Antiviral agent

 

(57) Abstract:

The invention relates to medicine and the pharmaceutical industry and relates to formulations for the prevention and treatment of viral diseases, containing recombinant interferon. The essence of the invention: antiviral agent contains alpha-, or beta-, or gamma-interferon, an immunomodulator, an anti-microbial agent and/or anti-inflammatory drug, stabilizer, and pharmaceutically acceptable additives target. The tool itself is a liquid, or soft, or solid dosage forms. Effect: expanding Arsenal of drugs antiviral action. 18 C.p. f-crystals, 9 PL.

The invention relates to medicine and the pharmaceutical industry and relates to dosage forms containing recombinant interferon for prevention and treatment of viral diseases.

Known antiviral agent containing alpha-or beta-, or gamma-interferon for prevention and treatment of viral diseases.

(RU, patent 2073522, a 61 K 38/21, 1997).

Well-known drug for the treatment of viral, chlamydial and bacterial infections on the basis of the antioxidant properties. As this substance use alpha-tocopherol acetate. The drug may be in the form of rectal capsules or candles and is introduced rectally.

(RU, patent 2057544, a 61 K 38/21, 1996).

Known drug for the treatment of viral infections, a single dosage form of a mixture of interferon and substances containing not less than 2.2% of polyunsaturated fatty acids. The drug may be in the form of rectal capsules or candles and is introduced rectally.

(RU, patent 2097061, a 61 K 38/21, 1997).

Known drug "Locteron for the treatment and prevention of viral diseases on the basis of human leukocyte interferon. The drug "Locteron contains interferon synthesized by leukocytes of donor blood under the influence of the virus inductor strain of parainfluenza virus 1 Sadi GKV 2339.

(RU, patent 2108804, a 61 K 38/21, 1998).

Known antiviral drug actions, including human interferon and a synergist. As a synergist it contains human immunoglobulins. As human interferon it contains recombinant alpha-or beta-, or gamma-interferon person. As immunoglobulins CLASS="ptx2">

(RU, patent 2073522, a 61 K 38/21, 1997).

The closest one is an antiviral agent containing alpha-or beta-, or gamma-interferon, stabilizer biological, physico-chemical properties and/or resistance to microbial contamination and consistentread basis

(RU, patent 2150291, a 61 K 38/21, 1999).

The technical result of the invention is to provide a preparation with prolonged action as ointment, gel, suppository, paste, cream, liniment, tablets, capsules, drops in a nose on the basis of recombinant interferon, ensuring good penetration ability and possessing antiviral, antibacterial, anti-inflammatory, detoxifying, local anesthetic action.

To achieve the technical result antiviral agent containing alpha-or beta-, or gamma-interferon, stabilizer and pharmaceutically acceptable additives target, according to the invention further comprises an immunomodulator, an anti-microbial agent and/or anti-inflammatory medication.

The tool contains an immunomodulator selected from the group of cytokines, metronidazole, in the amount of 0.00 is estva.

As it contains cytokine interleukin-2 in the amount of 1000-20000 ME and/or tumor necrosis factor alpha or beta in the number 1000-10000000 ME on 1 g of product.

The product contains anti-inflammatory drug selected from the group: diclofenac sodium, indomethacin, ibuprofen, naproxen, kortikosteroidnye drugs: hydrocortisone, fludrocortisone, flumetazon, betamethasone, mometazon, perkantoran, triamcinolon in the amount of 0.002-0.01 g to 1 g of product.

Antiviral agent additionally contains vitamins selected from the group of: vitamin E, vitamin C, vitamin D3,vitamin PP in the amount of 0.005-0.025 g per 1 g of product.

As vitamin E. it contains alpha-tocopherol acetate.

The tool also contains retinoids: synthetic retinoids, vitamin a and beta-carotene in the amount is 0.0002-0,0006 1 g of product.

The tool contains a stabilizer selected from the group of: polyvinylpyrrolidone, polyethylene oxide, polyvinyl alcohol, glycerol, derived methylcellulose (NaKM) and nipagin in the amount of 0.0001-0.09 g per 1 g of product.

Antimicrobial agent selected from the group of silver-containing component in an amount of 0.001-0.05 g per 1 g of the agent, Quaternary AMM is 1 g of product.

As a silver-containing component it contains paverpol.

As Quaternary ammonium compounds it contains atony, or benzathine chloride or benzalkonium chloride.

The broad-spectrum antibiotics selected from the group: amoxicillin, ampicillin, oxacillin, methicillin, cephalexin.

As pharmaceutically acceptable target additives it contains one or more ingredients from the group of additives, including fat, cocoa butter, paraffin, petrolatum, lanolin, emulsifier, dimethylsulfoxide, witepsol, soklin, tallow type CH, glycerin, polyethylene oxide, propylene glycol, proxanol is chosen-268, lactose, sucrose, calcium stearate and acetylcellulose.

Additionally, the product contains antioxidant and topical anesthetic drug.

As an antioxidant it contains Trilon B and/or butylacetyl in the amount of 0.0001-0,0006 g per 1 g of product.

As local anesthetic drug it contains lidocaine in an amount of 0.01-0.05 g per 1 funds.

The tool itself is a liquid, or soft, or solid dosage forms. Solid dosage form has an acid-resistant coating.

With the red means. To obtain gel prepare a solution of the stabilizer: 1% nipagina, 6% polyvinylpyrrolidone and polyethylene oxide. Add paverpol and necessary pharmaceutically acceptable additives mentioned above. Mix the components, and sterilize by autoclaving. Then add alpha, or beta, or gamma-interferon, interleukin-2, tumor necrosis factor alpha or beta and mix. Ready the product Packed in the required capacity (e.g., tubes), seal and label. These components take in the ratio of 1 g of product are shown in table.1

Example 2. Carried out analogously to example 1.

Take the components in the ratio of 1 g of product are shown in table.2.

Example 3. Carried out analogously to example 1.

Components take in the ratio of 1 g of product are shown in table.3.

Example 4. For more ointment take: polyvinyl alcohol, 10% solution etoniya, or benzathine chloride or benzalkonium chloride. Add antioxidant - 10% solution of the trylon B, ibuprofen, synthetic retinoids, vitamin D3, C, PP, Radostin. Mix everything with the required pharmaceutically acceptable targeted supplements mentioned above. Sterilize and add alpha, elementy take in the ratio of 1 g of product, are given in table.4.

Example 5. For preparation of cream mixed solution NaKM and chlorhexidine with butylacetophenone. Then add beta-carotene, broad-spectrum antibiotics (amoxicillin, or ampicillin or oxacillin or methicillin, or cephalexin), vitamins D3, PP, E and naproxen. Connect with the desired molten pharmaceutically acceptable target additives mentioned above, and then add alpha, or beta, or gamma-interferon, tumor necrosis factor alpha or beta. Next, as in example 1. These components take in the ratio of 1 g of product are shown in table.5.

Example 6. To obtain candles mixed solution etoniya with butylacetyl, Trilon B. Then add corticosteroids (hydrocortisone, or flumetazon, or atamazon, or mometasone, or forcertain, or triamcinolone), havergal. Connect with the desired molten pharmaceutically acceptable targeted supplements and add alpha, or beta, or gamma-interferon, metronidazol, polyoxidonium. The mixture is then poured into molds for candles, cooled and packaged. These components take in the ratio of 1 g of product, given butylacetophenone. Add vitamins a and C, diclofenac sodium, broad-spectrum antibiotics. Connect with the required pharmaceutically acceptable targeted supplements, add alpha, or beta, or gamma-interferon and interleukin-2. The mixture is molded in the form of tablets and put them acid-based coating, for example, acetylcellulose taken in the amount of 4.5% of the total mass above the base.

To obtain capsules these components fill gelatin capsules.

These components take in the ratio of 1 g of product are shown in table.7.

Example 8. To obtain emulsion mix atony with Trilon B. Add naproxen, vitamins a and E, paverpol and necessary pharmaceutically acceptable additives target, in the proper ratio. And then enter the alpha, or beta, or gamma-interferon and tumor necrosis factor alpha or beta.

These components take in the ratio of 1 g of product are shown in table.8.

Example 9. To get drops in the nose prepare separate solutions of components: 50%-aqueous solution of polyethylene oxide, 6% solution of the polyvinylpyrrolidone, 10%-aqueous solution of the trylon B.'s solutions bring in one tank in specified sequence and sterilized. Then add corticosteroids (fludrocortisone), paverpol, alpha-, or beta-, or gamma-interferon, interleukin-2 and vitamin A. All components are mixed. The resulting tool is poured into the desired container, seal and label.

These components take in the ratio of 1 ml of buffer mixtures are given in table.9.

Received antiviral agent is kind of hard, soft or liquid forms.

Laboratory testing tool on the model of cell cultures, experimental animals have shown that it is non-toxic, non-pyrogenic, retains its physico-chemical and biological properties.

Clinical trials on human volunteers aged 18-20 years of age show that the drug is safe, well tolerated, does not cause allergic reactions.

1. Antiviral agent containing alpha-or beta-, or gamma-interferon, stabilizer and pharmaceutically acceptable additives target, characterized in that it further comprises an immunomodulator, an anti-microbial agent and/or anti-inflammatory medication.

2. Antiviral agent under item 1, characterized in that it contains them is icesto 0,006-0.04 g per 1 g of product, polyoxidonium in the amount of 0.003-0,012 g per 1 g of product.

3. Antiviral agent for PP.1 and 2, characterized in that as cytokines it contains interleukin-2 in the amount of 1000-20000 ME and/or tumor necrosis factor alpha or beta in the number 1000-10000000 ME on 1 g of product.

4. Antiviral agent under item 1, characterized in that it contains anti-inflammatory drug selected from the group: diclofenac sodium, indomethacin, ibuprofen, naproxen, corticosteroids: hydrocortisone, fludrocortisone, flumetazon, betamethasone, mometazon, perkantoran, triamcinolon in the amount of 0.002-0.01 g to 1 g of product.

5. Antiviral agent under item 1, characterized in that it additionally contains vitamins selected from the group of: vitamin E, vitamin C, vitamin D3the vitamin e in the amount of 0.005-0.025 g per 1 g of product.

6. Antiviral agent under item 5, characterized in that as the vitamin E it contains alpha-tocopherol acetate.

7. Antiviral agent under item 1, characterized in that it additionally contains retinoids: synthetic retinoids or vitamin a in number is 0.0002-0,0006 1 g of product.

8. Antiviral agent under item 1, featuring overuse tool under item 1, characterized in that it contains a stabilizer selected from the group of: polyvinylpyrrolidone, polyethylene oxide, polyvinyl alcohol, glycerol, derived methyl cellulose (Na CMC) and nipagin in the amount of 0.0001-0.09 g per 1 g of product.

10. Antiviral agent under item 1, characterized in that it comprises an antimicrobial agent selected from the group of silver-containing component in an amount of 0.001-0.05 g per 1 g of the agent, Quaternary ammonium compounds, chlorhexidine, Miramistin, broad-spectrum antibiotics in the amount of 0.0001-0.04 g per 1 g of product.

11. Antiviral agent under item 10, characterized in that as a silver-containing component it contains paverpol.

12. Antiviral agent under item 10, characterized in that the Quaternary ammonium compounds it contains atony or benzathine chloride or benzalkonium chloride.

13. Antiviral agent under item 10, wherein the broad-spectrum antibiotics selected from the group: amoxicillin, ampicillin, oxacillin, methicillin, cephalexin.

14. Antiviral agent under item 1, characterized in that as a pharmaceutically acceptable target additives it contains adiator, dimethyl sulfoxide, witepsol, soklin, tallow type CH, glycerin, polyethylene oxide, propylene glycol, proxanol is chosen-268, lactose, sucrose, calcium stearate and acetylcellulose.

15. Antiviral agent under item 1, characterized in that additionally it contains an antioxidant or local anesthetic drug.

16. Antiviral agent under item 15, characterized in that as an antioxidant it contains Trilon B and/or butylacetyl in the amount of 0.0001-0,0006 g per 1 g of product.

17. Antiviral agent under item 15, characterized in that as a local anesthetic drug it contains lidocaine in an amount of 0.01-0.05 g per 1 g of product.

18. Antiviral agent for PP. 1 -17, characterized in that it is a liquid, or soft, or solid dosage forms.

19. Antiviral agent under item 18, wherein the solid dosage form has an acid-resistant coating.

 

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