Pharmacokinetics of Intravenous Nalbuphine in Healthy Volunteers
CAI Li-jing1，2，ZHANG Jun1，2，PENG Wen-xing1， ZHU Rong-hua1*，WANG Xiu-mei1，YANG Jian1，ZHANG Qi-zhi1
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1. Clinical Pharmaceutical Research Institute， the Second Xiangya Hospital， Central South University， Changsha 410011， China； 2. Jiangxi Provincial People′s Hospital， Nanchang 330006， China
OBJECTIVE To assess the pharmacokinetic properties of nalbuphine after single intravenous administration in healthy Chinese volunteers.METHODS Sixteen healthy volunteers (8 males and 8 females) were enroued in this study. The 16 healthy volunteers were divided into two groups (each group consisted of 4 males and 4 females) and received intravenous administration of nalbuphine at doses of 10， 20 mg， respectively. Blood samples (4 mL) were immediately collected into heparinized tubes before injection and at 0， 5， 10， 15， 30， 45 min， 1， 1.5， 2， 4， 6， 8， 12 h after injection. The pharmacokinetic parameters including ρmax， tl/2， AUC0-t， AUC0-∞， CL， V and MRT0-t were calculated. Tolerability was assessed throughout the study.RESULTS The main pharmacokinetic parameters for nalbuphine after intravenous administration at doses of 10 and 20 mg were as follows：AUC0-12（213.4±195.7） ng·h·mL-1， （325.7±26.8） ng·h·mL-1， AUC0-∞（218.1±200.7） ng·h·mL-1， （332.0±25.8） ng·h·mL-1， t1/2（2.2±0.4） h， （2.2±0.2） h， V （202.9±114.2） L， （194.1±24.3） L; CL（63.7±25.4） L·h-1 and （60.6±4.5） L·h-1，MRT0～12（3.4±0.6） h and （3.1±0.6） h. AUC0-12 and AUC0-∞ increased proportionally with the dose levels.CONCLUSION The t1/2， MRT， V and CL were very similar between 10 and 20 mg. No significant differences were observed in t1/2 values between different doses. No significant differences were found in AUC and ρmax men women after dose and body weightnormaliz.
CI Li-jing;ZHNG Jun;PENG Wen-xing;ZHU Rong-hu;WNG Xiu-mei;YNG Jin;ZHNG Qi-zhi.
Pharmacokinetics of Intravenous Nalbuphine in Healthy Volunteers[J]. Chinese Pharmaceutical Journal, 2011, 46(20): 1597-1600
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