单剂量口服国产和进口阿西美辛胶囊的生物等效性

Bioequivalence of a single oral dose of imported and domestic acemetacin capsule in healthy Chinese men

目的 :评价国产和进口阿西美辛 (AC)胶囊的生物等效性。方法 :采用双交叉试验设计 ,2 4名健康受试者随机接受单剂量口服参比制剂或试验制剂 90mg ,清洗期 7d ;采用固相萃取 HPLC UV法测定AC及其代谢物吲哚美辛 (ID)的血药浓度。cmax,tmax采用实测值 ,梯形法计算AUC ,双单侧t检验法用于生物等效性检验。结果 :国产AC胶囊的相对生物利用度以AC计算 (98 35± 10 35 ) % ,以ID计算 (10 1 46± 10 5 7) % ,经方差分析及双单侧t检验表明两者具有生物等效性。结论

AIM: To evaluate the bioequivalence of imported and domestic acemetacin capsules. METHODS: The study was an open, two-stage, double cross designed trial. The volunteers were randomly assigned to 2 treatment groups. Twenty-four volunteers were administered with a single oral dose of 90 mg acemetacin time-released capsule (imported or domestic) in each stage. There were 7 d 'washout' period between 2 stages. Then 6 mL of whole blood samples were taken to the heparin-decoagulated and acidified (with 50 μL of 1 mol·L -1 of hydrochloride acid) tube after taking the drugs in different time, and the plasma were separated and stored at -30 ℃ . The concentration of acemetacin and its metabolite indomethacin in human plasma was determined by HPLC using UV detector after solid phase extraction. The values of c max and t max were directly measured, and AUC was caculated by linear trapezoid method, while the biological effects of domestic and imported acemetacin were compared by two one-side test. RESULTS: The relative bioavailability of the domestic acemetacin compared with imported one calculated as acemetacin was (98.35±10.35)% and as indomethacin was (101.46±10.57)%. CONCLUSION: The 2 drugs are bioequivalent in healthy Chinese men.