pH dependent carriers for targeted release of pharmaceuticals along the gastrointestinal tract, compositions therefrom, and making and using same

摘要

Novel drug carriers capable of targeted and/or pH dependent release of biologically active agents into selected pH environments including the gastrointestinal (GI), ophthalmic, urinary, or reproductive tracts. Unexpectedly, carriers including free fatty acids (FFA) are able to deliver biologically active agents to various pH environments. Such targeted delivery is tailorable and useful for active agents that are: (a) injurious to the upper GI tract (esophagus, stomach, and duodenum), (b) acid labile, (c) impermeable/insoluble compounds in GI fluids, (d) susceptible to first pass metabolism, and/or (e) cause stomach irritation, upset, or dyspepsia.

主权项

1. A method of targeting release of a non-steroidal anti-inflammatory drug (NSAID) to the small intestine of a subject, comprising:
orally administering to the subject an ingestible composition consisting of a non-aqueous solid-in-oil suspension of an effective amount of the solid NSAID in a carrier, wherein the carrier comprises at least one free fatty acid having at least 8 carbon atoms in an amount greater than about 10 wt. %, and wherein the carrier comprises from about 0.0001 wt. % to about 5 wt. % of zwitterionic phospholipids, whereby the composition displays less gastrointestinal toxicity than the NSAID alone.