Antiviral pharmaceutical composition

 

(57) Abstract:

The invention relates to the field of medicine and relates to a pharmaceutical composition with antiviral activity. The composition includes, g per 100 ml as the active ingredients of acyclovir 0,1-20,0 as auxiliary substances - derived cellulose is 0.1 to 15.0, mono - or disaccharide or a mixture of these sugars 12,0-65,0, alcohol, 0.5 to 45, 0mm; water to 100 ml, and optionally a preservative 0-3,0. The composition may further comprise a flavoring in an amount of 0.1 mg to 5.0 g per 100 ml of composition. A new pharmaceutical composition receive conventional methods in the form of a suspension. The composition meets the requirements of the pharmaceutical agent and stable during storage. 6 C.p. f-crystals, 1 table.

The invention relates to medicine, specifically to a pharmaceutical composition for the treatment of viral diseases of the skin and mucous membranes caused by a simple virus or herpes zoster, as well as for prevention of these diseases in patients with immune system disorders.

Acyclovir (or 9-(2-hydroxyethoxymethyl)guanine), inhibiting the multiplication of the herpes virus and with no impact on cellular metabolism uninfected cells, shows vysokoizbiratelnoe means, so 2, ed. 13th, Kharkov: Torsing, 1997, S. 357].

In medical practice, acyclovir can be used in the form of various dosage forms. However, when administered orally in the body, especially for children of the younger age group, the undoubted convenience are liquid dosage forms, including suspension.

Known pharmaceutical composition comprising acyclovir, a hydrophobic component, an organic solvent and auxiliary substances (patent of Russian Federation N 2128503, 1999). For example, wt.%: acyclovir 5,0; hydrophobic component 24,05; clearinterval 11,0; propylene glycol 29,0; triethanolamine 1,4; emulsifiers 8,0; preservatives 0,23; water - the rest.

However, the composition of auxiliary ingredients is not possible to obtain a liquid oral dosage form is a suspension of acyclovir with satisfactory quality indicators, in particular on the sedimentation stability.

The objective of this invention is to provide a pharmaceutical composition with an optimal combination of excipients for liquid oral dosage forms - suspension.

The technical result obtained by the invention is that the during storage.

This technical result is achieved by the fact that the proposed pharmaceutical composition with antiviral activity comprising as the active ingredients of acyclovir and as auxiliary substances, alcohol, water and, optionally, a preservative, and optionally contains a derivative of cellulose and a saccharide in the following ingredients, grams per 100 ml: acyclovir 0,1-20,0; derived cellulose is 0.1 to 15.0; saccharide 12,0-65,0; alcohol 0,5-45, 0mm; preservative 0-3,0; water to 100 ml.

According to the claimed invention, the use of auxiliary substances in the specified qualitative and quantitative ratios provides high sedimentation stability of the composition. So, in the shaking of the composition for 2 min is not visible delamination of the suspension over a period of time not less than 1 h and observed a uniform distribution of particles of the solid phase in the dispersion medium. In addition, the presence of a derivative of cellulose in the specified quantity allows to achieve stability indicators of quality for an extended period of time and thus increase the shelf life of the composition (over 2 years).

As a derivative of cellulose used microcrystalline cellulose, IU edocfile microcrystalline cellulose, or sodium carboxymethylcellulose, or their mixture.

As saccharide use of mono-or disaccharide, or their mixture. Examples of such substances are sucrose, glucose, xylitol, sorbitol and other sugars, preferably sorbitol.

As alcohol use pharmaceutically acceptable mono-, di - or polynuclear alcohols, for example ethanol, propylene glycol, glycerol or a mixture thereof, preferably glycerin.

The presence of a preservative and also increases the stability of the new structure to microbial contamination, but is not strictly required. In the role of preservative can be applied sorbic acid, benzoic acid, esters of n-oksibenzoynoy acid and other antimicrobial stabilizers permitted for medical use, preferably nipagin (methyl ester of n-oksibenzoynoy acid) or nipazol (propyl ether, n-oksibenzoynoy acid), or their mixture.

Introduction to the composition of corrigenda taste and smell (fragrance) allows to improve the organoleptic properties of the composition and, thus, the attractiveness of medicines for use in children, especially the younger age group. As flavoring you can use food flavouring essences, such as the AP is Fernie oil. The optimum content of the flavoring in the composition is from 0.1 mg to 5 g per 100 ml Lower limit of the content of the flavoring is determined by the presence or absence of the effect and the upper and economic expediency.

The proposed pharmaceutical composition is in the form of a syrup, which ensures manufacturability subsequent packaging and ease of use.

The claimed medicinal product may be obtained by known standard methods used to obtain suspensions.

The invention is illustrated in the examples in the table.

Example 1. Mix the water solution of saccharide (prepared from 50.0 g of sorbitol), 12.0 g of glycerol, 0.15 g nipagina, 0.05 g nipazola and suspension of microcrystalline cellulose (MCC, 2.0 g), sodium carboxymethylcellulose (NCMC, 0.6 g) and acyclovir (5.0 g), then bring 0.2 g of aromatic food essence (orange). Mix to obtain a homogeneous suspension volume was adjusted with water to 100 ml and give the extract with stirring for 30 minutes

The resulting suspension meets pharmaceutical agent (in appearance, sedimentation stability, microsuspension) satisfy the requirements of the pharmaceutical agent. The results of the fabrication of the suspension shown in the table.

1. Antiviral composition comprising as the active ingredients of acyclovir and as auxiliary substances, alcohol, water and optionally a preservative, characterized in that it additionally contains a derivative of cellulose and mono - or disaccharide or a mixture of the following ingredients, grams per 100 ml:

Acyclovir - 0,1-20,0

Derived cellulose is 0.1 to 15.0

Mono - or disaccharide or a mixture - 12,0-65,0

Preservative - 0-3,0

Alcohol is 0.5 - 45,0

Water ml 100

2. The antiviral composition according to p. 1, characterized in that it further comprises a flavoring in an amount of 0.1 mg to 5.0 g per 100 ml of composition.

3. The antiviral composition according to p. 2, characterized in that as a flavoring food contains aromatic essence.

4. Antiviral composition under item 1 or 2, characterized in that as a derivative of cellulose contains microcrystalline cellulose, or sodium carboxymethylcellulose, or their mixture.

5. Antiviral composition under item 1 or 2, characterized in that as monosaccharide contains sorbitol.

6. Antiviral composition under item 1 or 2, characterized in that to the fact is made in the form of a suspension.

 

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