Bullingham R E, McQuay H J, Moore A, Bennett M R
Clin Pharmacol Ther. 1980 Nov;28(5):667-72. doi: 10.1038/clpt.1980.219.
Buprenorphine kinetics was determined in surgical patients using radioimmunoassay. Buprenorphine was measured in the plasma of 24 patients who had received 0.3 mg buprenorphine intraoperatively. After 3 hr 10 of these patients then received a further 0.3 mg buprenorphine intravenously for postoperative pain relief, and 11 patients were given 0.3 mg intramuscularly; again, plasma levels were measured for 3 hr. The data fitted closely to a triexponential decay curve. There was a very fast initial phase, with a half-life (t1/2) of 2 min. The terminal t1/2 was slow, approximately 3 hr. Comparison of the kinetics of the same patient, awake and anesthetized, showed that the clearance was significantly lower in the anesthetized state. A notable feature of the drug given intramuscularly is rapid systemic availability, so that peaks are obtained in 2 to 5 min, and in 10 min the resulting levels are the same as for the intravenous and intramuscular routes.
采用放射免疫分析法测定了外科手术患者中丁丙诺啡的动力学。对24例术中接受0.3mg丁丙诺啡的患者血浆中的丁丙诺啡进行了测定。3小时后，其中10例患者为缓解术后疼痛又静脉注射了0.3mg丁丙诺啡，11例患者接受了0.3mg肌肉注射；同样，测量血浆水平3小时。数据与三指数衰减曲线拟合得非常紧密。有一个非常快速的初始阶段，半衰期（t1/2）为2分钟。终末t1/2较慢，约为3小时。对同一患者清醒和麻醉状态下的动力学进行比较，结果显示麻醉状态下的清除率显著降低。肌肉注射该药的一个显著特点是全身快速起效，因此在2至5分钟内达到峰值，10分钟时达到的水平与静脉注射和肌肉注射途径相同。
