Bioavailability of sublingual buprenorphine
Bioavailability of sublingual buprenorphine
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DOI：
10.1177/009127009703700106
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发表时间：
1997-01-01
影响因子：
2.9
通讯作者：
Jones, RT
中科院分区：
文献类型：
--
作者：
Mendelson, J;Upton, RA;Jones, RT
丁丙诺啡舌下注射是一种很有前途的阿片依赖治疗方法。利用一种新的、灵敏和特异的气相色谱电子捕获技术，通过比较舌下含药2毫克和静脉注射丁丙诺啡1毫克的6名健康志愿者3分钟和5分钟的血药浓度。在22名受试者舌下含2毫克丁丙诺啡2分钟、4分钟和10分钟后，测量唾液中未吸收丁丙诺啡的量。药动学参数经方差分析，生物等效性评价采用Schuirmann双侧检验。3分钟和5分钟的舌下暴露各允许29+/-10%的生物利用度(未外推的血药浓度-时间曲线下面积)，并且具有生物等效性。丁丙诺啡在2分钟、4分钟和IO分钟暴露后从唾液中恢复的平均剂量是剂量的52%到55%。唾液pH值升高与唾液回收率降低相关。研究结果表明，丁丙诺啡舌下含药的生物利用度约为30%。舌下接触的时间在3到5分钟之间会产生相同的结果。丁丙诺啡残留在唾液中会导致对生物利用度的几乎两倍高估。
Buprenorphine administered sublingually is a promising treatment for opiate dependence. Utilizing a new, sensitive, and specific gas chromatographic electron-capture in six healthy volunteers by comparing plasma concentrations after 3- and 5-minute exposures to 2 mg sublingual and I mg intravenous buprenorphine. The amount of unabsorbed buprenorphine in saliva was measured after 2-, 4-, and 10-minute exposures to 2 mg sublingual buprenorphine in 22 participants. Pharmacokinetic parameters were analyzed by analysis of variance; bioequivalence was evaluated by the Schuirmann two-sided test. The 3- and 5- minute sublingual exposures each allowed 29 +/- 10% bioavailability (area under the plasma concentration-time curve unextrapolated) and were bioequivalent. Buprenorphine recovered from saliva after 2-, 4-, and IO-minute exposures was, on average, 52% to 55% of dose. Increased saliva pH was correlated with decreased recovery from saliva. Study results indicate that bioavailability of sublingual buprenorphine is approximately 30%. Sublingual exposure times between 3 and 5 minutes produce equivalent results. Buprenorphine remaining in saliva causes an almost twofold overestimation of bioavailability.