地氯雷他定片在中国健康受试者的生物等效性研究  

Bioequivalence of lacosamide tablets in Chinese healthy subjects

作　　者：单娜[1,2] 苗琳琳 江大海 郝沛琪 王晓梅 党艳妮[1,2] 张笑笑 武焱旻[3] 刘敬浩 刘媛媛 经慧[3] 李轲 刘峰[1,2] SHAN Na;MIAO Lin-lin;JIANG Da-hai;HAO Pei-qi;WANG Xiao-mei;DANG Yan-ni;ZHANG Xiao-xiao;WU Yan-min;LIU Jing-hao;LIU Yuan-yuan;JING Hui;LI Ke;LIU Feng(School of Medicine,Shaanxi Institute of Intrenational Trade&Commerce,Xianyang 712046,Shaanxi Province,China;Shandong Danhong Pharmaceutical Co.,Ltd.,Heze 712000,Shandong Province,China;PhaseⅠClinical Laboratory,The Central Hostpital of Xuzhou City,Xuzhou 430040,Jiangsu Province,China)

机构地区：[1]陕西国际商贸学院医药学院,陕西咸阳712046 [2]山东丹红制药有限公司,山东菏泽712000 [3]徐州市中心医院Ⅰ期临床试验研究室,江苏徐州430040

出　　处：《中国临床药理学杂志》2023年第11期1608-1612,共5页The Chinese Journal of Clinical Pharmacology

摘　　要：目的评价地氯雷他定片仿制药与原研药在中国健康受试者中单剂量空腹和餐后条件下给药的生物等效性。方法用单中心、随机、开放、单次给药、两制剂、两周期、双交叉试验设计,空腹和餐后试验各入组24例受试者。空腹或餐后条件下单次口服地氯雷他定片受试制剂和参比制剂5 mg,用液相色谱串联质谱法测定血浆中地氯雷他定的浓度。用Phoenix WinNonlin 8.0软件计算主要药代动力学(PK)参数。结果空腹组的地氯雷他定片受试制剂和参比制剂主要PK参数:地氯雷他定C_(max)分别为(3.81±1.44)和(3.76±1.25)ng·mL(-1),AUC_(0-t)分别为(52.18±19.21)和(50.71±18.21)ng·mL(-1)·h,AUC_(0-∞)分别为(54.52±19.71)和(53.19±19.07)ng·mL(-1)·h。餐后组的地氯雷他定片受试制剂和参比制剂主要PK参数:地氯雷他定C_(max)分别为(3.52±1.20)和(3.55±1.10)ng·mL(-1),AUC_(0-t)分别为(64.33±52.76)和(61.59±42.24)ng·mL(-1)·h,AUC_(0-∞)分别为(75.48±93.64)和(72.03±64.78)ng·mL(-1)·h。在空腹和餐后条件下,受试制剂与参比制剂主要PK参数的90%置信区间均在80.00%~125.00%内。结论在空腹和餐后条件下,中国健康受试者单次口服地氯雷他定片仿制药与原研药具有生物等效性。Objective To study the bioequivalence of generic and original desloratadine tablets in Chinese healthy subjects after single dose under fasting and postprandial conditions.Methods A single-center,random,open,single-dose,two-preparations,double-period,crossover study was adopted.A total of 48 healthy adult male and female subjects(24 cases of fasting test and 24 cases of postprandial test)were included in the random crossover administration.Single oral dose 5 mg of test and reference were taken under fasting and postprandial conditions,respectively.Plasma concentration of desloratadine were determined by liquid chromatography tandem mass spectrometry.The main pharmacokinetic(PK)parameters were calculated by Phoenix WinNonlin 8.0 software.Results The main PK parameters of the test and reference preparations of desloratadine tablets in the fasting group were as follows:C_(max) were(3.81±1.44)and(3.76±1.25)ng·mL^(-1);AUC_(0-t) were(52.18±19.21)and(50.71±18.21)ng·mL^(-1)·h;AUC_(0-∞)were(54.52±19.71)and(53.19±19.07)ng·mL^(-1)·h.The main PK parameters of the test and reference preparations of desloratadine tablets in the postprandial group were as follows:C_(max) were(3.52±1.20)and(3.55±1.10)ng·mL^(-1);AUC_(0-t) were(64.33±52.76)and(61.59±42.24)ng·mL^(-1)·h;AUC_(0-∞)were(75.48±93.64)and(72.03±64.78)ng·mL^(-1)·h.Under fasting and postprandial conditions,the 90%confidence intervals of the main PK parameters of the test and reference preparations are both 80.00%-125.00%.Conclusion Under fasting and postprandial conditions,a single oral dose of generic and original desloratadine tablets in Chinese healthy adult volunteers showed bioequivalence.

关 键 词：地氯雷他定 3-羟基地氯雷他定 生物等效性 药代动力学 

分 类 号：R976[医药卫生—药品]