For the treatment of inflammatory diseases

 

(57) Abstract:

The invention relates to medicine, namely to pharmacology, and relates to means for the treatment of inflammatory diseases of female sexual sphere. The invention consists in that the means for the treatment of inflammatory diseases contains sea buckthorn oil, Hexapeptide structural formula arginyl-alpha-aspartyl-lysyl-poured-tyrosyl-arginine, suppository basis and glycine at a certain ratio of components. The invention provides a wider range of pharmacological properties, providing immunoregulatory, anti-inflammatory, detoxification, anti-virus and wound healing effect in complex therapy of oncological and hematological diseases. 1 C.p. f-crystals, 1 table.

The invention relates to medicine, namely to pharmacology, and can be used for the treatment of inflammatory diseases of female sexual sphere, in patients with infectious diseases, and also in the treatment of oncological and hematological diseases.

In modern medicine there is a certain Arsenal of medicines containing natural or synthetic substances that are used in cured theta and in the complex treatment of oncological diseases.

It is known the use of interferon Alfa-2A in the form of a suppository containing AIDS such as alpha-tocopherol and ascorbic acid, for the treatment of gynecological diseases in adults and viral infections in children (patent N 2024253, Russia).

However, the known tool does not have sufficient efficacy in the treatment of viral infections and like other medicines containing interferon-alpha can cause some side effects, including the strengthening of autoimmune disorders.

The closest in composition analogous to the patent-pending tool is a dosage form in the form of a rectal suppository containing as active substance 5-10% sea buckthorn oil, and as suppository basis emulsifier and cooking oil to 100% (Ant I. A. Extra way to obtain suppositories with sea-buckthorn oil. //In the book: The main directions of development of pharmacy. - Riga. - 1984. - S. 203-204).

Known medicine has found application as anti-inflammatory agents in proctologic practice. Suppositories containing sea buckthorn oil have local wound-healing and anti-inflammatory effect. Prisutstvie the I immune response of the body and reduce symptoms of intoxication. However, the known drug does not have sufficient anti-inflammatory and immunostimulant effect, does not cause an antiviral effect.

Patentable invention is directed to the development of a similar drug with a wide range of pharmacological properties, providing immunoregulatory, anti-inflammatory, detoxification, anti-virus and wound healing in the treatment of oncological, hematological, erosive and infectious diseases.

The solution of this problem is provided by the fact that the remedy for the treatment of inflammatory diseases containing sea buckthorn oil and suppository basis, in contrast to the known, additionally contains Hexapeptide structural formula arginyl-alpha-aspartyl-lysyl-poured-tyrosyl-arginine and glycine in the following ratio of components, wt.%:

Hexapeptide structural formula arginyl-alpha-aspartyl-lysyl-poured-tyrosyl-arginine - 0,001 - 1

glycine is 0.05 - 5

sea buckthorn oil - 1 - 9

suppository basis - Rest

And that suppository base contains an emulsifier and cooking oil in the following ratio, wt.%:

emulsifier - 1 - 9
< treatment of cancer, hematological, erosive and infectious diseases.

The most preferred form of patentable funds in the form of suppositories containing as active ingredient is 0.01% (0.0001 g) of the Hexapeptide structural formula arginyl-alpha-aspartyl-lysyl-poured-tyrosyl-arginine, 5% (0.05 g) sea buckthorn oil of 0.5% (0.005 g) glycine, and as suppository 5% emulsifier and cooking oil to 100%.

Drug (the authors called suppositories immunophenotype) developed in the research-and-production enterprise "Bionics" and its members are clearly not following properties that enhance wound healing and anti-inflammatory action with achievement pronounced antiviral, immunoregulatory and detoxification effect in the treatment of oncological, hematological and infectious diseases.

Experimental and clinical study of patented tools shows that it does not cause adverse reactions.

The drug is called "Suppositories immunophenotype" is preferably produced in the form of a rectal vaginal suppository containing 0.01% of the specified Hexapeptide, 0.5% glycine and 5% sea buckthorn BR>
1. "Suppositories immunophenotype" stimulate mitotic activity of lymphocytes in 2 times more efficient in comparison with the known drug (table. 1), restore the performance of T-cell immunity, stimulate the production of b-lymphocytes (CD22) (example 3 and 4).

2. Patented tool enhances antiviral immunity, inhibits the replication of virus, causes elimination of viral antigens (HBs and Hbe) and has a pronounced therapeutic effect in patients with viral hepatitis (example 4). Known means does not possess these properties.

3. Patented tool has a pronounced anti-inflammatory and detoxifying effect, normalizes the disturbed biochemical indicators of liver function, increases the effectiveness of antibiotic therapy and eliminates contraindications to chemotherapy in cancer patients.

4. Determination of the chronic toxicity of the medicinal product demonstrates its harmlessness. Identified variations in hematological and biochemical parameters during its introduction to the animals daily for one month, at therapeutic dose or 10-fold excess of therapeutic dose, after the abolition of Lek is m does not cause local irritation, the drug has no allergenic and mutagenic activity.

The drug has shown good clinical results in the treatment of chronic infectious and inflammatory diseases of female sexual sphere, viral infections and combination chemotherapy of cancer patients.

The drug has a local anti-inflammatory effect on the mucous membrane of the rectum or vagina. Resorptive action is determined by the ability of the Hexapeptide and glycine quickly absorbed from the place of introduction and to generate a signal in the target cells. Resorptive action occurs in 5-10 minutes after administration of the drug and occurs within 2-4 days in the form of a reduction of the phenomena of intoxication (fast phase), followed by increased phagocytic activity of neutrophils, the normalization of the balance of subpopulations of T - and b-lymphocytes, increasing amounts of specific antibodies by elimination of viral and bacterial particles (average and the slow phase lasting up to 3-4 months). The drug is prescribed courses in the form of rectal and vaginal suppository, one suppository 1 time per day total amount of from 5 to 15 injections. In the case of chronic viral or about the ü course of therapy is determined by the results of clinical effects, data hematological, immunological and biochemical examination.

Clinical use of suppositories immunotherapy in patients with infectious and inflammatory diseases of female sexual sphere were carried out as in the scheme of the combined radical and conservative combination therapy.

Specific examples of descriptions received, biological and therapeutic properties of drugs.

Example 1.

The manufacturer of the medicinal product.

The manufacture of suppositories immunogenomic takes place in three stages: preparation of hydrophilic active substances, the preparation of lipophilic bases and formation of candles. For the preparation of hydrophilic active ingredients taking 0.07 g Hexapeptide structural formula: arginyl-alpha-aspartyl-lysyl-poured-tyrosyl-arginine (Immunofan) and 3.5 g of glycine. Glycine is dissolved in 50 ml of distilled water. The resulting solution of glycine is dissolved a portion of Immunofan. The resulting solution of Immunofan and glycine freeze-dried. For the preparation of lyophilic basics take fat food 1000 g paraffin wax 60 g, emulsifier T-2 (GHMT) and 33.5 g of sea buckthorn oil 33,5 g and thoroughly mixed at a temperature of 37-40is lizina. The resulting mass is poured into cellular outline package OST 64-074-91 film PVC brand EP-73 according to GOST 25250-88. Each candle weighing 1.5 g contains: Immunofan 0,00010,00001 g, glycine 0,0050,0005 g, sea buckthorn oil 0,050,005,

Example 2.

The study of the influence of patented medicines and suppositories with sea-buckthorn oil (prototype) on the proliferative activity of lymphocytes.

Guinea pigs administered cyclophosphamide (CP) at a dose of 100 mg/kg intraperitoneally, after 5 days the animals injected per rectum suppositories containing patented medicine volume 1/5 candles (3 animals per group) and suppositories containing the substance of the prototype in the same volume (3 mice per group). After 22-24 hours after injection of candles experimental animals slaughtered and extract cells of the spleen, which are used in further work.

Proliferative response of lymphocytes evaluated by the standard procedure, reaction of besttransport on the action concavalin A (Con A). For this purpose, cells of the Guinea-pig spleen were cultured in 96-well flat-bottom plates in medium RPMI -1640 with the addition of 2 mm L-glutamine, 40 μg/ml gentamicin, 10 mm HEPES-buffer pH 7,2; 510-5mm beta-mercaptoethanol the CO2.

The proliferative response of lymphoid cells into the pot And determined after 72 hours by the inclusion of 3H-thymidine (1 MK Cu per well 96-well plate) in DNA of lymphocytes. Thymidine-labeled radioactive tritium add for 4-6 hours before the end of the cultivation. After incubation the contents of the wells is transferred onto the filters ("Titertek, UK) using a cell harvester ("Titertek, UK). The dried filters are placed in vials with scintillation fluid and determine the level of incorporation of radioactive label by using scintillation beta-counter. The determination results are presented in table. 1. As follows from the data presented in the newly developed tool causes the amplification reaction besttransport lymphocytes after its inhibition. Fit more efficiently in comparison with the tool prototype.

Thus, patent-pending tool exceeds its immunological activity means the prototype in a test restore disturbed immunologic reaction besttransport lymphocytes.

Example 3.

Treatment patented tool inflammatory diseases of female genital organs.

Patient M., 25 years. Clinical d is alas lower abdominal pain, the deterioration of General condition, fever up to 38.5oC, menstrual dysfunction. At vaginal examination appendages of the uterus painful, moderately enlarged, partially movable. Immunological examination shows the presence of immunodeficiency States: the reduction reaction of besttransport of lymphocytes to PHA by 32%, reducing immunoregulatory index helper and suspensory lymphocytes (CD4/CD8) to 0.9, reducing the number of b lymphocytes (CD22) 194 - abs/µl and increase the sedimentation rate of 34 mm/h. Conducted comprehensive anti-inflammatory therapy within 10 days from the appointment of antibacterial drugs with a broad spectrum of action. On the background of positive dynamics from the phenomena of intoxication after the course of antibiotic therapy, the patient remains moderate fever, weakness, asthenic syndrome without apparent changes of immunological indexes. On the 11th day the patient is assigned suppositories immunophenotype 1 time in 5 day course of injections intravaginalno. On the background of the application patentable funds decreased body temperature to normal, improving overall health, the emergence of appetite, normalization of sleep, recovery of bowel function. Put the physiological norm, increase immunoregulatory index to 1.2, the rise in the number of b-lymphocytes to 256 abs/µl and decrease of the sedimentation rate of 16 mm/hour. Adverse reactions to the introduction of suppositories immunogenomic not marked. The patient was discharged from hospital in satisfactory condition. Recommended continuation courses suppositories immunogenomic under outpatient supervision. Thus, the use of suppositories immunogenomic in the complex treatment of inflammatory diseases of female sexual sphere provides a pronounced therapeutic effect after a long period with the elimination of antibiotic resistance and clinical and laboratory manifestations of secondary immunodeficiency States.

Example 4.

The use of suppositories immunotherapy in a patient with viral hepatitis b and hemoblastosis.

Patient I. , 15 years is on the treatment of lymphoblastic lymphosarcoma option (defeat ileocecal intestine). Conducted laparotomy with right-hand hemicolectomies. Repeatedly transfused whole blood. The first course of chemotherapy. After a month and a half after the start of treatment without signs of recurrence of the tumor process in a patient with weakness, red eye reduction is of getosname sclera chemotherapy was interrupted. The clinical state of moderate severity. Moderate symptoms of intoxicatie. Urine dark, feces clarified. The liver stands out from the edge of the rib arc 2 cm, photoelasticity consistency. Serum contents of total bilirubin 128,2 µmol/l is associated - 83.5 mmol/l, free of 44.7 μmol/L. Active Alat - 480, U/l, AST - 430 U/l, HBs Ag titer of 1:32. Immunological parameters changed dramatically: the number of T-lymphocytes 32,4%, T-helper cells (CD4) - 18,8%, T-suppressor (CD8) by 16.7%. Immunoregulatory T-helper/T-suppressor -1,1. Clinical diagnosis of viral hepatitis b, typical, moderate to severe form. The patient is assigned suppositories immunophenotype for rectal injection daily for 1 dose within 10 days. During therapy proposed by the tool marked marked reduction of symptoms of intoxication, improving overall health, elimination of skin itching, getosname, recovery, sleep and appetite. After 1 week was a repeat course of complex treatment by suppositories immunophenotype and generally accepted means of pathogenetic and symptomatic therapy. The liver edge of the costal arch, painless. Serum contents of total bilirubin 12.8 µmol/l is associated - 8.5 µmol/l, svobodnaia norms: the number of T-lymphocytes of 42.3%, T-helper cells (CD4) and 36.2%, T-suppressor (CD8) to 18.7%. Immunoregulatory T-helper/T-suppressor - for 1.9. Reduction of symptoms of intoxication, as well as improvement of biochemical indicators of activity of the pathological process in the liver, recovery of immune status were allowed to continue the course of polychemotherapy in full. The patient was discharged from hospital in remission.

Thus, the use of patent-pending tool allows you to achieve a pronounced therapeutic effect in a patient with viral hepatitis b, to ensure the effectiveness of treatment of a cancer patient.

1. For the treatment of inflammatory diseases containing sea buckthorn oil and suppository base, characterized in that it additionally contains Hexapeptide structural formula arginyl-alpha-aspartyl-lysyl-poured-tyrosyl-arginine and glycine in the following ratio, wt.%:

Hexapeptide structural formula arginyl-alpha-aspartyl-lysyl-poured-tyrosyl-arginine - 0,001 - 1

Glycine is 0.05 - 5

Sea buckthorn oil - 1 - 9

Suppository basis - Rest

2. Means under item 1, characterized in that suppository base contains an emulsifier and a cooking fat when following the

 

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