Antiherpetic agent

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to agent possessing antiviral action, and may be used for treating herpes infections, including lip sore. The given agent contains the ingredients, wt %: a solution readily permeable through biological membranes of soapy amphiphilic complex of high-polymer RNA of Saccharomyces cerevisiae and oleic acid (as an interferon inducer) - 49.96; Vaseline oil - 20; Tween-80 - 17; Emulsifier T-2 - 13; Chlorhexidine Bigluconate - 0.04.

EFFECT: preparation shows high antiherpetic activity, good tolerability and ability to reduce a recurrence rate considerably.

 

The invention relates to the field of medicine and the pharmaceutical industry, in particular to the means possessing antiviral effect, and can be used to treat herpes infections, including herpes lips.

Known drug Acyclovir" company Glaxo Wellcome (UK) for the treatment of herpes and other viral infections, which is an acyclic nucleoside analogue of guanine, obtained by synthesis. Ointment form contains 3% of acyclovir and is used to treat Herpes simplex genital [1]. Other antiherpetic agent is the ointment "Laifan" (made in Latvia) containing 0.05% of high-molecular inducer of interferon natural origin, representing double-stranded RNA phage , with a molecular weight above 200,000 in [2].

Closest to the proposed is effective antiherpetic agent main active principle of which is double-stranded RNA derived from killer yeast strains [3]. This tool is in the form of a topical composition contains 0.15 to 0.5 wt.% complex sodium salts of single - and double-stranded ribonucleic acids from Saccharomyces cerevisiae (complex ds RNA)enclosed in the aqueous phase of emulsion bases of the following composition: liquid paraffin 20%tween - 80 - 17%, emulsifier T-2 (13%), chlorhexidine digluconate - ,04% water to 100%. It is effective when used for dermatological treatment of lesions caused by the herpes virus has a prolonged action and harmless to human body.

However, the complex ds RNA derived from scarce raw materials, it is costly and complex to manufacture.

The aim of the present invention is to reduce the costs in industrial production of anti-herpes ointment.

The objective is achieved by the fact that the wax composition of the complex ds RNA is replaced by natural highly effective inducer of interferon extracted from dry Baker's yeast using titrated with alkali oleic acid is easily diffuse through biological membranes soapy amphiphilic high polymer complex RNA of Saccharomyces cerevisiae with oleic acid enclosed in the aqueous phase is the basis for the following content, wt.%:

The solution easily penetrates through biological membranes soapy amphiphilic high polymer complex RNA of Saccharomyces cerevisiae with oleic acid - 49,96

Liquid paraffin - 20

Tween-80 - 17

Emulsifier T-2 - 13

Chlorhexidine digluconate - 0,04

An example of the proposed method

300 g of dry Baker's yeast {Saccharomyces cerevisiae, Novosibirsk yeast factory, GOST 28483-90) suspended portions (first portions of the pinch, the first 2-3 pinches for a few seconds before boiling) for -6 min 5 l high pan in 3 l of boiling distilled water, containing 20 ml of 2.5 M NaOH titrated to 50.3 ml of oleic acid. The temperature of the suspension was not lower than 98°C., the Suspension is boiled for 40 min at 98-100°C stirring occasionally. After 10, 20 and 30 min after suspension last portion of yeast in boiling suspension was added to 10 ml of 2.5 M NaOH. After extraction, the suspension was cooled to 20-30°C in the sink in 3 changes of cold water for ~20 min and then centrifuged in a centrifuge S70D firm "Janetzki, Germany (3000-3200 min-1, 10 min, room temperature). The supernatant (~1.7 l), containing the high polymer solution of yeast RNA in complex with oleic acid, was filtered through 4 layers of sterile gauze, was added freshly distilled water to 2 l and stirred. After that used for the preparation of ointments.

The ointment was prepared as follows: 20 g of paraffin oil, 17 g of tween-80 and 13 g of emulsifier T-2 were mixed in a glass beaker 400 ml) and was heated on a water bath (75°C) until complete melting of the mixture; ~50 ml of a solution of high polymer yeast RNA in complex with oleic acid, heated to 75°C, was slowly injected into the molten mass under stirring; reduce the temperature to 40°C and was added 200 μl of a 20%aqueous solution of chlorhexidine digluconate. The agitation led to the formation of stable emulsions. Ointment (estimated market sq is th name - Metalang-2i) was packaged in bottles of dark glass 5 g and closed with plastic caps. Kept in the refrigerator at 4-10°C.

Antiherpetic properties of the drug Metalang-2i have been tested by us in Novosibirsk in 2010-2012 in the treatment of herpes of the lips themselves and family members (5 persons). The ointment was applied on the affected by herpes virus 3-4 times a day for two days. Thus by the end of the second day the wound had dried up. Significantly decreased the recurrence rate.

Thus, the drug Metalang-2i is an effective anti-herpes agent, and after the appropriate pre-clinical and clinical trials can be recommended for the treatment of herpes virus, including herpes lips.

Work is executed at financial support of the Ministry of education and science of the Russian Federation (State contract no 16.512.11.2018 from 11.02.2011).

Sources of information

1. Ershov FI, Chizhov, NP, Tselakova AB // Antivirals (Handbook), St. Petersburg 1993, p.23-24.

2. Ershov FI, Chizhov, NP, Tselakova AB // Antivirals (Handbook), St. Petersburg 1993, s-70.

3. Patent RU 2123339 C1, 20.12.1998.

Antiherpetic agent-based interferon inducer for external use based on the emulsion, including vaseline oil, tween-80, emulsifier T-2 and chlorhexidine biglycan is, characterized in that it as interferon inducer contains easily diffuse through biological membranes soapy amphiphilic high polymer complex RNA of Saccharomyces cerevisiae with oleic acid, enclosed in the aqueous phase is the basis for the following content, wt.%:

The solution easily penetrates through
biological membranes soapy
amphiphilic high polymer complex
RNA of Saccharomyces cerevisiae with oleic acid49,96
Vaseline oil20
Tween-8017
Emulsifier T-213
Chlorhexidine digluconate0,04



 

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