Evaluation, synthesis and characterization of tacrolimus impurities

被引:0
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作者
Patrizia Ferraboschi
Diego Colombo
Maria De Mieri
Paride Grisenti
机构
[1] Biochimica e Biotecnologie per la Medicina,Dipartimento di Chimica
[2] Università degli Studi di Milano,undefined
[3] EUTICALS SpA,undefined
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关键词
ascomycin; 23,24-anhydro tacrolimus; 39,40-dihydro tacrolimus; immunosuppressant; macrolactam;
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摘要
Tacrolimus is an immunosuppressant macrolactam of fermentative origin. By means of HPLC, LC-MS and NMR analyses, coupled with the reference standard synthesis, the main impurities of tacrolimus bulk drug samples were identified and their chemical-physical properties reported. Known ascomycin and tautomers I and II were detected. The correct relative retention time HPLC value of 39,40-dihydro tacrolimus was established. The not described 23,24-anhydro derivative was detected and completely characterized. A full characterization of ascomycin and 39,40-dihydro tacrolimus was also reported.
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页码:349 / 354
页数:5
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