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Pharmacokinetic evaluation of indomethacin ethyl ester-loaded nanoencapsules.

Authors :
Cattani VB
Pohlmann AR
Dalla Costa T
Source :
International journal of pharmaceutics [Int J Pharm] 2008 Nov 03; Vol. 363 (1-2), pp. 214-6. Date of Electronic Publication: 2008 Jul 16.
Publication Year :
2008

Abstract

Goals were to evaluate indomethacin ethyl ester-nanoencapsules (IndOEt-NC) pharmacokinetics in rats and the in vivo ester conversion to indomethacin (IndOH). After i.v. and oral administration exclusively IndOH was detected in plasma. The AUC(IndOEt-NC)/AUC(IndOH) ratio after i.v. dosing was 0.68, accounting for dose and molecular weight differences, probably due to increased IndOH clearance after IndOEt-NC administration (alpha=0.05). The results confirm that antiedematogenic activity reported for IndOEt-NC is due to IndOH. Encapsulation did not protect the ester which in vivo is rapidly released and converted to IndOH, acting as a pro-drug.

Details

Language :
English
ISSN :
0378-5173
Volume :
363
Issue :
1-2
Database :
MEDLINE
Journal :
International journal of pharmaceutics
Publication Type :
Academic Journal
Accession number :
18678236
Full Text :
https://doi.org/10.1016/j.ijpharm.2008.07.008