高效液相色谱法测定人血浆中的头孢克洛及在制剂生物等效性研究中的应用  

Determination of cefaclor in human plasma with HPLC: for the pharmacokinetics and bioequivalence study

作　　者：王晓波[1] 刘丹[1] 姚文[1] 宋晓楠[1] 隋淼[1] 

机构地区：[1]解放军第210医院临床药理基地,辽宁大连116021

出　　处：《中国医院药学杂志》2009年第20期1727-1730,共4页Chinese Journal of Hospital Pharmacy

摘　　要：目的:建立HPLC法测定血浆中的头孢克洛并用于其制剂的生物等效性研究。方法:色谱柱为迪马C18柱(150mm×4.6mm,5μm),流动相为乙腈-0.05mol.L-1磷酸盐缓冲液(pH4.5)(7∶93),流速为1.5mL.min-1,检测波长254nm,柱温为室温。用自身交叉2周期设计,18名健康男性志愿者单次口服头孢克洛片受试制剂和参比制剂,用HPLC法测定血浆中头孢克洛浓度,用DAS2.0软件包计算头孢克洛片受试制剂和参比制剂的药动学参数并进行生物等效性评价。结果:头孢克洛片受试制剂和参比制剂在人体内药动学行为相似,两者的Cmax分别为(8.5±0.8),(8.2±0.9)mg.L-1;tmax分别为(0.80±0.10),(0.80±0.20)h;t1/2分别为(1.10±0.20),(1.0±0.4)h;AUC0-t分别为(12.6±1.6),(12.6±2.2)mg.h.L-1;AUC0-∞分别为(13.1±1.6),(13.2±2.5)mg.h.L-1,头孢克洛片的相对生物利用度为(100.7±8.1)%。结论:头孢克洛片受试制剂和参比制剂为生物等效制剂。OBJECtIVE To develop an HPLC method for determination of the concentration of cefaclor in human plasma. and study the bioequivalence of two eefaelor tablets. METHODS Chromatographic separation was performed in Diamonsil C18 column at room temperature with the mobile phase consisting of acetonitrile-0. 05 mol·L^-1 phosphate buffer （pH 4. 5） （7：93）. The flow rate was 1.5 mL·min ^-1 . and the detection wavelength was 254 nm. A single oral dose 500 mg cefaclor of test or reference formulation was given to each volunteer according to an open randomized crossover design. The cefaclor concentrations in plasma were determined by HPLC with UV detection method. The pharmacokinetic parameters were determined by DAS 2.0 program and bioequivalence were evaluated. RESULTS The main pharmacokinetics parameters of eefaclor were as the follows： Cmax were （8.5 ± 0. 8） and （8.2 ± 0. 9） mg·L ^-1 . tmax were （0. 80 ± 0. 10） and （0. 80 ± 0. 20）h;t1/ 2 were （ 1.10 ± 0. 20） and （ 1.0± 0. 4） h, AUC0-t, were （ 12.6 ± 1.6） and （ 12.6 ± 2.2） mg· h· L ^-1 . AUG0 -∞ were （ 13.1 ＋ 1.6） and （ 13.2 ＋ 2.5 ） mg· h·L^-1 for test and reference formulations, respectively. The relative bioavailability of test to reference drug were （ 100. 7 ± 8. 1 ） %. CONCLUSION The results of statistical analysis shows that the tow formulations are bioequivalent.

关 键 词：头孢克洛片 药动学 生物等效性 高效液相色谱法 

分 类 号：R927.2[医药卫生—药学] R969.1