Transdermal Buprenorphine for Opiate Antagonist Therapy

描述（由申请人提供）：阿片拮抗剂治疗是最近戒断的麻醉成瘾者的重要治疗方法。丁丙诺啡是一种具有激动剂和拮抗剂混合特性的药物，它通过阻止吗啡类药物的任何主观奖励来消除生理强化。丁丙诺啡非常有效，比美沙酮或纳曲酮更可取。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。丁丙诺啡贴片可以避免频繁的临床访问带来的不便，丁丙诺啡激动剂作用的稳定维持应该通过提供更多的正强化来激励依从性。BIOTEK之前已经证明了丁丙诺啡的高透皮递送率。最近一项使用BIOTEK的可注射丁丙诺啡微胶囊的人类受试者的研究结果表明，有效的阿片类药物阻断可以通过比以前认为的必要剂量低得多的丁丙诺啡剂量率来维持。该计划的目的是开发一种有效的拮抗剂贴剂，其中含有太少的丁丙诺啡，使其成为颠覆或滥用的有吸引力的目标。

DESCRIPTION (provided by applicant): Opiate antagonist therapy is an important treatment for recently withdrawn narcotic addicts. Buprenorphine is a drug with mixed agonist-antagonist properties, which eliminates physiological reinforcement by preventing any subjective reward from morphine-like drugs. Buprenorphine is very effective and is preferred by subjects to either methadone or naltrexone. BIOTEK proposes to improve buprenorphine therapy by developing a 3-day transdermal delivery system. A buprenorphine patch would avoid the inconvenience of frequent clinical visits, and steady maintenance of the agonist action of buprenorphine should motivate compliance by providing more positive reinforcement. BIOTEK has previously demonstrated high transdermal delivery rates for buprenorphine. Recent results from a study of human subjects using BIOTEK's injectable buprenorphine microcapsules suggest that effective opiate blockade can be maintained by a much lower buprenorphine dose rate than previously thought necessary. It is the purpose of the proposed program to develop an effective antagonist patch containing too little buprenorphine to be an attractive target for subversion or abuse.