HPLC测定健康人体内头孢泊肟含量及其药动学  

Studies on determination of cefpodoxime in plasma by HPLC and its pharm acokinetics in human

作　　者：刘蕾[1] 彭雯[2] 赫广威[1] 殷琦[1] 孙春华[1] 

机构地区：[1]卫生部北京医院临床药理基地,北京100730 [2]北京大学药学院,药学97级实习生北京100083

出　　处：《中国药学杂志》2003年第2期123-127,共5页Chinese Pharmaceutical Journal

摘　　要：目的　建立HPLC UV检测方法测定健康人体内头孢泊肟含量的方法 ,并用该法研究头孢泊肟在健康人体内的药动学。方法　色谱柱为KromasilC1 8(1 50mm× 4 .6mm ,5μm) ,流动相为水 乙腈 三乙胺 (1 0 0 0∶1 36∶5) (以磷酸调节 pH =4.6) ,检测波长 2 54nm。以头孢克罗为内标 ,血样以固相萃取法进行预处理 ,尿样稀释 1 0倍后直接进样。结果　血浆样品线性范围 0 .0 50～ 6 .40 0mg·L- 1 (r =0 .9997) ,尿样线性范围 0 .2～ 2 5 .6mg·L- 1 (r =0 .9999) ,血浆样品萃取回收率均在 79%以上 ,日内、日间的RSD皆小于 1 2 %。应用该法研究 2 0名健康受试者 po 2 0 0mg头孢泊肟酯片剂后的药动学 ,其体内过程符合一室模型 ,其药动学参数为 :tmax为 (3 .0± 0 .4)h ,cmax为 (3 .4± 0 .4)mg·L- 1 ,用梯形法计算所得的AUC0～t为 (1 7.7± 2 .1 )mg·h·L- 1 ,V为 (37± 6)L ,1 2h尿药排泄率为 (47.8± 2 .9) %。结论　此方法准确 ,灵敏 ,适于药物分析 ,其药动学参数 。OBJECTIVE A HPLC UV method was established for th e determination of cefpodoxime in plasma and was applied to the pharmacokinetic study of cefpodoxime in 20 volunteers.METHODS The chromato graphic separation was achieved on a Kromasil C 18 (150 mm×4.6 mm,5 μm), the mobile phase was consisted of water acetonitrile triethylamine(1000∶136∶ 5)(adjusted to pH=4.6 with phosphoric acid),The detection wavelength was at 2 54 nm.The internal standard was cefaclor,The plasma samples were extracted with solid phase extraction and the urine sample were dilute 10 times.RES ULTS A good linearity was obtained from 0.050 to 6.400 mg·L -1 in plasma with a correlation coefficient of 0.999 7 and from 0.2 to 25.6 mg·L -1 in urine with a correlation coefficient of 0.999 9,respectively.The recover y of plasma extraction was more than 79%.The within day and between day RSD we re less than 12.0% .The pharamacokinetic analysis of cefpodoxime after oral a dministration of 200 mg cefpodoxime proxetil tablets was studied.It was found to be fitted to a one compartment open model and its pharmacokinetic parameters w ere as follow: t max (3.0±0.4) h, c max (3.4±0.4) mg·L -1 ,AUC 0～t (17.7±2.1) mg·h·L -1 and V (37±6) L,respectively. The accumulation elimination rates of cefpoxime in urine were(47.8±2.9)% after 12 h.CONCLUSION The pharmacokinetics of cefpoxime in human p rovided a useful index for clinical trial.

关 键 词：HPLC 头孢泊肟 药动学 高效液相色谱法 

分 类 号：R978.11[医药卫生—药品] R969.1[医药卫生—药学]