摘要
目的研究市售两种头孢哌酮胶囊(代号CP05、CP06)的药代动力学参数,为上述两种制剂的临床合理用药提供参考。方法动物实验采用SD大鼠,于口服给药后0～24h内按时间点取样,经蛋白沉淀后的血浆样品进HPLC分析,采用Diamonsil C_(18)色谱柱(4.6×150mm,5μm),乙腈-0.1%磷酸二氢钠为流动相,流速1.0mL·min^(-1),柱温30℃,检测波长254nm,进样量10μL。结果口服给药市售两种头孢哌酮胶囊100mg/只后,两种制剂的t_(1/2)分别为2.99±0.16h和3.26±0.15h,MRT分别为6.51±0.71h和7.14±1.01h,AUC_(0～24)分别为191.86±18.64μg/(h·mL)和135.51±5.73μg/(h·mL),AUC_(0～∞)分别为192.96±18.73μg/(h·mL)和136.80±5.59μg/(h·mL)。结论 CS05和CS06均以原形入血,且CS05的吸收、代谢和生物利用度高于CS06,在用药时应注意适当调整药量和给药间隔。
OBJECTIVE To investigate pharmacokinetic parameters of two commercial available cefoperazone capsules for the purpose of providing reasonable guidance for the two preparations.METHODS Animal experiment used SD rats,and the plasma was taken as designed intervals within 24 hours,the protein precipitated samples were analyzed by HPLC,with a Diamonsil C18 column(4.6×150 mm,5μm),and the mobile phase containing acetonitrile-0.1%sodium dihydrogen phosphate,the flow rate was 1.0 mL·min^-1,column temperature was 30℃,detection wavelength was 254 nm and the injection volume was 10μL.RESULTS After oral administration of the two capsules at the dosage of 100 mg per rat,t1/2 were 2.99±0.16 and 3.26±0.15 h,MRT were 6.51±0.71 and 7.14±1.01 h,AUC0~24 were 191.86±18.64μg/(h·mL)and 135.51±5.73μg/(h·mL),AUC0~∞were 192.96±18.73μg/(h·mL)and 136.80±5.59μg/(h·mL),respectively.CONCLUSION Both CS05 and CS06 was taken by the blood in original form,while the former had higher absorption and bioavailability,as well as faster metabolism than that of the latter,indicating the necessity of proper adjustment in dosage and interval of it.
作者
何健进
吴星火
李植桐
HE Jian-jin;WU Xing-huo;LI Zhi-tong(Guangdong Second Provincial Hospital of T.C.M.(Guangdong Province Engineering Technology Research Institute of T.C.M.),Guangzhou 510095,China)
出处
《海峡药学》
2019年第4期18-21,共4页
Strait Pharmaceutical Journal
关键词
头孢哌酮
药代动力学
比较研究
Cefoperazone
Pharmacokinetic
Comparative research
