Microemulsion preparation containing a slightly absorbable subst

Drug – bio-affecting and body treating compositions – Dispersion or emulsion

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Details

514807, 514808, A61K 9107

Patent

active

059488255

DESCRIPTION:

BRIEF SUMMARY
TECHNICAL FIELD

This invention relates to a microemulsion preparation that contains a physiologically active substance such as a high-molecular weight peptide which inherently can not be easily absorbed through the skin or mucous membrance but which is incorporated in such a way that its absorption through the skin or mucous membrance is improved.


BACKGROUND ART

The preparation of microemulsions is one attempt that has been made to improve the absorption of physiologically active substances through the skin or mucous membrane.
Microemulsions have been proposed that use alcohols such as octanol and butanol. However, they are not particularly suitable for oral administration since the alcohols they use have malodors. If microemulsions are prepared using large amounts of ionic surfactants, they are irritant to the mucous membrane and skin.
Peptides such as insulin and calcitonin have low absorbability through the mucous membrane. With a view to dealing with this problem, the use of absorption enhancers such as bile salts has been attempted but they have been found to damage or destroy epithelial cells of the mucous membrane.


DISCLOSURE OF INVENTION

An object of the invention is to prepare a microemulsion that is less irritating to the mucous membrane and skin and which uses neither malodorous higher alcohols such as butanol and octanol nor conventional absorption enhancers such as bile salts that will damage epithelial cells. It is another object of the invention to improve the absorption of certain physiologically active substances through the skin or mucous membranes by means of preparing such microemulsions.
The invention provides a microemulsion preparation that successfully solves the aforementioned problems of the prior art by combining at least two specified surfactants.
The surfactants to be used in the invention are selected from the following three classes (a), (b) and (c), among which a surfactant in class (c) is essential and combined with a surfactant in either one of classes (a) and (b). The surfactants in the respective classes are as follows: atoms); in 30-80, preferably 40-60, moles on average); acid is a saturated or unsaturated aliphatic acid having 16-20, preferably 18, carbon atoms and ethylene glycol is added in 10-40 moles on average); and carbon atoms and oxyethylene is added in 4-25 moles on average); and saturated or unsaturated aliphatic acid having 16-20, preferably 18, carbon atoms and it is added in 1-2 moles per mole of glycerin, which is added in 0-4 moles); unsaturated aliphatic acid having 16-20, preferably 16-18, carbon atoms and added in 1-3 moles); and in 3-20, preferably 8-12, more preferably 10, moles on average).
The dispersion media that can be used in the invention are fats or oils that are not irritating to the skin or mucous membranes and which are liquid at room temperature or dissolve when heated by the body temperature to become liquid. Specific examples that may be used include edible vegetable or animal oils (aliphatic acid glycerin esters) such as soybean oil, sesame oil and olive oil; saturated or unsaturated aliphatic acids; and mono-, di- or triglycerin esters of middle-chain aliphatic acids (C.sub.6 -C.sub.18).
The microemulsion of the invention can be prepared by a conventionally known method as follows.
A suitable combination of surfactants is added to an oil component as a dispersion medium and the ingredients are agitated and mixed thoroughly to prepare a uniform oily mixture. When the oil component is solid at room temperature, it is heated to melt the oil component before the surfactants are added and mixed. An active ingredient, or a physiologically active substance, such as calcitonin, erythropoietin or other peptide is dissolved in water.
The thus prepared aqueous solution of the physiologically active substance is added to the separately prepared oily mixture under agitation. Further agitation yields a microemulsion as a clear liquid. If necessary, an additional amount of the oil component may be added to adjust the concentration of the ac

REFERENCES:
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patent: 4931210 (1990-06-01), Takahashi et al.
patent: 5037653 (1991-08-01), Dawson
patent: 5281580 (1994-01-01), Yamamoto et al.
patent: 5496811 (1996-03-01), Aviv et al.
patent: 5576016 (1996-11-01), Amselem et al.
patent: 5662932 (1997-09-01), Amselem et al.
patent: 5716637 (1998-02-01), Anselem et al.

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