中国临床药理学杂志2024，Vol.40Issue(6)：894-898,5.DOI:10.13699/j.cnki.1001-6821.2024.06.023
拉莫三嗪片在中国健康受试者中的生物等效性的研究
Bioequivalence of lamotrigine tablets in Chinese healthy subjects
摘要
Abstract
Objective To study the pharmacokinetic characteristics of lamotrigine tablets in Chinese healthy subjects under fasting and fed conditions,and to evaluate the bioequivalence and safety profiles between the domestic test preparation and the original reference preparation.Methods Twenty-four Chinese healthy male and female subjects were enrolled under fasting and fed conditions,18 male and 6 female subjects under fasting conditions,17 male and 7 female subjects under fed conditions.A random,open,single-dose,two preparations,two sequences and double-crossover design was used.Plasma samples were collected over a 72-hour period after give the test or reference preparations 50 mg under fasting and fed conditions.The concentration of lamotrigine in plasma was detected by liquid chromatography-tandem mass spectrometry,and the main pharmacokinetic parameters were calculated to evaluate the bioequivalence by WinNonLin 8.1 program.Results The main pharmacokinetic parameters of single-dose the tested and reference preparations were as follows:The fasting condition Cmax were(910.93±248.02)and(855.87±214.36)ng·mL-1;tmax were 0.50(0.25,4.00)and 1.00(0.25,3.50)h;t1/2 were(36.1±9.2)and(36.0±8.2)h;AUC0_72h were(27 402.40±4 752.00)and(26 933.90±4 085.80)h·ng·mL-1.The fed condition Cmax were(701.62±120.67)and(718.95±94.81)ng·mL-1;tmax were 4.00(1.00,5.00)and 4.00(0.50,5.00)h;t1/2 were(44.2±12.4)and(44.0±12.0)h;AUC0-72h were(30 253.20±7 018.00)and(30 324.60±6 147.70)h·ng·mL-1.The 90％confidence intervals of the geometric mean ratios of Cmax and AUC0-72 hfor the test preparation and reference preparation were all between 80.00％and 125.00％under fasting and fed conditions.Conclusion Two kinds of lamotrigine tablets are bioequivalent,and have similar safety in Chinese healthy male and female subjects under fasting and fed conditions.关键词
拉莫三嗪片/药代动力学/生物等效性/液相色谱-串联质谱Key words
lamotrigine/pharmacokinetics/bioequivalence/liquid chromatography-tandem mass spectrometry分类
医药卫生引用本文复制引用
姜金生,欧阳冬生,陈红英,陈俊,陈尧,陈开义,张雪花,胡杰,刘鑫,黄馨仪..拉莫三嗪片在中国健康受试者中的生物等效性的研究[J].中国临床药理学杂志,2024,40(6):894-898,5.基金项目
国家自然科学基金资助项目(82073942) （82073942）
湖南省自然科学基金资助项目(2022JJ80097、2022JJ80113) （2022JJ80097、2022JJ80113）
