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. [10.1038/ja.2012.28]
Evaluation, synthesis and characterization of tacrolimus impurities
P. FerraboschiPrimo
;D.R. ColomboSecondo
;M. De MieriPenultimo
;
2012
Abstract
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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