Transdermal Buprenorphine for Opiate Antagonist Therapy

描述（由申请人提供）：阿片拮抗剂治疗是近期戒断阿片成瘾者的重要治疗方法。丁丙诺啡是一种混合激动剂-拮抗剂，通过阻断主观阿片奖励来消除生理强化。丁丙诺啡最近作为舌下片剂上市，非常有效，比美沙酮或纳曲酮更受受试者青睐。BIOTEK提出通过开发一种3天的透皮给药系统来改善丁丙诺啡的治疗。这样的贴片将提供稳定的维持激动剂治疗，以促进依从性。如果这种贴片含有相对较少的丁丙诺啡，那么颠覆和滥用的动机将是最小的。在I期获得的人体皮肤的体外实验结果有力地支持了这种贴片的可行性，而兔子的刺激研究表明它将是无刺激性的。阶段

DESCRIPTION (provided by applicant): Opiate antagonist therapy is an important treatment for recently withdrawn opiate addicts. Buprenorphine is a mixed agonist-antagonist which eliminates physiological reinforcement by blocking subjective opiate reward. Recently marketed as sublingual tablets, buprenorphine is very effective and is preferred by subjects to methadone or naltrexone. BIOTEK proposes to improve buprenorphine therapy by developing a 3-day transdermal delivery system. Such a patch would provide steady maintenance of agonist therapy to foster compliance. If such a patch can be made to contain relatively little buprenorphine, the motivation for subversion and abuse will be minimal. In vitro results on human skin obtained during Phase I strongly support the feasibility of such a patch, and rabbit irritation studies suggest that it will be non-irritating. Phase II will establish patch specifications suitable for GMP manufacture, confirm the in vitro performance of the selected formulation, prepare and characterize GMP clinical samples, initiate stability studies, submit an IND, and conduct an initial human study of safety and pharmacokinetics.