国产酮咯酸氨丁三醇分散片的人体相对生物利用度研究

Study on relative bioavailability of ketorolac tromethamine dispersible tablets in healthy volunteers

目的评价酮咯酸氨丁三醇分散片剂的人体相对生物利用度,并与胶囊剂比较其生物等效性。方法 18名男性健康受试者随机、自身对照交叉单剂量口服酮咯酸氨丁三醇分散片和胶囊,采用RP-HPLC法测定血浆中酮咯酸氨丁三醇的浓度。结果单剂量口服含酮咯酸氨丁三醇20 mg的受试和参比制剂,其达峰时间Tmax分别为(0.68±0.30)、(0.80±0.38)h;血药浓度峰值Cmax分别为(3 124.44±382.96)、(3 170.28±289.03)ng/mL;药时曲线下面积AUC(0→24)分别为(13 939.32±2 471.53)、(14 312.29±2 268.26)ng.h/mL。两种制剂的药物动力学参数比较差异无统计学意义(P>0.05),受试制剂的相对生物利用度(F)为97.86%±11.62%。结论两种制剂具有生物等效性。

Objective To evaluate the relative bioavailability of ketorolac tromethamine dispersible tablets and to compare reference bioequivalence with capsules in healthy volunteers. Methods 18 male healthy volunteers orally took a single dose of 20 mg dispersible tablets and capsules in randomized self-crossover ways.The plasma concentration of ketorolac tromethamine was determined by RP-HPLC. Results The pharmacokinetic parameters of reference and test drugs were as follows：Tmax（0.68±0.30）and（0.80±0.38）h;Cmax（3 124.44±382.96）and（3 170.28±289.03）ng/mL;AUC（0→24）（13 939.32±2 471.53）and（14 312.29±2 268.26）ng·h/mL respectively.There was no significant difference between ketorolac tromethamine dispersible tablets and capsules in pharmacokinetic parameters（P〈0.05）.The relative bioavailability of ketorolac tromethamine tablets was 97.86%±11.62%. Conclusion Two preparations of ketorolac tromethamine dispersible tablets and capsules are bioequivalence.