地氯雷他定片在中国健康受试者的等效性研究  

Bioequivalence study of desloratadine tablets in healthy Chinese subjects

作　　者：谢朋飞[1] 陈元璐 崔宏娣 龙辉[1] 赵永刚[1] 黄启山 杨鹏 周燕 张永东[1] XIE Peng-fei;CHEN Yuan-lu;CUI Hong-di;LONG Hui;ZHAO Yong-gang;HUANG Qi-shan;YANG Peng;ZHOU Yan;ZHANG Yong-dong(PhaseⅠClinical Centre,Chenzhou No.1 People's Hospital,Chenzhou 423000,Hunan Province,China;Anhui Menjie Technology Development Co.,Ltd,Hefei 230601,Anhui Province,China;Anhui Wanbang Pharmaceutical Technology Co.,Ltd,Hefei 230000,Anhui Province,China)

机构地区：[1]郴州市第一人民医院Ⅰ期临床研究室,湖南郴州423000 [2]安徽门捷科技发展有限公司,安徽合肥230601 [3]安徽万邦医药科技股份有限公司,安徽合肥230000

出　　处：《中国临床药理学杂志》2025年第2期220-224,共5页The Chinese Journal of Clinical Pharmacology

基　　金：郴州市科技发展计划基金资助项目(yfzx201912)。

摘　　要：目的探究地氯雷他定片受试制剂与参比药物在健康受试者中药代动力学(PK)特征,并评价其生物等效性及安全性。方法用随机、开放、两周期交叉设计,受试者空腹或高脂餐后单次口服地氯雷他定片受试制剂或参比药物5mg,用液质联用技术(LC-MS/MS)检测和分析受试者血浆样品中地氯雷他定及代谢物3-羟基地氯雷他定的浓度,并经统计分析软件WinNonLin8.1计算和分析地两制剂主要药代动力学参数,评价其生物等效性。结果空腹试验地氯雷他定片受试制剂与参比药物的主要PK指标:地氯雷他定的C_(max)分别为(3809.82±1016.54)和(3642.36±777.07)pg·mL^(-1);AUC_(0-120h)分别为(5.75×10^(4)±5.03×10^(4))和(5.51×10^(4)±4.00×10^(4))pghmL;AUC_(0-∞)分别为(6.85×10^(4)±1.03×10^(4))和(6.37×10^(4)±7.92×10^(4))pg·h·mL^(-1)。餐后试验地氯雷他定片受试制剂与参比药物的主要PK指标:地氯雷他定的C_(max)分别为(4398.98±1191.22)和(4744.4±1511.97)pg·mL^(-1);AUC_(0-120h)分别为(5.25×10^(4)±1.82×10^(4))和(5.55×10^(4)±1.98×10^(4))pg·h·mL^(-1);AUC_(0-∞)分别为(5.37×10^(4)±1.86×10)和(5.68×10^(4)±2.55×10^(4))pg·h·mL^(-1)。空腹试验和餐后试验地氯雷他定的C_(max)、AUC_(0-t)、AUC_(0-∞)的几何均值比值(GMR,T/R)及其90%置信区间的统计结果均在80.00%~125.00%内。结论空腹或高脂餐后条件下,地氯雷他定片受试制剂与参比药物的主要药代动力学参数无明显差异,具有生物等效性,且安全性及耐受性良好。Objective To explore the pharmacokinetic(PK)characteristics of desloratadine tablets and reference drugs in healthy subjects,and evaluate their bioequivalence and safety.Methods The random,open,two-period,cross-over pharmacokinetic study method was adopted,each subject received a single oral dose of desloratadine tablets test drug(T)or reference drug(R)for 5 mg.The concentrations of desloratadine and 3-hydroxy desloratadine in plasma were determined by liquid chromatography-tandem mass spectrometry(LC-MS/MS);and the PK parameters were calculated by WinNonlin 8.1 software to evaluate the bioequivalence.Results The main PK parameters of T and R of desloratadine were as follows:the fasting condition Cmax were respectively(3809.82±1016.54)and(3642.36±777.07)pg·mL^(-1);AUC_(0-120h)were respectively(5.75×10^(4)±5.03×10^(4))and(5.51×10^(4)±4.00×10^(4))pg·h·mL^(-1);AUC_(0-∞)were respectively(6.85×10^(4)±1.03×10^(4))and(6.37×10^(4)±7.92×10^(4))pg-h·mL^(-1).The fed condition C_(max)were respectively(4398.98±1191.22)and(474.4±1511.97)g·mL^(-1);AUC_(0-120h)were respectively(5.25×10^(4)±1.82×10^(4))and(5.55×10^(4)±1.98×10^(4))pg·h·mL^(-1);AUC_(0-∞)were respectively(5.37×10^(4)±1.86×10^(4))and(5.68×10^(4)±2.04×10^(4))pg·h·mL^(-1).The 90%confidence interval of C_(max),AUC_(0-t)and AUC_(0-∞)of desloratadine were all within 80.00%~125.00%.ConclusionTThere was no significant difference in the main PK parameters between T tablets and R under fasting or high-fat postprandial conditions,and desloratadine tablets were bioequivalent,safe and well tolerated.

关 键 词：地氯雷他定片 中国健康受试者 药代动力学 生物等效性 

分 类 号：R976[医药卫生—药品]