Drug – bio-affecting and body treating compositions – Designated organic nonactive ingredient containing other... – Carbohydrate or lignin – or derivative
Patent
1983-05-13
1986-06-03
Friedman, Stanley J.
Drug, bio-affecting and body treating compositions
Designated organic nonactive ingredient containing other...
Carbohydrate or lignin, or derivative
514772, 514789, A61K 4700
Patent
active
045930481
DESCRIPTION:
BRIEF SUMMARY
TECHNICAL FIELD
This invention relates to a base composition capable of increasing the percutaneous absorption of drugs, to a pharmaceutical composition for external use in which said base composition is used, and to a method of promoting the percutaneous absorption of drugs.
BACKGROUND ART
The drugs so far administered to the outer skin have served the purpose of producing a local effect on the outer skin or hypodermal tissues, such as a bactericidal, disinfecting or analgesic effect. However, in recent years, attempts have also been made to administer drugs having a systemic activity to the outer skin, instead of by peroral administration or injection. The percutaneous administration of a drug, particularly a systemic drug, has the following advantages, among others: the drug efficacy can easily be maintained for a long while; the rate of drug absorption can easily be controlled, so that adverse effects due to overdosage can be minimized; since the drug is sparingly metabolized in the liver by the first pass effect as found in the case of oral administration, the drug can be used effectively; and even a drug possibly causing gastrointestinal disorders upon oral administration, such as indomethacin, can be administered safely.
However, the normal skin, which has a body-protecting action, is generally capable of resisting drug absorption or permeation. Therefore, drugs (especially systemic drugs), when simply administered in the conventional forms of ointment, lotion and so on, can scarcely be absorbed into the body in amounts sufficient to produce a satisfactory pharmacological effect.
DISCLOSURE OF THE INVENTION
Under these circumstances, the present inventors conducted intensive research and, as a result, obtained the following findings:
(1) That a composition comprising a lower alcohol and at least one adjuvant selected from among a saturated aliphatic hydrocarbon containing 5 to 20 carbon atoms, which may optionally be halogen-substituted, a carboxylic acid alcohol ester containing 13 to 24 carbon atoms in total, and an ether can improve the skin permeation and percutaneous absorption of drugs, and
(2) That the above-mentioned composition can be used as a base for drugs to be applied to the skin. These findings have led to the present invention.
Accordingly, a primary object of the present invention is to provide a base composition for external preparations which is capable of increasing the skin permeation and percutaneous absorption of drugs.
A second object of the invention is to provide a pharmaceutical composition for external use which is satisfactory in skin permeation and percutaneous absorption of drugs.
A third object of the invention is to provide a method of increasing the skin permeation and percutaneous absorption of drugs.
Thus, the present invention provides:
(1) A base composition for external preparations which comprises a lower alcohol and at least one adjuvant selected from among a saturated aliphatic hydrocarbon containing 5 to 20 carbon atoms, which may optionally be halogen-substituted, a carboxylic acid alcohol ester containing 13 to 24 carbon atoms in total, and an ether;
(2) A pharmaceutical composition for external use which comprises a drug and the above-mentioned base composition; and
(3) A method of promoting the skin permeation and percutaneous absorption of a drug which comprises administering the drug to the skin together with the above-mentioned base composition.
The lower alcohol to be used in the practice of the present invention is preferably a monohydric lower alcohol containing 1 to 4 carbon atoms, including methyl alcohol, ethyl alcohol, n-propyl alcohol, isopropyl alcohol, n-butyl alcohol, isobutyl alcohol, sec-butyl alcohol and t-butyl alcohol. Among these, ethyl alcohol is particularly preferred.
The saturated aliphatic hydrocarbon containing 5 to 20 carbon atoms, which may optionally be halogen-substituted, may be acylic (straight-chained or branched) or cyclic. The straight-chained one includes among others n-pentane, n-hexane, n-heptane, n-octane, n
REFERENCES:
patent: 4309414 (1982-01-01), Inagi et al.
Chem. Abst., 97 (150740h) (1982), 98 (221852e)-1983, & 89 (48905p) (1978).
Sato Susumu
Takakura Umiko
Tamada Mitsuru
Friedman Stanley J.
Nitto Electric Industrial Co. Ltd.
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