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 containing scopolamine in a solid dosage form for buccal or sublingual delivery comprising:
scopolamine in an amount of about 0.1 mg to about 5 mg; a complementary lipophilic species in an amount of about 0.1 mg to about 10 mg; a solid adsorbent in an amount up to about 50 mg; a solid water-soluble excipient in an amount of about 25 mg to about 500 mg; a disintegrant in an amount of about 0.5 mg to about 50 mg; and a lubricant in an amount of about 0.1 mg to about 15 mg.