Cone E J, Gorodetzky C W, Yousefnejad D, Buchwald W F, Johnson R E
Drug Metab Dispos. 1984 Sep-Oct;12(5):577-81.
Buprenorphine, a powerful mixed agonist-antagonist analgesic which shows promise of providing maintenance pharmacotherapy for heroin addicts, is metabolized in male human subjects to norbuprenorphine and to conjugated buprenorphine and norbuprenorphine. Following subcutaneous, sublingual, and oral buprenorphine administration to a single subject, total metabolite excretion in urine was 2, 13.4, and 12.1%, respectively. No free parent drug was detected in urine. The amount of norbuprenorphine metabolite excreted in urine generally exceeded that of conjugated buprenorphine. In contrast, free and conjugated buprenorphine equaled or greatly exceeded total norbuprenorphine content in fecal samples following oral or sublingual administration. The greatest amount of drug and metabolite eliminated in feces occurred at 4 to 6 days following buprenorphine administration at times when there was very little urinary excretion of conjugated buprenorphine. This latter evidence indicates an enterohepatic circulation of buprenorphine in humans.
丁丙诺啡是一种强效的混合激动剂-拮抗剂镇痛药，有望为海洛因成瘾者提供维持性药物治疗。在男性人体受试者中，丁丙诺啡代谢为去甲丁丙诺啡以及结合型丁丙诺啡和去甲丁丙诺啡。对一名受试者分别进行皮下、舌下和口服丁丙诺啡给药后，尿液中总代谢物排泄量分别为2%、13.4%和12.1%。尿液中未检测到游离的母体药物。尿液中排泄的去甲丁丙诺啡代谢物量通常超过结合型丁丙诺啡。相比之下，口服或舌下给药后，粪便样本中游离和结合型丁丙诺啡等于或大大超过总去甲丁丙诺啡含量。丁丙诺啡给药后4至6天，粪便中消除的药物和代谢物量最大，此时结合型丁丙诺啡的尿液排泄量很少。后一项证据表明丁丙诺啡在人体内存在肠肝循环。
