SU1364339A1 - Base for suppository - Google Patents

Abstract

In order to increase the bioavailability of the drug substance from the base and the uniformity of its distribution, the base contains, in wt.%: Solid re-esterified fat 92-99.4; silicon dioxide 0) 1-3; distilled monoglycerides or glycerol monostearate 0.5-5. The base is prepared by mixing solid pre-esterified fat with an emulsifier, silicon dioxide is added with heating, then the mass is cooled.

Description

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The invention relates to medicine, namely to pharmacology, and can be used in the manufacture of drugs to expand the range of rectal and vaginal dosage forms with a wide range of effects.

The purpose of the invention is to increase the bioavailability of the drug substance from the base and the uniformity of its distribution.

The basis for suppositories has the following composition, May.%

Hard Reterium

fatsirovanny fat 92,0-99,4 Silicon dioxide 0.1-3.0 Distilled or monoglycerides

monostearate gly

cerin 0.5-5.0

Trans-oleic acid is contained in the solid transesterified fat. The ratio of silica to trans-oleic acid in the base is 0.01-0j4. In combination with an emulsifier (distilled monoglycerides or glycerol monostearate) in the amount of 0.5-5.0, such a composition of the base creates the most favorable conditions. for even distribution of hard-to-disperse drugs.

With the introduction of silicon dioxide less than 0.1 wt.%, Sedimentation of the drug occurs. The introduction of silicon dioxide more than 3.0 wt.% Reduces the fluidity of the base, leads to the formation of many cracks when cooled candles. The presence of silica at the base makes it possible to form a resistant gel with aqueous solutions of drugs.

The introduction of the emulsifier below O, 5 wt. leads to a decrease in the plasticity of candles and their cracking, an increase in sedimentation of medicinal substances. An increase in the emulsifier content above 5% by weight increases the melting point and pour point of the mass.

A suppository base is prepared by mixing solid, transesterified fat with an emulsifier, then silica is added with heating. The resulting mass is cooled.

Example 1. The basis for suppositories has the following ratio of components, wt.%:

Solid interesterified fat

98.5

1.0

(0.017)

Silicon dioxide (Aerosil) Stearic acid monoglycerides (glycerol monostearate) 0.5 Physical and chemical indicators of the base:

Temperature

melting, C35

Solidification temperature, c32 Difference between melting point and solidification temperature, c3 Hardness at 20 ° C, kg / e2 2.8 Iodine number 6.9 On this basis, vaginal suppositories with trichomonacide and suppositories with papaverine hydrochloride and dibazole have been developed. The preparations are well compatible with the base, are evenly distributed in it, have good bioavailability from the base. In the manufacture of candles on the surface there are no cracks, grooves. Suppositories correspond to pharmacopoeia become m. Vaginal supposi-, - torii with trichomonacid are allowed by the pharmacological committee.

Example 2. The basis for suppositories has the following ratio of components, wt.%:

Hard-interesterified fat

WITH

96.0

ABOUT

five

Silica (Aerosil) 1.5

Stearic monoglycerides (glycerol monostearate) 2.5 Physical and chemical indicators of the base:

Temperature melting: 36, 0

nor, C solidification temperature, s

33.0

3

Difference between melting temperature and solidification temperature, C3.0 Hardness at 20 ° C, kg / s 4.0 Iodine number 6.9 On this basis, candles with potassium bicarbonate are made. The drug is evenly distributed at the base, sedimentation is not observed for 8 hours at 38 ° C, candles do not have cracks and tears, the bioavailability of the preparation from the base is good.

Candles are responsible for all indicators of the VFS project during storage for 1.5 g.

EXAMPLE 3. A suppository base contains the following components, in wt%:

Solid interesterified fat

m

(--- 0.4) one

92.0

Silica (Aerosil) 3.0

Stearic acid monoglycerides (glycerol monostearate) 5.0 Physical and chemical indicators are based on

you:

39

34

Melting point

° С

Hardening temperature, ° C Difference between melting point and hardening temperature, ° C5 Hardness at 20 ° C, kg / s 4.5 Iodine value6.9 Candles with rosehip oil are made on this basis. Candles are uniform and the smearing surface of the candles is satisfactory. The bioavailability of the drug is good. There is no difficulty in making candles.

Example 4. The basis for suppositories has the following ratio of components, wt.%:

643394

Solids transesterified fat

(--- 0.01) 99.4

5 ™

Silicon dioxide

(aerosil) 0,1

Distilled monoglycerides0, 5 10 Physical and chemical indicators basis:

Melting point, C34.5 Hardening temperature - 15 Devi, C31.5 Difference between the pinning temperature and the hardening temperature, ° C3 20 Hardness at 20 ° С,

kg / ev2.5

Iodine Number6.9

On this basis, made candles with salazopyridazin and vaginal 25 suppositories with syntomycin.

The preparations are evenly distributed in the base; when removed from the shape of a candle, they do not have cracks, plumes, do not collapse with a strong blow. 30 A good bioavailability of drugs from the base is observed. Candles meet the requirements of pharmacopoeial articles.

35

Claims (1)

Invention Formula A suppository base containing solid transesterified fat and an emulsifier, characterized in that, in order to increase the bioavailability of the drug substance from the base and its uniformity of distribution, it additionally contains silicon dioxide and as an emulsifier Distilled monoglycerides and glycerol monostearate in the following ratio ingredients, May,% Solid interesterified fat 92.0-99.4 Silicon dioxide 0.1-3.0 Distilled monoglycerides or glycerol monostearate 0.5-5.0