Pharmaceutical compositions for topical application
OwnerIzhak Blank, Alon Blankinventors
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Abstract
A pharmaceutical and cosmetical preparation which rapidly penetrates through human skin, and which thus is able to bring about the rapid transdermal penetration of a wide variety of active ingredients. The compounds which enhance the rate of dermal penetration are also anti-oxidative agents and thus protect active substances susceptible to oxidative degradation. Preferred agents enhancing penetration and which protect against oxidation are higher esters and higher amides of thioglycolic acid and of mercaptopropionic acid. The preparations can be in the form of mixtures or there may be prepared chemical compounds which are a combination of the active substance and the said thioacids.
Claims11
Pharmaceutical and cosmetic compositions for enhancing transdermal penetration which provide for antioxidative protection against degradation of oxidation sensitive active ingredients, comprising a non-irritating combination of a higher ester or higher amide of thioglycolic acid or mercaptopropionic acid of the general formula:
- HS--(CH.sub.2).sub.n COQ
- where n is 1 or 2;
- Q is --OR or --NHR, R being an alkyl chain from 8 to 32 carbon atoms, a pharmaceutically active substance or cosmetically active substance and at least one member selected from the group consisting of solvents, thickeners, emollients, surfactants, film-forming polymers and occluders.
A compound of the formula
- HS--(CH.sub.2).sub.n --CONHQ'
- where n is 1 or 2, and where Q' is
- --C.sub.12 H.sub.25 or --C.sub.18 H.sub.37.
- 9.
A compound of the formula:
- HS--(CH.sub.2).sub.n --COR.sup.1
- where R.sup.1 is a tocopheryl residue and n is 1 or 2.
A method for enhancing transdermal penetration of a pharmaceutically active substance or a cosmetically active substance which provides antioxidative protection against degradation of oxidation sensitive active ingredients, comprising applying a non-irritating combination of a higher ester or higher amide of thioglycolic acid or mercaptopropionic acid of the general formula:
- HS--(CH.sub.2).sub.n COQ
- where n is 1 or 2;
- Q is --OR or --NHR, R being an alkyl chain from 8 to 32 carbon atoms, a pharmaceutically active substance or cosmetically active substance and at least one member selected from the group consisting of solvents, thickeners, emollients, surfactants, film-forming polymers and occluders.
Dependencies are inferred from the claim text.