国产洛索洛芬钠片剂的人体相对生物利用度

Ralative Bioavailability of Loxoprofen Sodium Tablet in Healthy Volunteers

目的:研究健康受试者口服洛索洛芬钠片(loxoprofen sodium)的药代动力学,以进口洛索洛芬钠(loxonin,日本三共株式会社生产)作为参比制剂计算相对生物利用度,判断两种制剂是否生物等效。方法:20名健康受试者按体重指数进行分层随机服用洛索洛芬钠被试制剂或参比制剂60mg,用高效液相色谱法测定血浆中洛索洛芬钠的浓度。结果:经3P97程序拟合,口服国产和进口洛索洛芬钠60mg的主要药代动力学参数分别为:t_(1/2ke)为93.9±19.8min和92.4±16.3min;AUC_(0-t)为596.97±104.12μg·min·mL^(-1)和598.78±109.62μg·min·mL^(-1),C_(max)为6.40±2.12μg·mL^(-1)和6.60±2.04μg·mL^(-1),t_(max)为25.0±14.3min和23.5±10.3min。结论:国产洛索洛芬钠片的相对生物利用度为(101.2±17.4)％。经统计学分析,两制剂具有生物等效性。

OBJECTIVE: To study pharmacokinetics and relative bioavailability following oral administration of loxoprofen sodium tablet in healthy volunteers. METHODS: A single oral domestic and imported loxoprofen tablets were given according to a randomized 2 way cross-over design. Plasma concentration of loxoprofen was determined by HPLC. RESULTS: The main pharmacokinetic parameters after oral administration of domestic and imported loxoprofen sodium tablet(60mg) were: t1/2ke 93. 9 ± 19.8min, 92.4± 16.3min; AUC0-t 596.97 ± 104.l2μg.min.mL-1,598.18 ± 109.62μg. min.mL-1; Cmax 6.40 ± 2.12μg.mL-1 , 6.60 ± 2.04μg.mL-1,tmax 25.0± 14.3min,23. 5 ± 10.3min, respectively. CONCLUSION: The relative bioavailability of domestic loxoprofen sodium tablet was(101.2 ± 17.4)%. The results demonstrated that two formations of loxoprofen sodium tablet were bioequivalent.