洛索洛芬钠片剂的人体相对生物利用度研究

Relative bioavailability of loxoprofen in healthy volunteers

目的 :考察健康受试者口服洛索洛芬钠片的药代动力学 ,判断其与进口洛索洛芬钠 2种制剂是否生物等效。方法 :2 0例健康受试者按体重指数进行分层随机交叉服用洛索洛芬钠被试制剂或参比制剂 6 0mg ,采用高效液相色谱法测定血浆中洛索洛芬钠的浓度。结果 :口服 6 0mg洛索洛芬钠被试制剂和参比制剂的主要药代动力学参数分别为 :t1/ 2ke为 (96 .2± 2 3.1)和 (98.2± 17.1)min ;AUC0～t为 (5 6 3.1± 6 7.5 )和 (5 6 5 .4± 90 .8) μg·min·mL-1,Cmax为 (6 .36± 1.32 )和 (6 .0 9± 1.4 0 ) μg·mL-1,Tmax为 (2 3.5± 14 .2 )和 (2 3.0± 10 .2 )min。被试制剂的相对生物利用度为 (10 1.5± 17.4 ) %。结论 :2种制剂具有生物等效性。

Objective:To study pharmacokinetics and relative bioavailability following oral administration of loxoprofen in healthy volunteers.Methods:A single oral loxoprofen tablets were given according to a randomized 2 way cross over design with two preparations.Plasma concentration of loxoprofen was determined by HPLC.Results:The main pharmacokinetic parameters after oral administration of the test and reference loxoprofen(60mg) were as follows: t 1/2ke were (96.2±23.1) and (98.2± 17.1)min;AUC 0～t were(563.1±67.5) and (565.4±90.8)μg·min·mL -1 ; C max were (6.36± 1.32) and(6.09±1.40)μg·mL -1 ; T max were (23.5±14.2) and (23.0±10.2)min,respectively.The relative biovailability of the test loxoprofen was (101.5±17.4)%.Conclusion:Two formations of loxoprofen are bioequivalent.