Please use this identifier to cite or link to this item:
Title: Biopharmaceutics of β-Cyclodextrin Derivative-Based Formulations of Acitretin in Sprague-Dawley Rats
Authors: Liu, X.
Lin, H.-S. 
Chan, S.Y. 
Ho, P.C. 
Keywords: Acitretin
Bile excretion
Issue Date: Apr-2004
Citation: Liu, X., Lin, H.-S., Chan, S.Y., Ho, P.C. (2004-04). Biopharmaceutics of β-Cyclodextrin Derivative-Based Formulations of Acitretin in Sprague-Dawley Rats. Journal of Pharmaceutical Sciences 93 (4) : 805-815. ScholarBank@NUS Repository.
Abstract: Acitretin, an active metabolite of etretinate, is as effective as etretinate in the treatment of psoriasis. Recently, we developed some water-soluble formulations of acitretin with 2-hydroxypropyl-β -cyclodextrin (HPBCD)/randomly substituted methyl-β-cyclodextrin (RMBCD). In this study, the biopharmaceutic properties of these formulations were tested in Sprague-Dawley rats. After single intravenous dosing (2.5, 5, or 10 mg/kg) with the HPBCD-based formulation, the area under the plasma concentration-time curve of acitretin increased proportionally with the dose and its clearance remained unchanged within the tested dose range. We also found that the RMBCD-based formulation of acitretin improved its bioavailability and decreased the variations in various pharmacokinetic parameters. The improved biopharmaceutic properties of RMBCD-based acitretin might be attributed to its enhanced aqueous solubility. The elimination of acitretin through bile excretion was also studied. Our results indicated that the major fraction of acitretin (∼-40%) was excreted in the bile as β-glucuronide conjugate and only trace amounts were excreted as unconjugated acitretin (∼0.5%). This finding further confirmed the importance of conjugated metabolism and biliary excretion in the elimination of this drug. © 2004 Wiley-Liss, Inc. and the American Pharmacists Association.
Source Title: Journal of Pharmaceutical Sciences
ISSN: 00223549
DOI: 10.1002/jps.10578
Appears in Collections:Staff Publications

Show full item record
Files in This Item:
There are no files associated with this item.


checked on Jan 21, 2022


checked on Jan 21, 2022

Page view(s)

checked on Jan 20, 2022

Google ScholarTM



Items in DSpace are protected by copyright, with all rights reserved, unless otherwise indicated.