湖南中医药大学学报2025，Vol.45Issue(5)：856-861,6.DOI:10.3969/j.issn.1674-070X.2025.05.010
利格列汀片的制备及体内外评价
Preparation and in vitro/in vivo evaluation of linagliptin tablets
摘要
Abstract
Objective To develop a generic linagliptin tablet with consistent in vitro dissolution and in vivo bioequivalence to the reference preparation.Methods Linagliptin tablets were prepared.A high performance liquid chromatography(HPLC)-based in vitro dissolution testing method was established to determine the cumulative dissolution of both the test and the reference preparations in four media:pH 1.0 hydrochloric acid solution,pH 4.5 sodium acetate buffer,pH 6.8 potassium dihydrogen phosphate buffer,and water.The dissolution similarity between the preparations was assessed using the model-independent approach(f2 similarity factor).Concurrently,a single-dose,two-preparation,two-sequence,two-period crossover pharmacokinetic study was conducted in healthy adult subjects,with blood concentrations of linagliptin measured under fasting and high-fat post-meal conditions.Pharmacokinetic parameters were calculated.Results The cumulative dissolution profiles of the test and reference preparations were similar in all four dissolution media.Pharmacokinetic analysis revealed that under both fasting and fed conditions,the geometric mean ratios(GMRs)and 90％confidence intervals(CIs)for Cmax and AUC0-t of the test preparation relative to the reference preparation fell entirely within the acceptance range of 80.00％-125.00％.Conclusion The test preparation of linagliptin tablets exhibited similar in vitro dissolution and pharmacokinetic bioequivalence to the reference preparation.关键词
利格列汀片/溶出曲线/原研制剂/生物等效/高效液相色谱法Key words
linagliptin tablets/dissolution profile/reference preparation/bioequivalence/high performance liquid chromatography分类
药学引用本文复制引用
龙世玉,刘秀,秦杰峰,王玲兰,任超,刘文龙..利格列汀片的制备及体内外评价[J].湖南中医药大学学报,2025,45(5):856-861,6.基金项目
国家自然科学基金项目(81874344) （81874344）
湖南省自然科学基金项目(2022JJ80048). （2022JJ80048）
