酮咯酸氨丁三醇片的人体相对生物利用度

Study of relative bioavailability of ketorolac tromethamine tablets in healthy volunteers

目的:研究酮咯酸氨丁三醇片剂的人体相对生物利用度及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片剂和胶囊,采用高效液相色谱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20mg的受试和参比制剂的达峰时间tmax分别为(0.61±0.20)h和(0.73±0.21)h;血药浓度峰值Cmax分别为(3182.4±406.4)μg.L-1和(3176.2±450.6)μg.L-1;药时曲线下面积AUC0→24分别为(18464.8±4434.0)μg.h.L-1和(17490.7±4355.0)μg.h.L-1。2种制剂的药动学参数差异均无显著性(P>0.05),受试制剂的相对生物利用度为(105.6±8.6)%。结论:2种制剂具有生物等效性。

OBJECTIVE To study the relative bioavailability of ketorolac tromethamine tablets by comparing with reference capsules in healthy volunteers. METHODS 18 male healthy volunteers orally took a single dose of 20 mg tablets and capsules in randamized self-crossover way. The plasma concentrations of ketorolac tromethamine were determined by HPLC. RESULTS The pharmacokinetic parameters of reference and test drugs were as follows： tmax （0. 61±0. 20） and（0. 73± 0. 21） h; Cmax （3 182. 4± 406. 4）and （3 176. 2 ± 450. 6）μg·L^-1 ;AUC（0→24） （18 464. 8 ± 4 434. 0） and （17 490. 7 ±4 355.0）μg·h·L^-1. There was no statistical difference between ketorolac tromethamine tablets and capsules in pharmacokinetic parameters （P〉0. 05）. The relative bioavailability of ketorolac tromethamine tablets was （105.57 ± 8. 60） %. CONCLUSION Two preparations of ketorolac tromethamine tablets and capsules were bioequivalent.