中国药学杂志
    
           首页  |  期刊介绍  |  编 委 会  |  投稿指南  |  期刊订阅  |  广告服务  |  会议信息  |  联系我们  | 
�й�ҩѧ��־ 2011, Vol. 46 Issue (20) :1597-1600    DOI:
���� ����Ŀ¼ | ����Ŀ¼ | ������� | �߼����� << | >>
�ɲ���ע��Һ�ڽ����������е�ҩ������ѧ�о�
�����1��2���ſ�1��������1�����ٻ�1*������÷1������1���ņ���1
1.���ϴ�ѧ���Ŷ�ҽԺ�ٴ�ҩѧ�����ң���ɳ 410011��2.����ʡ����ҽԺ���ϲ� 330006
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

Download: PDF (626KB)   HTML (0KB)   Export: BibTeX or EndNote (RIS)      Supporting Info
ժҪ Ŀ�� �о�����ע�������ɲ��Ⱥ��ҩ������ѧ��Ϊ��ҩ�ٴ��о���������ҩ�ṩ���ݡ����� 16�����������ߣ���Ů���룬��Ϊ���飬�������������������ƣ�����ֱ𵥼���ע��10��20 mg�������ɲ���ע��Һ���ֱ��ڸ�ҩǰ����ҩ��0��5��10��15��30��45 min��1��1.5��2��4��6��8��12 h�ֱ�ɼ�����Ѫ4 mL������LC-MS/MS���ⶨѪ����Ʒ���ɲ��ȵ�ѪҩŨ�ȣ���������Ҫ��ҩ��ѧ��������� ������ע��10��20 mg�������ɲ���ע��Һ��AUC0-12�ֱ�Ϊ��213.4��195.7���ͣ�325.7��26.8�� ng��h��mL-1��AUC0-���ֱ�Ϊ��218.1��200.7���ͣ�332.0��25.8�� ng��h��mL-1��t1/2�ֱ�Ϊ��2.2��0.4���ͣ�2.2��0.2�� h��V�ֱ�Ϊ��202.9��114.2���ͣ�194.1��24.3�� L��CL�ֱ�Ϊ��63.7��25.4���ͣ�60.6��4.5�� L��h-1��MRT0��12�ֱ�Ϊ��3.4��0.6���ͣ�3.1��0.6��h������ ���ּ���������ʡ���������ʱ���ҩ��������˥����������ҩ�����޹أ������������ҩ��ѧ�����������������У����������������ߵ�ҩ��ѧ����AUC0-12��AUC0-�����Ա�֮����ͳ��ѧ���졣
Service
�ѱ����Ƽ�������
�����ҵ����
�������ù�����
Email Alert
RSS
�����������
�����1
2
�ſ�1
������1
���ٻ�1*
����÷1
����1
�����1
2
�ſ�1
������1
���ٻ�1*
����÷1
����1
�ؼ����� �ɲ���   ҩ������ѧ   Һ��ɫ��-�������׷�     
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.
Keywords�� nalbuphine,   pharmacokinetics,   LC-MS/MS     
�ո�����: 2011-11-11;
���ñ���:   
�����1, 2, �ſ�1�� .�ɲ���ע��Һ�ڽ����������е�ҩ������ѧ�о�[J]  �й�ҩѧ��־, 2011,V46(20): 1597-1600
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
��
[1] SCHMIDT W K�� TAM S W��SHOTZBERGER G S��et al. Nalbuphine [J]. Drug Alcohol Depend�� 1985�� 14(3-4)��339-362. [2] DE SOUZA E B�� SCHMIDT W K�� KUHAR M J. Nalbuphine��an autoradiographic opioid receptor binding profile in the central nervous system of an agonist/antagonist analgesic [J]. J Pharmacol Exp Ther�� 1988�� 244(1)��391-402. [3] ERRICK J K�� HEEL R C. Nalbuphine. A preliminary review of its pharmacological properties and therapeutic efficacy [J]. Drugs�� 1983�� 26(3)��191-211. [4] LAKE C L�� DUCKWORTH E N��DIFAZIO C A�� et al. Cardiovascular effects of nalbuphine in patients with coronary or valvular heart disease [J]. Anesthesiology�� 1982�� 57(6)��498-503. [5] PCHELINTSEV M V��GORBACHEVA E N��ZVARTAU E E. Simple methodology of assessment of analgesics�� addictive potential in mice [J]. Pharmacol Biochem Behav�� 1991�� 39(4)��873-876. [6] WOOLLARD M�� JONES T�� PITT K�� et al. Hitting them where it hurts? Low dose nalbuphine therapy [J]. Emerg Med J�� 2002�� 19(6)��565-570. [7] AITKENHEAD A R��LIN E S�� ACHOLA K J. The pharmacokinetics of oral and intravenous nalbuphine in healthy volunteers [J]. Br J Clin Pharmacol�� 1988�� 25(2)��264-268. [8] LO M W�� LEE F H�� SCHARY W L�� et al. The pharmacokinetics of intravenous�� intramuscular�� and subcutaneous nalbuphine in healthy subjects [J]. Eur J Clin Pharmacol�� 1987�� 33(3)��297-301. [9] LAKE C L�� DIFAZIO C A�� DUCKWORTH E N�� et al. High-performance liquid chromatographic analysis of plasma levels of nalbuphine in cardiac surgicalpatients [J]. J Chromatography�� 1982�� 233(10)��410-416.
[1] ������ л�� ����� ����� ţ��ӱ.���������ڼ���CCl4�����˴����������������ڵ�ҩ������ѧ�Ƚ��о�[J]. �й�ҩѧ��־, 2012,47(7): 534-538
[2] ʩ���� ���� ���ļ� ��ȫӢ .����������͡��Ĥ��Ƭ�������Ч���о�[J]. �й�ҩѧ��־, 2012,47(5): 367-370
[3] ���ж� ����Ƽ ʩТ�� ������ ���� ���� ������.�������Կڷ�����������͸�ҩ��������̬���ҩ��ѧ�������Ч������[J]. �й�ҩѧ��־, 2011,46(24): 1923-1928
[4] ��� ��� ������ ��ܿ .CYP3A5�����̬�Զ��ٴ�ҩ������ѧӰ����о���չ[J]. �й�ҩѧ��־, 2011,46(20): 1541-1545
[5] ������ �־�Ө ½���� ½�� ��ά�� ��ˮ�� ���һ ���.LC-MS/MSͬʱ�ⶨ��Ѫ����5�ֿ�������ҩ���9�ֿ�����ҩ���Ũ��[J]. �й�ҩѧ��־, 2011,46(1): 57-60
[6] ������ �Ϸ��� ���̷� ˾���� ����ޱ ������.����޽���ڴ������ڵ�ҩ��ѧ�о�[J]. �й�ҩѧ��־, 2010,45(7): 539-542
[7] ¥���� ���� �����.HPLC-MS�ⶨ��Ѫ���а�������Ũ�ȼ�ҩ��ѧ[J]. �й�ҩѧ��־, 2010,45(4): 292-294
[8] ����Т.�ҹ�ҩ������ѧ�о���չ�Ļع�[J]. �й�ҩѧ��־, 2010,45(2): 81-89
[9] �Ŵ��� �챦Ӣ ������ ������ ���� ������.��ЧҺ��ɫ��-�������׷��ⶨ��Ѫ�����ȷ�������Ũ��[J]. �й�ҩѧ��־, 2010,45(19): 1492-1495
[10] �ַƷ� ��Ц�� ������ �Ӵ�� .Һ��ɫ��-�������׷��ⶨ��Ѫ���л�����ù��[J]. �й�ҩѧ��־, 2010,45(13): 1020-1023
[11] ���� ��̫�� ���� ���� ����÷ ������.HPLC-MS/MS�ⶨ��������չ���ѪҩŨ��[J]. �й�ҩѧ��־, 2010,45(10): 772-774
[12] ����� �Ὺ�� ��Ц�� ���ݷ� �Ӵ�� ���ϴ�.����ǰ�д�Ƭ��ͬ��ҩ;��������ҩ��ѧ�о�[J]. �й�ҩѧ��־, 2010,45(1): 52-55
[13] ë��� ۣ��ΰ ���� ���� ����.Һ��ɫ��-�������׷�ͬʱ�ⶨ��ҩ����74��ũҩ������[J]. �й�ҩѧ��־, 2010,45(1): 64-70
[14] ���ķ�;����;���E;����;����.HPLC-MS/MS�ⶨ��Ѫ���ж��ݻ�ͪŨ�ȼ�����ҩ��ѧ[J]. �й�ҩѧ��־, 2009,44(07): 528-531
[15] ��ӱ��;������;���;����;������.Һ��ɫ��-�����������òⶨ��Ѫ����α��ƼO-ȥ�׻�����ɳ�Һͱ���������Ũ��[J]. �й�ҩѧ��־, 2009,44(06): 464-467
Copyright 2010 by �й�ҩѧ��־