Transdermal Buprenorphine for Opiate Antagonist Therapy

透皮丁丙诺啡用于阿片拮抗剂治疗

• 批准号: 6548271
• 负责人: LARRY D NICHOLS
• 金额: $ 9.99万
• 依托单位: BIOTEK, INC.
• 依托单位国家: 美国
• 财政年份: 2002
• 资助国家: 美国
• 起止时间: 2002-08-01 至 2004-01-31
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/6548271
• 关键词: buprenorphine; drug administration rate /duration; drug design /synthesis /production; human tissue; laboratory rabbit; narcotic antagonists; opiate alkaloid; pharmacokinetics; reinforcer; skin irritation /irritant; transdermal drug delivery

DESCRIPTION (provided by applicant): Opiate antagonist therapy is an important treatment for recently withdrawn narcotic addicts.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

描述（由申请人提供）：阿片拮抗剂疗法是最近戒毒的重要治疗方法。丁丙诺啡是一种具有混合激动剂-拮抗剂特性的药物，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，并且比美沙酮或纳曲酮更受受试者青睐。 BIOTEK 提议通过开发 3 天透皮给药系统来改进丁丙诺啡治疗。丁丙诺啡贴剂可以避免频繁临床就诊的不便，稳定维持丁丙诺啡的激动作用可以通过提供更多的正强化来激发依从性。 BIOTEK 此前已证明丁丙诺啡的高透皮递送率。使用 BIOTEK 的可注射丁丙诺啡微胶囊对人类受试者进行的一项研究的最新结果表明，可以通过比以前认为必要的低得多的丁丙诺啡剂量率来维持有效的阿片类药物封锁。拟议计划的目的是开发一种有效的拮抗剂贴剂，其丁丙诺啡含量太少，无法成为颠覆或滥用的有吸引力的目标。