-1350,05-0,17-

Studies show that the drug xidian in the form of the drug - suppositories may be recommended in the treatment of dysmetabolic nephropathy, and disorders of calcium metabolism in other organs and systems.

1. For the treatment of diseases caused by disturbance of calcium metabolism, in the form of a suppository, containing the active substance base, emulsifier, characterized in that the active substance contains Califon, the emulsifier is ethoxylated lanolin, monoglycerides or Aerosil, Foundation - cocoa butter or Witepsol when the weight of one suppository from 1.0 to 2.5 g in the following components on a single suppository, wt.%:

Xidian1,0-10,0
The emulsifier is ethoxylated
lanolin, monoglycerides,0.5 to 10.0
Aerosil3,0
Base - cocoa butter or WitepsolRest

2. The tool according to claim 1, characterized in that it further comprises chinatravel salt postemergency acid in kolichestvo,1-3 wt.% the total weight of the composition.

3. The tool according to claim 1, characterized in that it further comprises a biologically active additives selected from the group of vitamin B6, B12 or carbon dioxide solution chamomile in effective amounts.

4. The tool according to claim 1, characterized in that it further contains olive oil in the quantity constituting 1-5 wt.% the total weight of the composition.

5. The tool according to claim 1, characterized in that it contains pharmacologically acceptable preservatives in an amount of 0.01 to 0.3 wt.% of the total composition.



 

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EFFECT: reduced treatment time, lowered recurrence of diseases, lack of adverse effects, and lowered cost.

FIELD: medicine, proctology, pharmaceutics.

SUBSTANCE: the present innovation deals with obtaining medicinal forms as suppositories applied for treating proctological diseases. Medicinal preparation as suppositories containing active substance, anesthetic, purified water and foundation could additionally contain antiseptic and local irritating substance, as an active substance - glucocorticoid at the following ratio of components, weight%: glucocorticoid 0.0277-0.0368, anesthetic 1.8-2.2, antiseptic 2.8-3.52, local irritating substance 0.288-0.352, purified water 1.8-2.2, foundation - the rest. As glucocorticoid that inhibits the release of inflammation mediators and causes pronounced antiphlogistic and antiallergic action one should apply, for example, hydrocortisone or synaflane. As anesthetic one should apply, for example, anesthesin, lidocaine or trimecaine. As antiseptic being of astringent, drying off and analgesic actions one should apply, for example, dermatol or xeroform. As local irritating substance being of reflector, venotonic, analgesic and antiphlogistic and, also, antimicrobial actions one should apply, for example, racemic menthol or essential oils.

EFFECT: higher therapeutic efficiency.

5 cl, 3 ex, 4 tbl

FIELD: medicine and immunology, in particular treatment and prevention immunodeficiency conditions and diseases associated with bacterial or viral aggression.

SUBSTANCE: claimed method includes administration to a patient immunoglobulin drug (e.g., pharmaceutical composition containing 6-12 % of specific heterologous secreted immunoglobulin A, isolated from milk or foremilk of immunized ungulates). Administration is performed parenterally wherein single dose is at least 10 IU/kg of patient weight for treatment or at least 5 IU/kg for prophylaxis; or perorally in dose of 0.2-0.5 g and/or topically one-two times per day for 1-5 days. Method of present invention makes it possible to decrease dose of administrating immunoglobulin due to prolonged retention of its high titers in body fluids.

EFFECT: enlarged range of application and assortment of immunoglobulin drugs.

4 cl, 5 ex

FIELD: medicine.

SUBSTANCE: means has dibunol, 15% oil extraction of propolis, gelatin, glycerol and treated water taken in known component proportion.

EFFECT: enhanced effectiveness of treatment; prolonged regenerating and antibacterial action.

2 cl

FIELD: medicine, gynecology, pharmacology, pharmaceutical industry.

SUBSTANCE: invention proposes a preparation that comprises bacterial mass of live microorganisms as an active component, protecting medium and fat base. The preparation comprises lactobacilli as bacterial mass and one or some eubiotic microorganisms taken among the following group: bifidobacteria, streptococci and lactococci taken in the amount per a single dose. Also, the preparation comprises additionally an acceptable sorbent and a biologically active supplement. Also, invention relates to a method for preparing this preparation that involves preparing firstly lactobacilli bacterial mass and one or some genus of eubiotic microorganisms taken among the following group: bifidobacteria, streptococci and lactococci. Then the prepared bacterial mass of microorganisms is immobilized on sorbent used in medicine in its ratio to bacterial mass of microorganisms = (9-1):(1-9) followed by addition of the protecting medium and biologically active supplement to formed mass in the necessary amount. Also, invention describes a method for prophylaxis and treatment of bacterial vaginitis that involves intravaginal administration of the preparation described above in the amount 1-3 doses, 1-3 times per 24 h. The treatment course is prescribed individually. Invention provides expanding assortment of agents used for treatment of bacterial vaginitis. Invention can be used in obstetric-gynecological practice.

EFFECT: improved method for vaginitis treatment, valuable medicinal properties of preparation.

13 cl, 4 tbl, 1 ex

FIELD: medicine.

SUBSTANCE: the present innovation deals with applying biphosphonate for treating osteonecrosis and/or osteonecrosis dissecans. This medicinal preparation could be additionally applied for preventing the development of osteonecrosis and/or osteonecrosis dissecans and any complications associated with both diseases. Biphosphonate acts for the decrease or prevention of severe degree of deformation and/or destruction of a bone or a cartilage and provides the chance to form new bony tissue in a patient.

EFFECT: higher efficiency of therapy.

38 cl, 7 dwg, 1 tbl

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