WU Li-ping1�� WANG Shu-rong2�� CHEN Yu3�� CHEN Cong1�� WU Jia-qi1�� YE Li-ming1
1. West China School of Pharmacy�� Sichuan University�� Chengdu 610041�� China�� 2.Affiliated Hospital of Luzhou Medical College�� Luzhou 646000�� China��3. West China Hospital�� Sichuan University�� Chengdu 610041�� China
Abstract��
OBJECTIVE To develop the quantitative retention-activity relationship(QRAR) models by biopartitioning micellar chromatography(BMC) for estimating the pharmacokinetic parameters of ��-lactam antibiotics.METHODS The n-octanol-water partition coefficient was used to obtain the better qualification of BMC system,then the retention of drug was detected and calculated.The models were established by software with bioactivity parameters of ��-lactam antibiotics in literatures and retention values in BMC,and the model predictive ability was evaluated according to RMSEC,RMSECV,and RMSECVi.RESULTS The QRAR models of AUC,t1/2��,t1/2��,and F% obtained in physiological conditions were statistically significant,while ��max and Lag-T models showed no significance.CONCLUSION The results indicate that,using only one descriptor(the retention factor,K) to explain the bioactivity of ��-lactam antibiotics is feasible,in vitro approach is an advanced tool for pharmacokinetic research of the drugs.
2008, Vol. 43 
