关键词: 头孢丙烯, 药代动力学, 生物等效性, HPLC, 颗粒剂

Abstract: AIM: Use the HPLC-UV method to determine the contents of cis-cefprozil and trans-cefprozil in human plasma in orderto evaluate the pharmacokinetics and bioequivalence of cefprozil granules (testing granules and reference tablets) in healthy volunteers.METHODS: 20 healthy volunteers were classified into two groups forsingle dose and two-crossing test,with the dose of 500 mg,10 volunteers each grouPand seven days interval between two tests.Afterthe plasma protein was precipitated by 20 % trichloroacetic acid,endogenesis impurities in plasma was extracted with the mixtuerof acetonitrile and dichloromethane,then the supernatant was analyzed by HPLC.LichrospherC8 column(5μm,4.6 mm×30 cm)was applied,using acetonitrile-1.5 % acetic acid watersolution (15∶85,v/v)as mobile phase with the flow rate of 1.0 ml·min^-1.The detection wavelength was 280 nm and column temperature was 30 ℃,the internal standard was cefradine.RESULTS: Endogenous materies didn' t disturb the determination of cefprozil.Within the range of 0.0209-10.47μg·ml^-1,peak area and injection quantity were in linearcorrelation (r=0.9993).The limit of quantification was 0.0209 mg·L^-1.The main pharmacokinetic parameters Tmax,Cmax and t_1/2 were 1.7±0.3 h,4.45±1.25 mg·L^-1,1.89±0.45 h forthe reference tablets;1.8±0.2 h,4.88±1.08 mg·L-11.79±0.39 h forthe test granules respectively.AUC_0-12were 12.11±2.62,12.34±2.93 mg·L^-1·h^-1 and the relative bioavailability was (101.9±8.8)%.CONCLUSION: The method is simple,accurate and reliable.There is no significant difference between the two formulations in the C_max,and AUC_0-12.The two formulations are bioequivalence.

Key words: cefprozil, pharmacokinetics, bioequivalence, HPLC, granules