Transdermal Buprenorphine for Opiate Antagonist Therapy

描述(申请人提供)：阿片拮抗剂疗法是最近戒断的毒品成瘾者的重要治疗方法。丁丙诺啡是一种具有混合激动剂和拮抗剂性质的药物，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，美沙酮或纳曲酮的受试者更喜欢丁丙诺啡。Biotek建议通过开发3天经皮给药系统来改进丁丙诺啡的治疗。丁丙诺啡贴片可以避免频繁的临床就诊带来的不便，稳定地维持丁丙诺啡的兴奋作用应该会通过提供更积极的强化来促进依从性。Biotek之前已经证明丁丙诺啡的透皮释放率很高。最近对使用Biotek公司的丁丙诺啡注射微囊的受试者进行的一项研究结果表明，有效的阿片类药物阻断可以通过比之前认为必要的低得多的丁丙诺啡剂量率来维持。拟议计划的目的是开发一种含有太少丁丙诺啡的有效拮抗剂贴片，不能成为有吸引力的颠覆或滥用目标。

DESCRIPTION (provided by applicant): Opiate antagonist therapy is an important treatment for recently withdrawn narcotic addicts.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.