安吡昔康胶囊的人体生物等效性

Study on bioequivalence of ampiroxicam capsules in Chinese healthy volunteers

目的：进行试验制剂安吡昔康胶囊与参比制剂安吡昔康片的单剂双交叉人体生物等效性考察。方法：采用高效液相色谱法测定安吡昔康代谢物吡罗昔康血浓度，以DAS软件计算吡罗昔康主要药动学参数，评价两制剂的生物等效性。结果：安吡昔康试验制剂和参比制剂活性代谢物吡罗昔康主要药动学参数t1／2分别为（44．7±9.0）h和（46．2±13.0）h，了k分别为（7．7±2．2）h和（7．2±1．6）h，Cmax分别为（2．6±0．5）mg·L^-1和（2．6±0．5）mg·L^-1，AUC0-144分别为（187．3±32．1）mg·L^-1·h和（188．7±30.0）mg·L^-1·h，AUC0-∞分别为（216．6±36．6）mg·L^-1·h和（219．1±40．2）mg·L^-1·h。试验制剂人体相对生物利用度（100．2±15．9）％。结论：安吡昔康试验制剂和参比制剂中吡罗昔康主要药动学参数周期间和剂型间无显著性差异，为生物等效制剂。

OBJECTIVE To investigate the bioequivalence of ampiroxicam capsule and tablet. METHODS An HPLC method was used to separate the active metabolite of ampiroxicam in plasma after liquid-liquid extraction and detected at ultraviolet wavelength of 360 nm. The main pharmacokinetic parameters were calculated and evaluated by DAS 2. 0. RESULTS The main pharmacokinetic parameters of ampiroxicam capsule and tablet, characterized as piroxicam, were as follows, t1/2 （44.7±9.0） h and （46.2±13.0）h, Tmax（7.7±2.2）h and （7.2±1.6）h,Cmax（2.6±0. 5）mg·L^-1 and （2.6±0.5）mg·L^-1,AUC0-144（187.3±32.1）mg·L^-1·h and （188.7±30.0）mg·L^-1·h,AUC0-∞ （216.6±36.6）mg·L^-1·h and （219.1±40.2）mg·L^-1·h,respec-tively. The relative bioavailability of ampiroxicam capsule was （100.2±15.9）%. CONCLUSION The ampiroxicam capsule and tablet were bioequivalent,and its main pharmacokinetic parameters had no significant difference.