利培酮口腔崩解片的生物等效性研究

目的研究利培酮口腔崩解片的生物等效性。方法采用双周期随机交叉试验设计。40名男性健康受试者分别服用1mg利培酮普通片和口腔崩解片后,采集不同时间点的静脉血样,液相色谱-串联质谱法测定血浆中利培酮和9-羟基利培酮的浓度。结果利培酮的药动学符合有滞后时间的一房室模型,利培酮的药动学参数AUC0-16分别为（23.65±6.23）和（23.20±5.08）ng.h.L-1,AUC0-∞为（25.01±6.63）和（24.44±5.38）ng.h.L-1,Cmax为（4.99±1.26）和（4.96±1.18）ng.L-1,tmax为（1.29±0.43）和（1.42±0.43）h。相对生物利用度为（100±12）%;9-羟基利培酮的药动学参数AUC0-96分别为（99.35±34.77）和（93.96±27.75）ng.h.L-1,AUC0-∞为（104.87±35.20）和（98.39±27.67）ng.h.L-1,Cmax为（4.12±1.62）和（4.20±1.82）ng.L-1,tmax为（5.36±3.63）和（5.40±3.58）h,相对生物利用度为（99±28）%。结论利培酮口腔崩解片与普通片具有生物等效性。

Bioequivalence of risperidone orally disintegrating tablets in healthy volunteers

Objective To investigate the bioequivalence of risperidone orally disintegrating tablets in healthy volun-teers.Methods The plasma concentrations of risperidone and 9-hydroxyrisperidone were assayed by LC-MS/MS after a single dose of 1mg reference or test tablets was given to 40healthy volunteers in a two-way crossover study.Results The characteristics of plasma concentration-time curve of risperidone fit the one compartment model.The main pharma-cokinetics parameters of risperidone tablets and orally disintegrating tablets were as follows：for risperidone,AUC0-16 was（23.65±6.23）and（23.20±5.08）ng.h.L-1,AUC0-∞ was（25.01±6.63）and（24.44±5.38）ng.h.L-1,Cmaxwas（4.99±1.26）and（4.96±1.18）ng.L-1,tmaxwas（1.29±0.43）and（1.42±0.43）h.The relative bio-availability was（100±12）%.For 9-hydroxyrisperidone,AUC0-96was（99.35±34.77）and（93.96±27.75）ng.h.L-1,AUC0-∞ was（104.87±35.20）and（98.39±27.67）ng.h.L-1,Cmaxwas（4.12±1.62）and（4.20±1.82）ng.L-1,tmaxwas（5.36±3.63）and（5.40±3.58）h.The relative bioavailability was（99±28）%.Conclusion The two formulations have similar pharmacokinetic characteristics and are bioequivalent.