Extended-release oral dosage forms for poorly soluble amine drugs

摘要

Oral dosage forms for poorly soluble amine drugs are provided. Such dosage forms include an ionizable compound such as an organic acid, an amphiphilic polymer and a release rate-controlling membrane. Such dosage forms allow for the consistent release of the active agent in both gastric pH conditions and in the intestine. Methods of making such dosage forms are also provided.

主权项

1. An extended-release oral dosage form for poorly soluble amine compounds comprising,
(a) a core having an ionizable compound, wherein the ionizable compound is an organic acid, wherein the organic acid is selected from the group consisting of citric acid, maleic acid and combinations thereof; (b) a barrier layer coating the core; (c) a mantle of a matrix having a poorly soluble amine compound and at least one amphiphilic polymer, wherein the amphiphilic polymer is selected from the group consisting of polyethylene glycol 6000/vinylcaprolactam/vinyl acetate 13/57/30, d-α-tocopheryl polyethyleneglycol 1000 succinate (Vitamin E-TPGS), and combinations thereof; and (d) a release-rate controlling layer coating the mantle; wherein the ionizable compound and the amphiphilic polymer are in amounts sufficient to provide synergistic solubility effect.