Enteric solid oral dosage form of bisphosphonate containing a chelating agent

Abstract

Oral dosage forms of a bisphosphonate comprised of a safe and effective amount of a pharmaceutical composition comprising a bisphosphonate, a chelating agent, and, means for effecting delayed release of the bisphosphonate and the chelating agent in the lower gastrointestinal tract provide delivery of the pharmaceutical composition to the lower gastrointestinal tract of the mammal subject and pharmaceutically effective absorption of the bisphosphonate with or without food or beverages. The present invention substantially alleviates the interaction between bisphosphonates and food or beverages, which interaction results in the bisphosphonate active ingredient not being available for absorption. The resulting oral dosage form may thus be taken with or without food. Further, the present invention effects delivery of the bisphosphonate and the chelating agent to the lower GI tract, substantially alleviating the upper GI irritation associated with bisphosphonate therapies. These benefits simplify previously complex treatment regimens and can lead to increased patient compliance with bisphosphonate therapies.

Description

field of invention

[0001] The present invention relates to an oral dosage form of a bisphosphonate consisting of a safe and effective amount of a pharmaceutical composition comprising a bisphosphonate, a chelating agent for administering the bisphosphonate active ingredient with food or drink, a A method for affecting the delayed release of bisphosphonates and chelating agents in the lower gastrointestinal tract, and one or more pharmaceutically acceptable excipients. The oral dosage forms of the present invention provide delivery of the pharmaceutical composition into the lower gastrointestinal tract of a mammalian subject and provide drug-effective absorption of the bisphosphonate with or without administration with food or beverage. The invention also relates to methods of treatment or prevention of disorders characterized by abnormal calcium and phosphate metabolism comprising administering an oral dosage form as described herein to a human or other mammal in need thereof....