Improved dosage form of interferon inducer

 

(57) Abstract:

The invention relates to an improved form of drug-candle. Candle contains inducer of interferon - dutrey complex polyborazylene and polyribosylribitol acids 200 to 250 mcg, hyaluronic acid, 10 - 20 mg, antioxidant blend of vitamins C and E 30 - 40 mg basis up to 1.5, the Mass ratio between vitamins C and E in a mixture of antioxidants is preferably 1:1. New dosage form is used in the treatment of viral diseases etiology and provides controlled release of the active principle in excluding unwanted side effects. 1 C.p. f-crystals.

The invention relates to medicine, specifically to an improved form of drug-candle-datausage complex polyribosylribitol and Polideportivo acid, abbreviated as poly - EN poly-A, used as inducer of interferon in the treatment of viral diseases of different etiologies.

The use of polyribonucleotides for the treatment of viral diseases known. In the application Germany N 1617545, MKI A 61 K 31/675, Appl. 1967 (patent issued 16 years later, in 1983!) for the treatment of influenza infection proposed by intraperitoneal injection of informationplease application UK N 2038628, MCI A 61 K 31/675. 1980, intravenously or intraperitoneally injected aqueous solution of 0.85% sodium chloride containing copolymer /4-tees/pridelava and cititravel acids, complex karboksimetilcelljulozy and polylysine. For stimulation of immunity at the request of great Britain N 2216416, MKI A 61 K 31/675, 1989, use of the pill or injectable solutions containing DNA, RNA, nucleobase or nucleosides, vitamins, minerals. Another adjuvant according to the U.S. patent N 5231085, NCI 514/44, 1993, contains arginine and ornithic and RNA (or DNA), eykozapentaenovuyu or docosahexaenoic acid, and can be administered intravenously or orally. Further in U.S. patent N 3980776, NCI 514/44, 1976, the induction of interferon called intraperitoneal or intranasal introduction dutrieu RNA extracted from spores or mycelium Cortinellus shiitake. For the treatment of viral hepatitis according to the U.S. patent N 5593973, NCI 514/44, 1997 use complex polyribosomes (I), polyribosylribitol (C) and polyborazylene (U) acids of the formula rInr(C11-14U).

Known use as an inducer of interferon datausage complex polyborazylene and polyribosylribitol acids poly-EN - poly-rA, which is called "Poludan" is used when virusa N 5091374, NCI 514/44, 1992 by infection with human immunodeficiency virus intravenous proposed to introduce the complex poly-EN-poly-rA, and in the application of UK N 2211847, MKI C 07 H 21/00, 1988 as an antiviral drug, containing a complex of poly-EN-poly-rA, provides pyrogen-free aqueous solution for intraperitoneal administration.

In the closest to the claimed, selected as a prototype of the solution according to the U.S. patent N 4283393, NCI 514/44, 1981 stated ophthalmic drug eye ointment, which is used to treat herpes infections of the eye and contains the interferon inducer poly-poly rI-rC, as well as its carrier: simple or complex esters of cellulose, polyvinyl alcohol, polyvinylpyrrolidone, carboxyvinyl polyesters and polyethylene glycol. In the description of the above-mentioned patent reads: "...interferon Inducers used in the new method of treatment in accordance with the present invention, are dwudazewyn synthetic polynucleotide complexes, such as poly-I:C, poly A:U or similar (lines 61-64)... For use as a vaginal or rectal suppositories compositions with controlled release in accordance with the present (i.e., U.S. Pat. USA 4283393) the invention have predlagaemoe the invention solves the problem of creating a form of drug-candles-inducer of interferon-datausage complex polyribosylribitol - polyribosylribitol acids (poly-EN poly-rA), access to which would allow to extend the possibilities of therapeutic use of the aforementioned inductor due to more precise metered release of the active principle in excluding undesirable side effects (microcline, irritation, inflammation and so on).

The problem is solved due to the fact that the dosage form datausage complex poly-EN poly-rA, made in the form of a rectal suppository, contains, in addition to interferon inducer, and even hyaluronic acid as an immunomodulator and vitamins C and E as antioxidants, in the following ratios between the ingredients:

inducer of interferon - dutrey complex polyborazylene and polyribosylribitol acid - 200 - 250 mcg

hyaluronic acid is 10 to 20 mg

the mixture of vitamins C and E, in a mass ratio of 1:1 to 30 - 40 mg

the basis of up to 1.5 grams

The basis can be represented: solid confectionery fat, a mixture of oxides, the substance known under the name "Witepsol", cocoa butter.

Natural polysaccharide hyaluronic acid, found, for example, in the umbilical cord of mammals, the crests of Mature birds, synovial liquid is erona.

Add a candle antioxidants-vitamins C and E, which membranoproliferative, improves the efficiency of the receipt of the beginning of the current in the human body. The relationship between vitamins C and E, generally speaking, can vary within a wide range, however, a pronounced synergistic action was observed when the ratio between them is equal to 1:1.

It should be noted that the refusal injection method of administration of the antiviral drug eliminates the risk of infection by hepatitis B and C, and HIV infection; in addition, the introduction of antiviral compositions in the form of candles provides you with a quick intake of the drug in the blood and organs, rich macrobiotically and lymphoid elements.

In detail the invention is illustrated by examples of its implementation.

Example 1. The usual way is formed into a candle from masses containing:

0.25 mg datausage complex poly-EN poly-rA,

0.015 g of hyaluronic acid,

0.015 g of vitamin C,

0.015 g of vitamin E and

basis - tallow - 1.5.

Example 2. Candles, obtained according to example 1, the hospital has treated 20 patients aged from 20 to 48 years (including 12 women and 8 men) about the recurrent heresay disease was noted on a monthly basis, their length ranged from 5-7 to 9-12 days. Ten patients (20) herpetic lesions were localizability in the genital area, five on the lips, three - on the skin of the buttocks; two patients were diagnosed with disseminated form of herpes. In 15 patients the relapse was accompanied by impairment of the General health; weakness, fever, pain was noted in the prodromal period for 6-24 hours before the appearance of lesions. All patients received treatment in the form of rectal suppositories in example 1, starting from the period of exacerbation of herpes (recurrent) and during the subsequent infusion of remission, at night, ten times, with an interval of 48 hours, before the full clinical recovery. The observed decrease in the duration of relapses in 2.5-3 times and, accordingly, increase the length of remission in 2-2,5 times in 75% of patients; 14 patients (20) noted the weakening or even complete disappearance of prodromal symptoms.

Example 3. The treatment of 20 patients with herpes zoster. Therapy was started on the second or third day of the disease, while 8 patients (control) received monotherapy drug "Zovirax" (400 mg 5 times a day), and 12 patients, along with spirits, additionally received the candles on PR is that depriving patients of the control group (so E. receiving only zovirax) occurred, on average, by 8, 7 day, while in the combined treatment (zovirax + candle) this row averaged, 5, 6 days. These laboratory studies have indicated that rectal candles actively induce interferon in vivo, providing a systemic effect. It is shown that in response to treatment (course of 10 candles) the level of serum interferon increases after 48 hours 9-13 times, the production of alpha - and gamma-interferon - 2-5,2 and 2.5-4.4 times, respectively.

Example 4. Candles, obtained according to example 1, was used in 20 patients with herpetic lesions of the cornea ("tree" keratitis). The diagnosis was established based on clinical and instrumental examination and confirmed by detection of antigen of herpes simplex virus in the scrapings of cells of the cornea patients. Candles from example 1 was used for relief of acute manifestations of the disease and was administered every day. After 24 hours, 48 hours and 7 days serum from a vein patients were investigated for the presence of interferon, and blood leukocytes were investigated on the ability to produce alpha - and gamma-interferons. The control 20 patients with keratin Yunosti application of interferon inducer in the form of candles. The beginning of remission was noted at 4,0 0,3 day (control - 9.5 1,0 day), epithelization of the affected cornea was already observed by 8.6 0,83 day( control - 17.7 1,2 day), and resorption of the infiltrate was observed at 12,5 1,0 day (control - 22.6 2,0 day). The total period of treatment decreased from 23.3 1.7 days in the control to 14.6 1.2 days in the experimental group when treatment was used candles. The significance of change is high and is p < 0,001.

The obtained clinical results can be explained by the active production of interferon, which significantly increased: for serum interferon, on average, 13 times in 24 hours, 9 times in 48 hours, 5 times a week; for leukocyte alpha interferon - 2 times in 24 hours, 5.2 times in 48 hours and 8.3 times a week; for leukocyte interferon-gamma - 2.5 times in 24 hours, 4.4 times in 48 hours and 4.2 times a week.

Example 5. Seven patients with recurrent, isio-sciatica (presumably viral etiology) was performed, along with conventional medication and physiotherapy, treatment with suppositories containing the interferon inducer poly-EN poly-rA, obtained in example 1. A control group of patients (10 people) who did not receive the course who were suppositories, recovery was observed after 10 to 3 days and the pain has stopped within 3-5 days.

1. Dosage form-candle containing the inducer of interferon-dutrey complex polyborazylene and polyribosylribitol acids, as well as the basis of candles, characterized in that it additionally contains hyaluronic acid and antioxidant blend of vitamins C and E, the following mass ratio between ingredients:

Dutrey complex polyborazylene and polyribosylribitol acid - 200 - 250 mcg

Hyaluronic acid is 10 to 20 mg

The mixture of vitamins C and E - 30 - 40 mg

The basis of Up to 1.5 grams

2. Dosage form under item 1, characterized in that the mass ratio between vitamin C and vitamin E in a mixture of antioxidants is 1 : 1.

 

Same patents:
The invention relates to food processing and pharmaceutical industries

The invention relates to medicine and pharmaceutical industry and for the development of new drugs

The invention relates to medicine, namely to the pharmaceutical industry, and for candles, which can find use for the treatment of external and internal hemorrhoids and rectal fissures

The invention relates to an external preparation for topical application, in particular to the outer local drug use, containing as activitiesthese substance 2-amino-2-(2-(4-octylphenyl)ethyl)propane-1,3-diol or its pharmaceutically acceptable acid salt additive

Rectal tool // 2152204
The invention relates to medicine and pharmaceutical industry and for the creation of new drugs used for the treatment of acute and chronic prostatitis

The invention relates to medicine, namely the pharmaceutical industry and relates to a medicinal product for the treatment of proctologic diseases
The invention relates to medicine, technology of medicinal forms with bacterial drugs
The invention relates to the pharmacy, the pharmaceutical form of human recombinant interferon Alfa-2 - rectal and vaginal suppositories

The invention relates to medicine, namely to Virology, immunology, gynecology and pharmacology
The invention relates to the field of cosmetology and relates to biologically active additives
The invention relates to the field of medicine and for use in cosmetics for correcting facial flaws as wrinkles and folds, as well as to improve the shape and volume of the lips and prevent skin aging

The invention relates to medicine, in particular to a health resort, and for the correction of metabolic disorders in patients with diabetes mellitus

The invention relates to medicine, namely to the chemical-pharmaceutical industry and relates to a method of obtaining water-soluble polysaccharides from the leaves of ginseng

The invention relates to medicine, pharmacology, veterinary medicine and biology

Antiseptic drug // 2151599
The invention relates to medicine, in particular to pharmacology

The invention relates to medicine, namely the pharmaceutical industry and relates to a medicinal product for the treatment of proctologic diseases

The invention relates to the field of joint processing of bee products and seafood and, in particular, to receive treatment-and-prophylactic drug "VINIUS-WITH" from ambrosia and ascorbic acid powder
Up!