Please use this identifier to cite or link to this item: https://doi.org/10.1002/jps.10578
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
Biopharmaceutics
Cyclodextrin
Pharmacokinetics
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. https://doi.org/10.1002/jps.10578
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
URI: http://scholarbank.nus.edu.sg/handle/10635/75670
ISSN: 00223549
DOI: 10.1002/jps.10578
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