高效液相色谱荧光法测定人血浆中唑吡坦浓度及生物等效性研究

目的：建立高效液相色谱荧光法（HPLC—FLU）测定人血浆中唑吡坦的血药浓度并对其口服制剂人体生物等效性进行研究，为临床用药提供参考依据。方法：采用随机自身对照双周期交叉实验设计，18名健康受试者口服受试制剂和参比制剂10mg，用HPLC—FLU法测定人血浆中的唑吡坦浓度，用非房室模型估算唑吡坦的药动学参数。结果：受试制剂和参比制剂的药动学参数如下：AUC0-t分别为（564．19±139．11）和（451．58±115．94）μg·h·L^-1；AUC0-∞分别为（588．49±139．40）和（474．56±119．43）μg·h·L^-1；Cmax分别为（155．48±39．43）和（125．11±33．33）μg·L^-1；tmax分别为（0．75±0．27）和（1．14±0．31）h；t1/2分别为（1．76±0．69）和（2．12±0．51）h。受试制剂的相对生物利用度为（126．0±12．0）％。结论：经统计学分析，两种国产唑吡坦片剂不具有生物等效性。

Determination of Zolpidem in Human Plasma by HPLC-FLU and Study on Its Bioequivalence

Objective ： To study the pharmacokinetics and relative bioavailability of zolpidem tablets made in China by HPLC-FLU in healthy volunteers and to guide the clinical medication. Method： Eighteen male healthy volunteers received 10 mg zolpidem tablet o- rally in a random crossover design. Drug concentrations in plasma were determined by HPLC-FLU and the pharmacokinetics parameters were estimated by non-compartment model. Result： The main pharmacokinetic parameters of tested and reference tablets were as follow：AUC0-t were （564.19 ±139.11） μg·h·L^-1 and （451.58 ±115.94） μg·h·L^-1 ,AUC0-∞ were （588.49 ± 139.40） μg·h·L^-1 and （474.56 ± 119.43）μg·h·L^-1 ,Cmax were （155.48 ±39.43） μg·L^-1 and （125.11 ±33.33） μg·L^-1 ,tmax were （0.75 ±0.27） h and （ 1.14 ± 0.31 ） h, t1/2 and （ 1.76 ± 0.69 ） h and （ 2.12 ± 0.51 ） h, respectively. The relative bioavailability of the test tablet was （126.0 ±12.0）% ;Conclusion： The results demonstrated that the two tablets were not bioequivalent.