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）