Transdermal Buprenorphine for Opiate Antagonist Therapy

透皮丁丙诺啡用于阿片拮抗剂治疗

• 批准号: 6917943
• 负责人: ELIE NUWAYSER
• 金额: $ 44.38万
• 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 2007-06-30
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/6917943
• 关键词: buprenorphine; chemical stability; clinical research; clinical trial phase I; drug abuse; drug abuse chemotherapy; drug administration rate /duration; drug adverse effect; drug design /synthesis /production; human subject; human therapy evaluation; human tissue; laboratory rabbit; narcotic antagonists; patient oriented research; pharmacology; psychopharmacology; residential care facility; skin irritation /irritant; transdermal drug delivery

DESCRIPTION (provided by applicant): Opiate antagonist therapy is an important treatment for recently withdrawn opiate addicts.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

描述（由申请人提供）：阿片拮抗剂治疗是近期戒断阿片类药物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。最近作为舌下片剂上市的丁丙诺啡非常有效，受试者首选美沙酮或纳洛酮。BIOTEK建议通过开发3天透皮给药系统来改善丁丙诺啡治疗。这样的贴剂将提供激动剂治疗的稳定维持以促进依从性。如果这种贴片可以制成含有相对较少的丁丙诺啡，颠覆和滥用的动机将是最小的。在第一阶段获得的人体皮肤体外结果强烈支持这种贴片的可行性，家兔刺激性研究表明，它将是无刺激性的。相 II将建立适合GMP生产的贴剂质量标准，确认所选制剂的体外性能，制备和表征GMP临床样品，启动稳定性研究，提交IND，并进行安全性和药代动力学的初步人体研究。

项目成果

Evaluation of a transdermal buprenorphine formulation in opioid detoxification.

评估透皮丁丙诺啡制剂在阿片类药物解毒中的作用。

• DOI: 10.1111/j.1360-0443.2007.01944.x
• 发表时间: 2007
• 期刊: Addiction (Abingdon, England)
• 作者: Lanier,RyanK;Umbricht,Annie;Harrison,JosephA;Nuwayser,ElieS;Bigelow,GeorgeE
• 通讯作者: Bigelow,GeorgeE