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. Ferraboschi
Primo
;
D.R. Colombo
Secondo
;
M. De Mieri
Penultimo
;
2012-07

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.
23,24-anhydro tacrolimus; 39,40-dihydro tacrolimus; ascomycin; immunosuppressant; macrolactam
Settore BIO/10 - Biochimica
Article (author)
File in questo prodotto:
Non ci sono file associati a questo prodotto.
Pubblicazioni consigliate

Caricamento pubblicazioni consigliate

I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.

Utilizza questo identificativo per citare o creare un link a questo documento: http://hdl.handle.net/2434/178069
Citazioni
  • ???jsp.display-item.citation.pmc??? 2
  • Scopus 10
  • ???jsp.display-item.citation.isi??? 10
social impact