CAI Li-jing1��2��ZHANG Jun1��2��PENG Wen-xing1�� ZHU Rong-hua1*��WANG Xiu-mei1��YANG Jian1��ZHANG Qi-zhi1
1. Clinical Pharmaceutical Research Institute�� the Second Xiangya Hospital�� Central South University�� Changsha 410011�� China�� 2. Jiangxi Provincial People��s Hospital�� Nanchang 330006�� China
Abstract��
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 ��max�� 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 ��max men women after dose and body weightnormaliz.
CAI Li-jing,
ZHANG Jun,
PENG Wen-xing etc
.Pharmacokinetics of Intravenous Nalbuphine in Healthy Volunteers[J] Chinese Pharmaceutical Journal, 2011,V46(20): 1597-1600
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2011, Vol. 46 
