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

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;AUC0~24(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,AUC0~24 and AUC0~∞ between granisetron hydrochloride orally disintegrating tablet and capsule(P0.05).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)%.