Enhancing absorption of drugs from gastrointestinal tract using acylcarnitines
AssigneeMerck & Co., Inc.
InventorsJose Alexander, Joseph A. Fix
Life of this patent
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Abstract
Acylcarnitines used as drug absorption enhancing agents for orally and rectally administered drugs.
Claims16
A method of enhancing the rate of gastrointestinal absorption of an orally or rectally administered poorly absorbed drug selected from the group consisting of .beta.-lactam antibiotics, aminoglycoside antibiotics, antiviral agents, amino acids, smooth muscle relaxants and polypeptides, said method comprising the steps of preparing a dosage form capable of being orally or rectally absorbed, said dosage form comprising a therapeutically effective dosage amount of said drug and an absorption enhancing effective amount of an acylcarnitine agent of the formula:
- ##STR2## wherein R is saturated acyl(C.sub.2 -C.sub.20), acyl(C.sub.2 -C.sub.20) with 1 to 6 double bonds, hydroxyacyl(C.sub.2 -C.sub.20) with 1 to 3 hydroxy groups, ketoacyl(C.sub.4 -C.sub.20), unsaturated hydroxyacyl(C.sub.5 -C.sub.20) or carbalkoxyacyl(C.sub.5 -C.sub.20) and X is a pharmaceutically acceptable counterion.
A pharmaceutical composition for enhancing gastrointestinal tract absorption of an orally or rectally administered formulation comprising a therapeutically effective dosage amount of a poorly absorbed drug selected from the group .beta.-lactam antibiotics, aminoglycoside antibiotics, antiviral agents, amino acids, smooth muscle relaxants and polypeptides and an absorption enhancing effective amount of an acylcarnitine agent of the formula:
- ##STR3## wherein R is saturated acyl(C.sub.2 -C.sub.20), acyl(C.sub.2 -C.sub.20) with 1 to 6 double bonds, hydroxyacyl(C.sub.2 -C.sub.20) with 1 to 3 hydroxy groups, ketoacyl(C.sub.4 -C.sub.20), unsaturated hydroxyacyl(C.sub.5 -C.sub.20) or carbalkoxyacyl(C.sub.5 -C.sub.20) and X is a pharmaceutically acceptable counterion.
Dependencies are inferred from the claim text.