尼美舒利口腔崩解片在健康人体内的药动学及生物等效性研究

目的:评价2种尼美舒利制剂的生物等效性。方法:20名健康男性志愿者随机交叉单剂量口服尼美舒利口腔崩解片(受试制剂)与尼美舒利片(参比制剂)200mg,采用反相高效液相色谱法测定其血药浓度,并用DAS软件计算药动学参数及评价生物等效性。结果:受试制剂与参比制剂的AUC0～24分别为(54.67±18.25)、(56.15±15.54)μg.h.mL-1,AUC0～∞分别为(56.38±18.03)、(57.63±15.26)μg.h.mL-1,Cmax分别为(7.61±2.72)、(7.50±2.19)μg.mL-1,tmax分别为(3.83±1.39)、(3.80±1.28)h。受试制剂相对于参比制剂的生物利用度为(98.7±22.9)%。结论:2种尼美舒利制剂具有生物等效性。

Pharmacokinetics and Bioequivalence of Nimesulide Orally Disintegrating Tablets in Healthy Volunteers

OBJECTIVE： To evaluate the bioavailability of two nimesulide preparations.METHODS： A total of 20 healthy male volunteers were enrolled in a randomized crossover study in which the subjects were randomly assigned to receive single dose of 200 mg nimesulide orally disintegrating tablets（test） or nimesulide tablets（reference） .The plasma concentrations of nimesulide were determined by RP- HPLC, and the pharmacokinetic parameters and bioavailability were calculated with DAS program.RESULTS： The main pharmacokinetic parameters of nimesulide test and reference preparations were as follow： AUC0-24： （54.67±18.25） vs. （56.15± 15.54）μg·h·mL^-1;AUC0-∞ （56.38± 18.03） vs. （57.63 ± 15.26）μg· h· mL^-1 ; Cmax： （7.61±2.72） vs.（7.50± 2.19）μg · mL^-1;tmax：（3.83± 1.39） and （3.80± 1.28） h,The relative bioavailability of nimesulide orally disintegrating tablets as against nimesulide tablet was（98.7±22.9） % .CONCLUSION： Nimesulide test and reference preparations were bioequivalent.