Oral peptide pharmaceutical products
AssigneeUnigene Laboratories Inc.
InventorsWilliam Stern, James P. Gilligan
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Abstract
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 virtue of an acid-resistant protective vehicle which transports components of the invention through the stomach. The composition includes an absorption enhancer and a sufficient amount of a pH-lowering agent to lower local intestinal pH. All components are released together into the intestine with the peptide.
Claims55
A pharmaceutical composition for oral delivery of a physiologically active peptide agent comprising:
- (A) a therapeutically effective amount of said active peptide;
- (B) at least one pharmaceutically acceptable pH-lowering agent;
- (C) at least one absorption enhancer effective to promote bioavailability of said active agent;
- and
- (D) an acid resistant protective vehicle effective to transport said pharmaceutical composition through the stomach of a patient while preventing contact between said active peptide agent and stomach proteases;
- wherein said pH-lowering agent is present in said pharmaceutical composition in a quantity which, if said composition were added to ten milliliters of 0.1M aqueous sodium bicarbonate solution, would be sufficient to lower the pH of said solution to no higher than 5.5.
A method for enhancing the bioavailability of a therapeutic peptide active agent delivered orally, said method comprising selectively releasing said peptide active agent, together with at least one pH-lowering agent and at least one absorption enhancer, into a patient's intestine following passage of said peptide active agent, pH-lowering agent and absorption enhancer through said patient's mouth and stomach under protection of an acid resistant protective vehicle which substantially prevents contact between stomach proteases and said peptide agent;
- wherein said pH-lowering agent and other compounds released therewith are released into said intestine in a quantity which, if added to 10 milliliters of 0.1M aqueous sodium bicarbonate solution, would be sufficient to lower pH of said solution to no higher than 5.5.
Dependencies are inferred from the claim text.