RU2098081C1 - Benzyl benzoate in aqueous-emulsion formula - Google Patents

Abstract

FIELD: pharmaceutical industry. SUBSTANCE: invention is developed to obtain a composition ensuring to get benzyl benzoate in both ointment and gel formula. Invention uses hydroxyalkylated aliphatic alcohols as surface-active substance of the general formula: R-O-

Description

 Benzyl benzoate in aqueous emulsion form.

 The invention relates to the pharmaceutical industry, in particular to the formulation (composition) of benzyl benzoate in gel and ointment form, used as a medicine for external use against scabies and pediculosis (gel and ointment of benzyl benzoate 10% for children, gel and ointment of benzyl benzoate 20% for adults )

Known ointment benzyl benzoate composition, wt. medical benzyl benzoate 10.0 or 20.0; triethanolamine 5.0; stearic acid 20.0; polyethylene glycol 400 5.0; purified water to 100 [1]
An ointment of benzyl benzoate composition, wt. medical benzyl benzoate 10.0 or 20.0; zacap 2.0; caustic soda 0.2; tween-80 1.0; nipagin 0.08; nipazole (propyl-2-hydroxybenzoate) 0.02; purified water to 100 [2]
However, the known compositions, in particular the triethanolamine salt of stearic acid and tween-80 (ethoxylated sorbitan mono-oleate) used in these compositions as surface-active substances (surfactants) do not allow obtaining benzyl benzoate in gel form, which is optimal for providing increased activity of pharmacological effects and stability during storage. In addition, the production of benzyl benzoate ointments according to known formulations (compositions) in connection with the high viscosity of the system requires the use of powerful high-speed mixers.

 The purpose of the invention is the development of a composition that allows to obtain benzyl benzoate in both gel and ointment forms and at the same time simplify the technology and reduce energy consumption when they are received.

,
где R алкил с числом углеродных атомов от 7 до 14;
n число оксипропильных групп от 12 до 16;
m число оксиэтильных групп от 45 до 60, со средней молекулярной массой в пределах 2500-3500 и одновременно введением в состав мази из водно-эмульсионного раствора бензилбензоата 22,5-32,0 мас. ПАВ.This goal is achieved by using known surfactants of known oxylalkylated fatty alcohols of the general formula

,
where R is alkyl with the number of carbon atoms from 7 to 14;
n the number of hydroxypropyl groups from 12 to 16;
m the number of hydroxyethyl groups from 45 to 60, with an average molecular weight in the range of 2500-3500 and at the same time the introduction of the composition of the ointment from the aqueous emulsion solution of benzyl benzoate 22.5-32.0 wt. Surfactant.

Example. Benzyl benzoate (20 h) and surfactant (30 h) are charged into a stainless steel or enameled reactor. The mixture is heated to 65 ^{° C.} until the surfactant is completely melted and dissolved in benzyl benzoate. Then, with stirring, continuously or in portions for 1 hour, a previously prepared solution of 95% ethyl alcohol (16 hours) in water is loaded. Stirring at 65 ^{° C. is} continued until a clear colloidal solution is obtained, after which perfume (0.2 h) is added, for example, linalool, geraniol, citral, bornyl or isobornyl acetate, etc. and put up. When cooled to room temperature, the product is a clear, colorless gel. Benzyl benzoate ointment is also prepared in a similar manner.

 The table shows the compositions of the gel and ointment.

All components that make up the gel and ointment of benzyl benzoate at 65 ^o C are liquids, and in fact the process of preparing the gel and ointment is to prepare a colloidal solution. For this reason, in contrast to the known compositions [1, 2] where the system has a high viscosity, mixers with a low speed and electric motors with a small power can be used. For example, to prepare a gel or ointment of benzyl benzoate in a reactor with a capacity of 40 l, an electric motor with a power of 200 W and a stirrer with a rotation frequency of 10 rpm are used.

The benzyl benzoate ointment obtained by the proposed and known [1, 2] formulations is stored under ordinary conditions at a temperature of about 20 ^o C. In contrast to the ointment, the benzyl benzoate gel is stored at a temperature of from -35 to +35 ^o C.

 Clinical trials have shown that, in comparison with known formulations, the gel and ointment of benzyl benzoate of the claimed composition have the following advantages: pleasant smell; easily absorbed into the skin; good tolerance even in patients with eczematization phenomena and in patients with an unfavorable allergic history; do not stain underwear and bedding, do not leave greasy spots on it; have an optimum consistency for work; greater pharmacological activity against scabies mites, especially for benzyl benzoate gel.

 Based on clinical trials, the gel and ointment of the benzyl benzoate of the claimed composition are recommended for approval by the pharmaceutical department of the Department of Health as an anti-scab.

Claims (1)

A water-emulsion solution of benzyl benzoate containing surfactants, characterized in that it contains oxyalkylated fatty alcohols of the general formula as a surfactant

with an average mol.m. within 2500 3500,
where R is alkyl with the number of carbon atoms 7 to 14;
n 12 16, the number of hydroxypropyl groups;
m 45 60, the number of hydroxyethyl groups,
in an amount of 22 32 wt. from the total composition of the aqueous emulsion solution.

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