Transmucosal drug delivery system

摘要

Disclosed are preparations and formulations of high thermodynamic activity lipophilic associations (LA), in which there is pairing between an ionizable pharmaceutical agent and a lipophilic species having ionic characteristics opposite to that of the pharmaceutical agent. Such lipophilic associations manifest high thermodynamic activity, as evidenced by their being predominantly in a liquid phase at room temperature or solvated in a lower-than-water dielectric solvent. Further the pharmaceutical agent being solubilized means that dissolution is not rate limiting to transmucosal absorption. This LA or LA-solvate is formulated into a low dielectric dosage form, from whence, upon the dosage form's hydration, the pharmaceutical agent is driven through the mucosal tissue and into systemic circulation. The invention therefore provides an enhanced transmucosal drug delivery system for ionizable pharmaceutical agents at or near physiological pH.

主权项

1. A pharmaceutical composition in a solid dosage form for buccal or sublingual delivery, comprising:
about 0.1 mg to about 5 mg nicotine; about 0.15 mg to about 10 mg of a complementary lipophilic species with which the nicotine is solvated; and up to about 30 mg of a solid adsorbent to which the solvated nicotine is adsorbed, wherein the nicotine in the solid dosage form of the composition is in solution.