Bioadhesive drug delivery system with enhanced gastric retention

摘要

Bioadhesive macrosphere delivery systems ("BDDS") having prolonged gastric retention time due to bioadhesion rather than physical density or size are described. In general, the macrospheres have diameters that are greater than 200 microns, more preferably greater than 500 microns. The bioadhesive macrospheres are released in the stomach where they reside in close proximity to the gastric mucosa for a prolonged period of time. Increased residence of BDDS in the upper GI can lead to increased systemic absorption of drug in the preferred site of systemic absorption, namely the upper GI tract (upper to mid-jejunum). The BDDS may be engineered either as a capsule with drug delivery controlled by a diffusion-limited membrane or degradable shell, or as a solid matrix system with drug delivery controlled by a combination of diffusion and polymer degradation kinetics.