摘要
建立测定人血浆中奥沙普秦的高效液相色谱法(HPLC),研究两种奥沙普秦肠溶片的相对生物利用度。血浆样品沉淀蛋白后经C18色谱柱分离,流动相为甲醇-12.5mmol/L乙酸铵缓冲液(pH=3.0)(71∶29)。血浆中奥沙普秦在0.5070.56μg.mL-1范围内线性关系良好,日内与日间标准差小于12.33%和10.42%。20名健康志愿者采用随机交叉方式分别单次服用奥沙普秦肠溶片参比制剂或受试制剂0.4g后,AUC0→264h分别为(4 917.44±629.57)μg.h.mL-1和(4 604.30±737.83)μg.h.mL-1;Cmax分别为(52.34±7.68)μg.mL-1和(48.66±4.87)μg.mL-1;Tmax分别为(18.70±2.27)h和(19.30±1.63)h;相对生物利用度为94.0%±13.7%。该方法简单、快速、选择性好,可用于奥沙普秦的体内过程研究;两种制剂主要药动学参数差异无统计学意义,表明两种制剂为生物等效制剂。
The present research was aimed to develop a high performance liquid chromatography （HPLC） method to determine oxaprozin in plasma and to evaluate the bioavailability of two oxaprozin enteric coated tablets. A C18 column was used to separate the plasma after protein precipitation and the mobile phase was methanol-12.5mmol/L am monium acetate buffer solution （pH=3.0）（71：29）. The calibration curve was linear in the concentration range of 0.50-70.56μg·ml^-1, and the intra and inter-day RSDs were less than 12.33% and 10.42% respectively. A single dose of 0.4 g reference preparation or test preparation of oxaprozin enterie coated tablets was administered to 20 healthy volunteers according to a randomized crossover study. AUC0-264h were （4 917.44±629.57） μg·h·ml^-1 and （4 604.30±737.83） μg·h·ml^-1, respectively; C were （52.34±7.68）μg·ml^-1 and （48.66±4.87） μg·ml^-1 , respectively; Tmax were （18.70±2.27） h and （ 19.30± 1.63） h, respectively; The relative bioavailability of test preparation was 94.0%-13.7%. The method is simple, rapid and selective for oxaprozin determination. There is no significant difference in the main pharmaeokinetie parameters between the test formulation and reference formulation and the two formulations are in bioequivalence.
出处
《生物医学工程学杂志》
EI
CAS
CSCD
北大核心
2013年第3期646-650,共5页
Journal of Biomedical Engineering
关键词
奥沙普秦
肠溶片
高效液相色谱法
生物等效性
Oxaprozin
Enteric coated tablets
High performance liquid chromatography （HPLC）
Bioequivalenee
