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.
Evaluation, synthesis and characterization of tacrolimus impurities / P. Ferraboschi, D.R. Colombo, M. De Mieri, P. Grisenti. - In: JOURNAL OF ANTIBIOTICS. - ISSN 0021-8820. - 65:7(2012 Jul), pp. 349-354.
|Titolo:||Evaluation, synthesis and characterization of tacrolimus impurities|
FERRABOSCHI, PATRIZIA (Primo)
COLOMBO, DIEGO RODOLFO (Secondo)
DE MIERI, MARIA (Penultimo)
|Parole Chiave:||23,24-anhydro tacrolimus; 39,40-dihydro tacrolimus; ascomycin; immunosuppressant; macrolactam|
|Settore Scientifico Disciplinare:||Settore BIO/10 - Biochimica|
|Data di pubblicazione:||lug-2012|
|Digital Object Identifier (DOI):||http://dx.doi.org/10.1038/ja.2012.28|
|Appare nelle tipologie:||01 - Articolo su periodico|