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Metabolic profiles of difluprednate in rabbit ocular tissues after instillation of difluprednate ophthalmic emulsion.
- Source :
-
Xenobiotica . Aug2010, Vol. 40 Issue 8, p569-577. 9p. 4 Diagrams, 3 Charts, 3 Graphs. - Publication Year :
- 2010
-
Abstract
- 1. Difluprednate (DFBA; 6a,9-difluoro-11β,17,21-trihydroxy-1,4-pregnadiene-3,20-dione 21-acetate 17-butyrate) is an effective anti-inflammatory agent derived from prednisolone. The present study aimed to evaluate the metabolite profile of DFBA in rabbit ocular tissues after instillation of DFBA ophthalmic emulsion. 2. The high-performance liquid chromatography with radiochemical detection was employed to analyze radioactivity in rabbit ocular tissues that had been instilled with a 3H-DFBA 0.05% ophthalmic emulsion. At 0.5 and 2 h after instillation, DFBA was not detected in the cornea, aqueous humor, or iris/ciliary body. Instead, 21-deacetylated DFBA (DFB), 17-debutylated DFB (DF), and an unknown metabolite were found. 3. The unknown metabolite was identified as de-17-side chain-glucocorticoid metabolite (DF21C), which is a novel glucocorticoid metabolite formed by the scission of the 17-side chain via an unknown metabolic reaction pathway. The Ki value of DF21C was 5.6 x 10-7 mol/L, indicating very weak glucocorticoid receptor binding of DF21C (approximately 1000-fold less than that of DFBA and DFB). [ABSTRACT FROM AUTHOR]
Details
- Language :
- English
- ISSN :
- 00498254
- Volume :
- 40
- Issue :
- 8
- Database :
- Academic Search Index
- Journal :
- Xenobiotica
- Publication Type :
- Academic Journal
- Accession number :
- 52175194
- Full Text :
- https://doi.org/10.3109/00498254.2010.490308