盐酸格拉司琼口腔崩解片生物等效性评价

Bioequivalence and relative bioavailability of granisetron hydrochloride orally disintegrating tablet in healthy volunteers

目的：研究盐酸格拉司琼口腔崩解片在健康人体内的药动学和相对生物利用度,并与市售盐酸格拉司琼胶囊比较,进行生物等效性评价。方法：20例男性健康受试者双周期随机交叉单剂量口服2 mg盐酸格拉司琼口腔崩解片和胶囊,两次试验间隔为1周,采用LC/MS/MS法测定血浆中格拉司琼浓度。结果：受试制剂与参比制剂的血药浓度-时间曲线基本一致,盐酸格拉司琼口腔崩解片和胶囊的cmax分别为（7.42±2.19）和（7.32±2.35）ng/mL;tmax分别为（1.3±0.4）和（1.4±0.3）h;t1/2分别为（5.62±1.95）和（5.74±1.96）h;AUC0-24分别为（43.18±13.04）和（38.41±9.88）ng.h.mL-1,AUC0-∞分别为（47.27±14.73）和（41.54±10.84）ng.h.mL-1。盐酸格拉司琼口腔崩解片和胶囊的主要药动学参数无显著性差异（P〉0.05）。结论：盐酸格拉司琼口腔崩解片和胶囊具有生物等效性,盐酸格拉司琼口腔崩解片的相对生物利用度为（111.41±13.55）%。

Objective：To evaluate the pharmacokinetics and relative bioavailability of granisetron hydrochloride orally disintegrating tablet in healthy volunteers.Methods： Twenty healthy male volunteers were enrolled in the study.A single oral dose（2 mg） of test and reference granisetron preparations were given respectively to the volunteers according to randomized two-way cross-over study design.The washout period was 1 week.The plasma concentrations of granisetron were determined by LC/MS/MS method.Results： Mean plasma concentration-time curve of the test product was highly close to that of the reference product.The main pharmacokinetic parameters of the test and reference preparations were as follows： cmax（7.42±2.19） and（7.32±2.35） ng/mL;tmax（1.3±0.4） and（1.4±0.3） h;t1/2（5.62±1.95） and（5.74±1.96） h;AUC024（43.18±13.04） and（38.41±9.88） ng·h·mL-1,AUC0∞（47.27±14.73） and（41.54±10.84） ng·h·mL-1,respectively.There was no significant difference in cmax,tmax,AUC024 and AUC0∞ between granisetron hydrochloride orally disintegrating tablet and capsule（P〉0.05）.Conclusion： The results of statistical analysis showed that the two formulations are bioequivalent.The relative bioavailability of orally disintegrating tablet is（111.41±13.55）%.