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US 4,731,360 AGranted
Acylcarnitines as absorption-enhancing agents for drug delivery through mucous membranes of the nasal, buccal, sublingual and vaginal compartments
AssigneeMerck & Co., Inc.
InventorsJose Alexander, A. J. Repta, Joseph A. Fix
Life of this patent
Estimating the term…
Abstract
Acylcarnitine used as a nasal, buccal, sublingual and vaginal drug absorption enhancing vehicle for poorly absorbed drugs.
Claims4
A method of enhancing the rate of absorption of a .beta.-lactam drug administered to the nasal, buccal, sublingual or vaginal cavity, which comprises administering a composition comprising a therapeutically effective dosage amount of said drug and an acylcarnitine absorption enhancing agent of the formula:
- [(CH.sub.3).sub.3 N.sup.+ CH.sub.2 CH(OCOR)CH.sub.2 CO.sub.2 H]X.sup.-
- wherein R is saturated alkyl (C.sub.2 -C.sub.20), alkenyl (C.sub.2 -C.sub.20) with 1 to 6 double bonds, hydroxyakyl (C.sub.2 -C.sub.20) with 1 to 3 hydroxy groups, ketoakyl (C.sub.4 -C.sub.20), unsaturated hydroxyakyl(C.sub.5 -C.sub.20), carboxyakyl (C.sub.4 -C.sub.20), arylakyl (C.sub.5 -C.sub.20), alkylaryl (C.sub.7 -C.sub.20) or carbalkoxyalkyl (C.sub.5 -C.sub.20) and X is a pharmaceutically acceptable counterion.
Dependencies are inferred from the claim text.