盐酸托烷司琼口崩片人体生物等效性研究

目的本试验旨在研究由广州莱泰制药有限公司研制的盐酸托烷司琼口崩片的相对生物利用度,评价其生物等效性。方法采用双周期随机自身交叉试验设计,18名男性健康受试者口服受试制剂或参比制剂的盐酸托烷司琼5mg,采用LC-MS法测定给药后不同时间点盐酸托烷司琼的血药浓度,用DASVer2.01计算药动学参数。结果盐酸托烷司琼参比制剂（R）与受试制剂（A）的主要药代动力学参数分别为（均数±标准差）Cmax15.37±7.62和15.58±8.46ng·mL-1;Tmax2.58±0.81和2.92±1.10h;AUC0-48179.39±123.59和172.33±96.49ng·h·mL-1和AUC0→∞204.85±156.26和190.16±112.03ng·mL-1。受试制剂对参比制剂的平均相对生物利用度F（以AUC0-48作为评价依据）为105.3%（92.3%～120.0%）。结论受试制剂与参比制剂具有生物等效性。

Bioequivalence of Tropisetron hydrochloride orally disintegrating tablets in healthy volunteers

Objective This study was designed to evaluate the relative bioavailability and bioequiavailability of tropisetron hydrochloride orally disintegrating tablets, which is produced by the Guangzhou Pharmaceutical Co., Ltd. Methods A single dose （5 mg test or reference formulation） was given to 18 healthy male volunteers ac- cording to an open randomized crossover design. The concertration of tropisetron hydrochloride in the plasma was determined by LC-MS. The parameters were calculated and the bioavailability and bioequivalence of two formula- tions were evaluated by DAS Ver 2.01. Results The pharmacokinetic parameters （mean ± standard deviation） oftropisetron hydrochloride reference formulation （R） and study formulation （A） as follows： Cmax （ng·mL-^1）： 15.37±7.62 and 15.58 ± 8.46; Tmax （h）： 2.58± 0.81 and 2.92 ±1.10; AUC0-48 （ng-h.mL^-1）： 179.39±123.59 and 172.33±96.49; AUCo0→∞ （ng·h·mL^-1）： 204.85 ±156.26 and 190.16±112.03. Using AUC0-48 as evaluate index, the average relative bioavailability F （the study formulation compare to the reference formulation） is 105.3%（92.3% - 120.0%）. Conclusion The tropisetron hydrochloride formulations are bioequivalent.