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健康志愿者口服和静脉注射纳布啡的药代动力学。

The pharmacokinetics of oral and intravenous nalbuphine in healthy volunteers.

作者信息

Aitkenhead A R, Lin E S, Achola K J

机构信息

University Department of Anaesthesia, Leicester Royal Infirmary.

出版信息

Br J Clin Pharmacol. 1988 Feb;25(2):264-8. doi: 10.1111/j.1365-2125.1988.tb03300.x.

Abstract

The pharmacokinetics of nalbuphine were studied in 10 healthy volunteers on two separate occasions following administration by either the intravenous (20 mg) or oral (60 mg) route. After administration, serum concentrations of nalbuphine were measured for 12 h using a high pressure liquid chromatography assay, and pharmacokinetic parameters were derived using a three compartment model. After i.v. administration, elimination half-life was 222 (111-460) min (mean and range) and total body clearance was 1.5 (0.8-2.3) 1 min-1.Cmax after oral administration was 21.4 (6.0-36.2) ng ml-1 and tmax was 46.6 (15.3-89.0) min. Bioavailability of the oral preparation was 11.8 (6.1-20.1)%.

摘要

在10名健康志愿者身上,分两次通过静脉注射(20毫克)或口服(60毫克)途径给药后,对纳布啡的药代动力学进行了研究。给药后,使用高压液相色谱分析法在12小时内测定纳布啡的血清浓度,并使用三室模型推导药代动力学参数。静脉注射给药后,消除半衰期为222(111 - 460)分钟(均值和范围),全身清除率为1.5(0.8 - 2.3)升/分钟。口服给药后的Cmax为21.4(6.0 - 36.2)纳克/毫升,tmax为46.6(15.3 - 89.0)分钟。口服制剂的生物利用度为11.8(6.1 - 20.1)%。

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Ceiling effect for respiratory depression by nalbuphine.纳布啡引起呼吸抑制的天花板效应。
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Evaluation of nalbuphine for abuse potential.纳布啡滥用可能性评估。
Clin Pharmacol Ther. 1972 Jan-Feb;13(1):78-90. doi: 10.1002/cpt197213178.

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