Transdermal and trans-membrane delivery of drugs
AssigneeConrex Pharmaceutical Corporation
InventorDean Hseih
Life of this patent
Estimating the term…
Abstract
The rate of absorption of drugs across skin and other body membranes such as mucous membranes and the blood brain barrier is enhanced by adding to the drug composition a compound which enhances the rate. This compound may be macrocyclic ester, diester, amide, diamide, amidine, diamidine, thioester, dithioester, thioamide, ketone or lactone. The macrocyclic ketone contains at least 12 carbon atoms.
Claims53
A method for increasing the rate of passage of a drug across animal or human skin, mucous membranes, or the blood brain barrier which comprises applying to the skin, mucous membrane or blood brain barrier a composition comprising an effective amount of the drug, a pharmaceutical carrier, and from about 0.1 to about 50% by weight of a compound (with or without dissolving in a solvent) effecting such increase in rate, said compound having the structure:
- ##STR6## wherein X and Y are oxygen, sulfur or an imino group of the structure ##STR7## or .dbd.N--R, with the proviso that when Y is an imino group, X is an imino group, and when Y is sulfur, X is sulfur or an imino group, A is a group having the structure ##STR8## wherein X and Y are as defined above, m and n are integers having a value from 1 to 20 and the sum of m+n is not greater than 25, p is an integer having a value of 0 or 1, q is an integer having a value of 0 or 1, r is an integer having a value of 0 or 1, and each of R, R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, and R.sub.6 is independently hydrogen or an alkyl group having from 1 to 6 carbon atoms which may be straight chained or branched, provided that only one of R.sub.1 to R.sub.6 can be alkyl group, with the proviso that when p, q and r are 0 and Y is oxygen, then m+n is at least 11, and with the further proviso that when X is an imino group, q is equal to 1, Y is oxygen, and p and r are 0, then m+n is at least 11.
A composition for administering a drug across skin, mucous membranes or blood brain barrier which contains an effective amount of a drug, a pharmaceutical carrier, and from about 0.1% to about 50% by weight of a compound (with or without dissolving in a solvent) which increases the rate of passage of the drug across the skin, the mucous membranes, or the blood brain barrier, said compound having the structure:
- ##STR14## wherein X and Y are oxygen, sulfur or an imino group of the structure ##STR15## or .dbd.N--R, with the proviso that when Y is an imino group, X is an imino group, and when Y is sulfur, X is sulfur or an imino group, A is a group having the structure ##STR16## wherein X and Y are as defined above, m and n are integers having a value from 1 to 20 and the sum of m+n is not greater than 25, p is an integer having a value of 0 or 1, q is an integer having a value of 0 or 1, r is an integer having a value of 0 or 1, and each of R, R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, and R.sub.6 is independently hydrogen or an alkyl group having from 1 to 6 carbon atoms which may be straight chained or branched, provided that only one of R.sub.1 to R.sub.6 can be alkyl group, with the proviso that when p, q and r are 0 and Y is oxygen, then m+n is at least 11, and with the further proviso that when X is an imino group, q is equal to 1, Y is oxygen, and p and r are 0, then m+n is at least 11.
Dependencies are inferred from the claim text.