利培酮片人体生物等效性研究  

Bioequivalence of Risperidone Tablets in Healthy Volunteers

作　　者：王蕊[1] 李云 闫黎明[1] WANG Rui;LI Yun;YAN Liming(Jiangsu Nhwa Pharmaceutical Co.LTD.,Xuzhou,Jiangsu 221007,China)

机构地区：[1]江苏恩华药业股份有限公司,徐州221007

出　　处：《药学与临床研究》2020年第4期255-258,共4页Pharmaceutical and Clinical Research

摘　　要：目的:考察2种利培酮片在健康受试者空腹和餐后状态下的药代动力学参数,进行生物等效性评价。方法:采用开放、随机、两周期、交叉试验设计,空腹和餐后各48例受试者交叉服用受试制剂或参比制剂,LC-MS/MS检测血浆中的利培酮和帕利哌酮的浓度。结果:在空腹状态下,受试制剂和参比制剂利培酮的Cmax为(7.06±3.42)和(6.77±2.81)ng·m L^-1,AUC0-t为(44.5±46.9)和(41.5±42.1)ng·h·m L^-1,AUC0-∞为(45.4±47.9)和(42.4±43.2)ng·h·m L^-1;帕利哌酮的Cmax为(4.20±1.59)和(4.13±1.51)ng·m L^-1,AUC0-t为(117±29)和(116±30)ng·h·m L^-1,AUC0-∞为(125±32)和(124±33)ng·h·m L^-1。在餐后状态下,受试制剂和参比制剂利培酮的Cmax为(6.30±3.06)和(6.47±3.03)ng·m L^-1,AUC0-t为(44.6±32.6)和(44.3±35.1)ng·h·m L^-1,AUC0-∞为(45.5±32.8)和(45.0±35.5)ng·h·m L^-1;帕利哌酮的Cmax为(4.24±2.08)和(4.20±2.14)ng·m L^-1,AUC0-t为(121±36)和(118±34)ng·h·m L^-1,AUC0-∞为(132±38)和(128±38)ng·h·m L^-1。结论:空腹和餐后状态下,利培酮和帕利哌酮的90%CI均在80%~125%,2种利培酮片具有生物等效性。Objective:To study the pharmacokinetics and bioequivalence of risperidone tablets in healthy volunteers.Methods:An open-label,randomized,crossover study was conducted in 48 healthy volunteers under the conditions of fasting and fed,respectively.Plasma concentrations of risperidone and pallipiperidone were determined by LC-MS/MS.Results:Under the condition of fasting,the main pharmacokinetic parameters of risperidone for the test and reference tablets were respectively as follows:Cmax,(7.06±3.42) and (6.77±2.81) ng·m L^-1;AUC0-t,(44.5±46.9) and (41.5±42.1) ng·h·m L^-1;AUC0-∞,(45.4±47.9)and (42.4±43.2) ng·h·m L^-1;and those of pallipiperidone:Cmax,(4.20±1.59) and (4.13±1.51) ng·m L^-1;AUC0-t,(117±29) and (116±30) ng·h·m L^-1;AUC0-∞,(125±32) and (124±33) ng·h·mL^-1.Under the condition of fed,the same parameters of risperidone for the test and reference were respectively as follows:Cmax,(6.30±3.06)and (6.47±3.03) ng·mL^-1;AUC0-t,(44.6±32.6) and (44.3±35.1) ng·h·m L^-1;AUC0-∞,(45.5±32.8) and (45.0±35.5) ng·h·m L^-1;and those of pallipiperidone:Cmax,(4.24±2.08) and (4.20±2.14) ng·mL^-1;AUC0-t,(121±36)and (118±34) ng·h·m L^-1;AUC0-∞,(132±38) and (128±38) ng·h·mL^-1.Conclusion:Under the conditions of fasting and fed,the 90%CIs of risperidone and pallipiperidone for the test to the reference were between80%-125%,and the two risperidone tablets were bioequivalent.

关 键 词：利培酮 帕利哌酮 药代动力学 生物等效性 

分 类 号：R969.1[医药卫生—药理学]