Oral delivery of peptide pharmaceutical compositions

摘要

Bioavailability of peptide active agents to be administered orally is enhanced by a pharmaceutical composition providing targeted release of the peptide to the intestine by combining the composition with an absorption enhancer. Bioavailability is further significantly increased by administering the composition in an acid-resistant protective vehicle which transports components of the invention through the stomach. The composition may optionally further include a sufficient amount of a pH-lowering agent to lower local intestinal pH. All components are released together into the intestine with the peptide.

主权项

1. A single solid dosage capsule comprising:
a peptide comprising a 2,6-dimethyltyrosine (Dmt) residue or a prodrug thereof; at least one pharmaceutically acceptable pH-lowering agent having a pKa no higher than 4.2 and comprising a carboxylic acid, wherein the at least one pH-lowering agent is one of acetylsalicylic acid, ascorbic acid, citric acid, fumaric acid, glucuronic acid, glyceric acid, glycocholic acid, glyoxylic acid, isocitric acid, lactic acid, maleic acid, oxaloacetic acid, oxalosuccinic acid, pyruvic acid, succinic acid, tartaric acid, or combinations thereof, wherein the weight ratio of the at least one pH lowering agent to the peptide exceeds 40:1; and at least one absorption enhancer.