Abstract
The deconvolution principle was used to evaluate the extent of absorption and first-pass elimination of selected drugs. In the first example, deconvolution of the portal blood profiles of etretinate (ET, a synthetic retinoid) indicated that there was significant gut-wall conversion of ET to acitretin (ETA, the primary metabolite of ET) during a 60-min intestinal perfusion of ET. In the second example, deconvolution was used to confirm that the extent of carbovir disappearing from the gastrointestinal lumen was matched by the extent of carbovir appearance in the portal blood. Thus, deconvolution has several important applications in the study of absorption and intestinal first-pass metabolism.
Footnotes
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Send reprint requests to: Cheryl L. Zimmerman, Ph.D., College of Pharmacy, University of Minnesota, 308 Harvard St. SE, Minneapolis, MN 55455.
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↵1 Present address: 17.2256C, Glaxo Wellcome, Five Moore Dr., Research Triangle Park, NC 27709.
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↵2 Present address: 3M Pharmaceuticals, 3M Center Building 270–3S-05, St. Paul MN 55144-1000.
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This work was supported in part by Glaxo Inc., PHS Grants RO1-AI28236 and RO1-CA55493, and the University of Minnesota International Student Work Opportunity Program.
- Abbreviations used are::
- AUC
- area under the curve
- ET
- etretinate
- CBV
- (−)-carbocyclic 2′,3′-dideoxy-2′,3′-didehydroguanosine
- PC
- phosphatidylcholine
- HPLC
- high performance liquid chromatography
- Received February 26, 1997.
- Accepted July 11, 1997.
- The American Society for Pharmacology and Experimental Therapeutics
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Use of the Deconvolution Principle in the Estimation of Absorption and Pre-systemic Intestinal Elimination of Drugs
