Formulations have been developed to improve the solubility of corticosteroids such as fluticasone proprionate in a composition designed to achieve localized release of the drug in the small intestine and/or colon. In one embodiment, solid dispersions of fluticasone are prepared wherein the drug is blended with or coated onto a highly water soluble substrate such as nonpareil (sugar beads) then coated with a layer of polymer soluble in small intestinal fluid, then coated with an enteric coating. The inner polymer layer controls release of the drug, and the enteric coating, a pH sensitive polymer that is broken down in the ileum and colon, controls localized release of drug at various sites within the gastrointestinal tract. The multilayer pharmaceutical composition can be in the form of pellets, tablets compressed from pellets or pellets packed into capsules. The release profile of the drug can be manipulated by (1) altering size or shape (i.e., surface area) and solubility of the inert substrate; (2) the ratio of drug to polymer, the polymer composition and solubility, the porosity of the polymer; (3) the drug form (i.e., free base or salt, or which salt); and the thickness and/or surface area of the drug/polymer and/or enteric coating. In a preferred embodiment, the composition is administered orally. This may also be packaged to provide for an escalating or tapering dosage.

 
Web www.patentalert.com

< NOVEL CONTROLLED RELEASE FORMULATIONS OF DIVALPROEX SODIUM

> Film Embedded Packaging and Method of Making Same

~ 00423