利格列汀片的制備及體內(nèi)外評價

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本文引用：龍世玉，劉，秀，秦杰峰，王玲蘭，任超，劉文龍。利格列汀片的制備及體內(nèi)外評價[JI.湖南中醫(yī)藥大學(xué)學(xué)報，2025，45（5）：856-861.

[關(guān)鍵詞]利格列汀片；溶出曲線；原研制劑；生物等效；高效液相色譜法 [中圖分類號]R927 [文獻(xiàn)標(biāo)志碼]A [文章編號]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

利格列汀作為二肽基肽酶-4（dipeptidyl pepti-dase-4，DPP-4）抑制劑，最初由勃林格殷格翰公司開發(fā)，并于2011年首次在美國批準(zhǔn)上市，適應(yīng)證為2型糖尿病。（剩余9066字）