Oral lipid medicinal composition

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Peptide containing doai

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514 11, 514 18, 514 19, 514 21, 514558, A61K 3726, A61K 3700, A61K 3120

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active

051207109

ABSTRACT:
To improve the absorption of actve ingredients, which are not adequately bio-available on oral administration, an oral lipid medicinal composition is formed by combining a semi-solid, lipophilic component with a solid, water-soluble component. The semi-solid component is a homogeneous lipid mixture that exists as a hard fat with thermally reversible fat/liquid melting property, at least 95% of which is present in the liquid aggregate state below the body temperature of 37.degree. C. and comprises monoacyl-, diacyl-, and triacylglycerides of saturated vegetable fatty acids with chain lengths ranging from 6 to 18 carbon atoms, preferably comprising a mixture of 40 to 60% monoacyl- and diacylglycerides and 40 to 60% triacylglycerides, in which the active ingredients are either dissolved, suspended or emulsified. The solid component comprises a non-diffusible, water-soluble shell which is not chemically bonded to the lipid compound and envelops the entire lipid compound and is preferably made of gelatin or starch. The use of protease inhibitors in the lipid mixture can improve the permeation conditions for peptides and proteins. The use of highly disperse silicon dioxide can stabilize the suspension formulations. Physical-chemical and biochemical aspects of the oral lipid medicinal form yield improvements for the absorption of drugs that are not adequately bio-available on oral administration.

REFERENCES:
patent: 4434159 (1984-02-01), Sekine et al.
patent: 4619794 (1986-10-01), Hauser
The Merck Index, Merck & Co., Inc., Rahway, N.J., pp. 137, 138, 249, 559, 789-791, and 1373 (1989).
Chemical Abstracts (93:101480g) 1980.
Chemical Abstracts (87:73384j) 1977.
Chemical Abstracts (108:101382e) 1988.

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