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�й�ҩѧ��־ 2005, Vol. 39 Issue (22) :1737-1740    DOI:
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1.�Ĵ���ѧ����ҩѧԺ �Ĵ� �ɶ� 610041;2.�Ĵ���ѧ����ҽԺ �Ĵ� �ɶ� 610041
YE Li-ming1�� MA Tao1�� CHEN Cong1�� CHEN Yu2
1.West China School of Pharmacy�� Sichuan University�� Chengdu 610041��China��2.West China Hospital�� Sichuan University�� Chengdu 610041��China

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ժҪ Ŀ�Ľ����Է������࿹��ҩ��ijЩҩ��ѧ��ҩЧѧ���ʾ���Ԥ��ͽ��������ġ���������-���Թ�ϵ��(QRAR)ģ�͡�������Brij35��Ũ��Ϊ0.02mol��L-1����Һ��ɫ�׶Լ��ַ������࿹��ҩ���з����ⶨ,����ʵ�����õĻ��������������(logk)����������������-ˮ�ķ���ϵ���Ķ���ֵ(logP)����������Ũ��(IC50)�������(CL)����˥��(t1/2)�Լ��ֲ��ݻ�(Vd)������ػع�����������������logP,CL,Vd��ģ�������Ŷ�Ϊ95%��ˮƽ����ͳ��ѧ����(P<0.05),���ģ��Ԥ����������;��t1/2,IC50�����Ŷ�Ϊ95%��ˮƽ����ͳ��ѧ����(P>0.05),���ģ��Ԥ�������ϲ����ʹ�ñ�����Լ�Brij35�Ľ���ɫ�׵õ��Ļ�����ı�����Ԥ��������࿹��ҩ��ҩ��ѧ��ҩЧѧ����,QRARģ����һ����Ч��Ԥ���»�����ҩ��ѧ��ҩЧѧ����������ģ�͡�
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Abstract�� OBJECTIVE To establish a Quantitative retention-activity relationship (QRAR) models to predict and interpret the pharmacokinetic and pharmacodynamic properties of non-steroidal anti-inflammatory drugs (NSAIDs) .METHODS Some NSAIDs were determined by reversed-phase liquid chromatography with the micellar solution of Brij 35 as mobile phase. The logk values of the compounds obtained under 0.02 mol��L-1 Brij 35 concentration were correlated with the corresponding logP values(the logarithm of octanol-water partition coefficient value) ,IC50(the concentration required to abtain 50% inhibition of cyclooxygenase-2),t1/2(half-life time),Vd(volume of distribution) and CL, (clearance) taken from literature.RESULTS There were statistically significant relationships between logP and Vd, CL,logk at 95% confidence level (P<0.05), and the models obtained had powerful predictive ability.There were not statistically significant relationships between IC50,t1/2 and logk at 95% confidence level(P> 0.05), and the obtained models had poor predictive ablitity. CONCLUSION The retention of compounds in MLC using Brij 35 as surfactant is able to describe and predict the pharmacokinetic and pharmacodynamic parameters of NSAIDs. QRAR model is a model which can estimate the pharmacokinetic and pharmacodynamic parameters of new compounds in vitro.
Keywords�� quantitative retention-activity relationships ( QRAR),   micellar liquid chromatography (MLC),   non-steroid anti-inflammatory drags (NSAIDs)      
�ո�����: 2005-03-08;
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Ҷ����, ����, �´ϵ� .����Һ��ɫ���з����忹��ҩ����������-���Թ�ϵ��Ԥ��ģ���о�[J]  �й�ҩѧ��־, 2005,V39(22): 1737-1740
YE Li-ming, MA Tao, CHEN Cong etc .Study on predictive quantitative retention-activity relationship models of non-steroidal anti-inflammatory drugs by micellar liquid chromatography [J]  Chinese Pharmaceutical Journal, 2005,V39(22): 1737-1740
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