国产酮咯酸氨丁三醇分散片的人体相对生物利用度研究

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。

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

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.