Oral absorption enhancement of carboxylic acid pharmaceuticals using (5-alkyl-2-oxo-1,3-dioxolen-4-yl)methyl ester group
AssigneeMerck & Co., Inc.
InventorBurton G. Christensen
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Abstract
The (5-R-2-oxo-1,3-dioxolen-4-yl)methyl moiety: ##STR1## wherein R is loweralkyl of 1-6 carbon atoms, especially methyl or t-butyl; when utilized as an ester on a pharmaceutical having a carboxylic acid functionality, enhances oral absorption of the pharmaceutical. This effect is applicable to a broad range of pharmaceutically active substances, including antibiotics, and antihypertensives as well as other classes of therapeutic agents.
Claims11
The (5-alkyl-2-oxo-1,3-dioxolen-4-yl)methyl ester of a carboxylic acid wherein alkyl has 1-6 carbon atoms and wherein said carboxylic acid is cefoxitin, methyldopa, 3.beta.-[2-methoxyimino-2-(2-amino-1,3-thiazolol-4-yl)acetamido]monobactam ic acid, 2-ethylthio)-6.beta.-(1R-hydroxyethyl)-penem-3-carboxylic acid or fosfomycin.
The compound 4-t-butyl-1,3-dioxol-2-one-5-ylmethyl(S)-3-hydroxy-.alpha.-methyltyrosinat e(2R,3R)hydrogentartrate, and in hemihydrate form.
The compound 4-methyl-1,3-dioxol-2-one-5-ylmethyl(S)-3-hydroxy-.alpha.-methyltyrosinate (2R,3R)hydrogentartrate, and in hemihydrate form.
Dependencies are inferred from the claim text.