Percutaneous absorption enhancers, compositions containing same

Details Percutaneous absorption enhancers, compositions containing same Percutaneous absorption enhancers, compositions containing same

1986-11-17

1989-08-29

Schenkman, Leonard

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Cyclopentanohydrophenanthrene ring system doai

514263, 514415, 514452, 514467, 514947, A61K 3156

Patent

active

048617644

ABSTRACT:
Novel 1,3-dioxolanes (1,3-dioxyacyclopentanes) are provided along with new 1,3-dioxolanes (1,3-dioxacyclopentanes) compositions which are useful in enhancing the absorption of therapeutic agents through the skin of humans and animals. The method for enhancing skin penetration of therapeutic agents using 1,3-dioxacycloalkanes is also described.
The preferred compounds are 1,3-dioxolanes (1,3-dioxacyclopentanes) and 1,3-dioxanes (1,3-dioxacyclohexanes). The preferred compounds have the formula: ##STR1## wherein R, R.sub.0, R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5 and R.sub.6 are each independently selected from hydrogen and C.sub.1 to C.sub.18 aliphatic groups, preferably alkyl, alkenyl, and the halo, hydroxy, carboxy, carboxamide and carboalkoxy substituted forms thereof, with at least one of said R's an alkyl or alkenyl group of C.sub.4 to C.sub.18 and n=0 or 1; the total number of carbon atoms in all of said R groups being no more than 40, and preferably less than 20 and not more than 1 thereof containing 18 or more carbon atoms.

REFERENCES:
patent: 4012520 (1977-03-01), Youngdale
patent: 4085222 (1978-04-01), Rhodes et al.
patent: 4085223 (1978-04-01), Carissimi et al.
patent: 4557934 (1985-12-01), Cooper

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