利格列汀片的制备及体内外评价

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本文引用: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[JI.湖南中医药大学学报,2025,45(5):856-861.

[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 [中图分类号]R927 [文献标志码]A [文章编号]doi:10.3969/j.issn.1674-070X.2025.05.010

[Abstract]Objective To developa generic linagliptintablet with consistentin vitro dissolutionandinvivo bioequivalence tothereferencepreparationMethodsLinagliptintabletswereprepared.Ahighperformanceliquidchromatography(HPLC)-based invitrodisslution testingmethodwasestablishedtodeterminethecumulativedisolutionofboththetestandthereference preparationsinfourmedia:pH1Ohydrochloricacidsolution,pH4.5sodiumacetatebufer,pH6.8potassiumdihydrogen phosphatebuffr,andwater.Thedissolutionsimilaritybetweenthepreparationswasassessedusingthemodel-independent approach ( I2 similarity factor).Concurrentlyasingle-dose,two-preparation,two-sequence,two-periodcrossverpharmacokinetic studywasconductedinhealthyadultsubjects,withbloodconcentrationsoflinagliptinmeasuredunderfastingandhighfatpostmeal conditions.Pharmacokineticparameters werecalculatedResultsThecumulativedisolutionprofilesofthetestandreference preparationsweresimilarinallfourdissolutionmediaPharmacokineticanalysisrevealedthatunderbothfastingandfed conditions,the geometric mean ratios (GMRs) and 90% confidence intervals (CIs) for Cmax and AUC 10+ of the test preparation relative to the reference preparation fell entirely within the acceptance range of 80.00% 1 .125.00% .Conclusion The test preparation of linagliptin tablets exhibited similar in vitro dissolutionand pharmacokinetic bioequivalence to thereference preparation.

[Keywords]nagliptintablets;diolutonprofileferencepreparatio;boeqilene;hghpformanceliquidhomtoga

利格列汀作为二肽基肽酶-4(dipeptidyl pepti-dase-4,DPP-4)抑制剂,最初由勃林格殷格翰公司开发,并于2011年首次在美国批准上市,适应证为2型糖尿病。(剩余9066字)

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