Gastroretentive dosage forms for doxycycline

摘要

The present disclosure relates to dosage forms, e.g., swell, float and bioadhesive, and methods that enhance the absorption of doxycycline in the gastrointestinal tract. The oral dosage forms control the spatial and temporal delivery of doxycycline in the gastrointestinal tract. This controlled spatial and temporal delivery provides a site and rate of release, respectively, of the doxycycline into the gastrointestinal tract that enhances the amount of the doxycycline absorbed into the bloodstream.

主权项

1. A method for increasing the bioavailability of orally administered doxycycline, the method comprising:
controlling the spatial and temporal delivery of the doxycycline administered in an oral dosage form into a gastrointestinal area of a patient in need thereof, wherein the gastrointestinal area is selected from the group consisting of the stomach, duodenum of the small intestine, and a combination thereof; wherein the oral dosage form has a modified release profile and a swellable physicochemical profile or property and comprises: a first layer and a second layer, wherein the first layer comprises one or more swellable excipients selected from the group consisting of a cellulose polymer, a polycarbonate polymer, polyvinyl acetate, agar, carbomer, polycarbophil, polyethylene oxide, chitosan, and alginate; and a second layer comprising doxycycline; wherein the oral dosage form regulates the site, commencement time, duration and rate of release of doxycycline into the gastrointestinal area of the patient, and the oral dosage form exhibits tmax and Cmax in the patient at sufficient levels so that gastrointestinal side effects are minimized or eliminated; wherein the controlled temporal release in the gastrointestinal area of the patient is completed in about 2.5 hours to about 7.0 hours after administration to the patient; and wherein the increased bioavailability is 90% or greater relative to an immediate release doxycycline profile.