盐酸非索非那定片在中国健康受试者中的生物等效性研究  

Bioequivalence study of fexofenadine hydrochloride tablets in healthy Chinese subjects

作　　者：崔英子[1] 崔东洋 于爽 杨海淼[1] CUI Ying-zi;CUI Dong-yang;YU Shuang;YANG Hai-miao(Laboratory Phase I Clinical Trial,Affiliated Hospital of Changchun University of Chinese Medicine,Chagnchun 130021,Jilin Province,China;Jiangsu Hengrui Medicine Co.,Ltd.,Lianyungang 222000,Jiangsu Province,China)

机构地区：[1]长春中医药大学附属医院Ⅰ期临床试验研究室,吉林长春130021 [2]江苏恒瑞医药股份有限公司,江苏连云港222000

出　　处：《中国临床药理学杂志》2023年第7期1018-1022,共5页The Chinese Journal of Clinical Pharmacology

摘　　要：目的评价盐酸非索非那定片在中国健康受试者的生物等效性和安全性。方法用随机、开放、空腹四周期、餐后两周期、重复交叉、自身对照的试验设计。空腹28例/餐后40例健康受试者口服盐酸非索非那定片受试制剂和参比制剂60 mg,用液相色谱-串联质谱法测定血药浓度,用非房室模型计算非索非那定的药代动力学参数。结果空腹试验中盐酸非索非那定片受试制剂和参比制剂的主要药代动力学参数如下:C_(max)分别为(242.00±109.00)和(230.00±97.90)ng·mL^(-1),AUC_(0-t)分别为(1483.77±444.73)和(1469.81±501.47)ng·mL^(-1)·h,AUC_(0-∝)分别为(1533.18±448.35)和(1525.18±505.80)ng·mL^(-1)·h。2种制剂的C_(max)、AUC_(0-t)和AUC_(0-∞)经对数转换后的90%置信区间分别为96.13%~114.62%、96.53%~109.88%和96.23%~109.18%。餐后试验中盐酸非索非那定片受试制剂和参比制剂的主要药代动力学参数如下:C_(max)分别为(98.10±32.50)和(106.00±29.90)ng·mL^(-1),AUC_(0-t)分别为(622.24±165.84)和(627.53±164.37)ng·mL^(-1)·h,AUC_(0-∝)分别为(677.04±174.82)和(684.69±177.12)ng·mL^(-1)·h。2种制剂的C_(max)、AUC_(0-t)和AUC_(0-∞)经对数转换后的90%置信区间分别为83.31%~100.86%、94.96%~103.30%和94.62%~103.37%。结论在空腹和餐后条件下,盐酸非索非那定片受试制剂与参比制剂具有生物等效性,安全性良好。Objective To evaluate the bioequivalence and safety of fexofenadine hydrochloride tablets in healthy Chinese subjects.Methods This study was a randomized,open-lable,4 fasting cycles,2 postprandial cycles,repeat-cross,own-controls design.28 healthy subjects were enrolled under fasting condition and 40 were enrolled under fed condition.These healthy subjects were given 60 mg oral fexofenadine hydrochloride tablets test and reference formulation;plasma drug concentrations were analyzed by liquid chromatography-tandem mass spectrometry;the pharmacokinetic parameters of Fexofenadine were calculated by non-compartmental methods.Results The main pharmacokinetic parameters of the fasting test:the C_(max)of the test and reference formulations were(242.00±109.00)and(230.00±97.90)ng·mL^(-1);AUC_(0-t)were(1483.77±444.73)and(1469.81±501.47)ng·mL^(-1)·h;AUC_(0-∝)were(1533.18±448.35)and(1525.18±505.80)ng·mL^(-1)·h.The 90%confidence intervals of the geometric mean ratios of C_(max),AUC_(0-t)and AUC_(0-∞) were 96.13%-114.62%,96.53%-109.88% and 96.23%-109.18%.In the postprandial state,the C_(max) of the testand reference formulations were(98.10±32.50)and(106.00±29.90)ng·mL^(-1);AUC_(0-t) were(622.24±165.84)and(627.53±164.37)ng·mL^(-1)·h;AUC_(0-∝) were(677.04±174.82)and(684.69±177.12)ng·mL^(-1)·h.The 90% confidence intervals of the geometric mean ratios of C_(max),AUC_(0-t) and AUC_(0-∞) were 83.31%-100.86%,94.96%-103.30% and 94.62%-103.37%.Conclusion Test and reference formulations of fexofenadine werebioequivalent under both fasting and fed states,with good safety.

关 键 词：盐酸非索非那定片 液相色谱-串联质谱法 生物等效性 

分 类 号：R976[医药卫生—药品]