头孢羟氨苄分散片的制剂分析与体内评价  

Preparation analysis and pharmacokinetics of cefadroxil dispersible tablets

作　　者：刘新宇[1] 吴芳[1] 范国荣[2] 胡晋红[2] 

机构地区：[1]深圳市福田区人民医院药剂科,深圳518033 [2]第二军医大学附属长海医院药材科,上海200433

出　　处：《中国新药杂志》2001年第9期676-678,共3页Chinese Journal of New Drugs

摘　　要：目的 :建立反相高效液相色谱方法 ,测定头孢羟氨苄分散片的含量及其在健康人体内的药代动力学。方法 :选择胸苷为内标 ,色谱柱为Hypersil ODS2 (2 0 0mm× 4.0mm ,5 μm) ,头孢羟氨苄分散片含量测定与体内分析的流动相比例分别为 0 .0 1mol·L-1磷酸二氢钠 乙腈 (96∶4)和 (98.2∶1.8) ,检测波长 2 5 4nm。 8名健康志愿者单剂量口服 75 0mg头孢羟氨苄分散片后 ,体内血药浓度采用 3P87程序方法处理。 结果 :在确定的色谱分离条件下 ,头孢羟氨苄和胸苷获得了理想的分离 ,且二者峰面积比与头孢羟氨苄浓度呈良好的线性关系。主要药代动力学参数Tmax,Cmax,t1/ 2 ,MRT ,AUC0～∞ 分别为 (1.6 3± 0 .35 )h ,(2 5 .0 0± 1.86 ) μg·mL-1,(2 .0 4± 0 .18)h ,(3.2 7± 0 .30 )h ,(89.2 6± 6 .2 5 ) μg·h·mL-1。结论 :本法操作简便快速 ,定量准确可靠 ,适用于头孢羟氨苄分散片的含量测定和药代动力学研究。Objective:To determine preparation content of cefadroxil dispersible tablets and study its pharmacokinetics in healthy volunteers by a new RP HPLC method.Methods:Thymidine was selected as the internal standard.The separation was performed on Hypersil ODS 2 (200mm× 4.0 mm,5μm)column and a mobile phase consisting of acetonitrile and 0.01mol·L -1 NaH 2PO 4 with two ratios of 4∶96 and 1.8∶98.2 was suitable for the preparation analysis and pharmacokinetic study of cefadroxil dispersible tablets.The detection wavelength was 254nm.8 healthy volunteers were given orally with a single dose of 750mg cefadroxil dispersible tablets and the plasma concentrations of cefadroxil were handled with 3P87 program.Results:Cefadroxil and thymidine were isolated ideally under the optimal chromatographic conditions and a good linearity was obtained between the peak area ratio of cefadroxil and thymidine and the plasma concentrations of cefadroxil.The main pharmacokinetic parameters were T max =(1.63±0.35)h, C max =(25.00±1.86)μg·mL -1 , t 1/2 =(2.04±0.18)h, MRT =(3.27± 0.30) h, AUC 0～∞ =(89.26±6.25)μg·h·mL -1 .Conclusion:This RP HPLC method is simple, quick, accurate,reliable and suitable for preparation analysis and pharmacokinetic study of cefadroxil dispersible tablets.

关 键 词：头孢羟氨苄 分散片 制剂 药代动力学 反相高效液相色谱法 

分 类 号：R978.11[医药卫生—药品] R944.4[医药卫生—药学]