Document Detail


Comparison of the gastrointestinal absorption and bioavailability of fenofibrate and fenofibric acid in humans.
MedLine Citation:
PMID:  20145261     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
This study compared the gastrointestinal (GI) absorption characteristics and absolute bioavailability of fenofibric acid and fenofibrate (which is converted to fenofibric acid in vivo) in healthy volunteers. Treatments were delivered to the proximal small bowel, distal small bowel, and colon using a site-specific delivery system (Enterion capsule) and to the stomach by oral administration of equimolar doses. Serial blood samples were collected for 120 hours postdose and assayed for plasma fenofibric acid concentrations. The absolute bioavailability of each treatment was determined relative to 50 mg of fenofibric acid administered intravenously. Plasma exposure to fenofibric acid following fenofibric acid administration was approximately 1.5 times higher than that following fenofibrate administration for delivery to the proximal and distal small bowel and following oral administration, and it was approximately 5 times higher following colon delivery. The absolute bioavailability in the stomach, proximal small bowel, distal small bowel, and colon was approximately 81%, 88%, 84%, and 78%, respectively, for fenofibric acid and 69%, 73%, 66%, and 22%, respectively, for fenofibrate (P < .0001 and P = .033 for fenofibric acid vs fenofibrate in the colon and distal small bowel, respectively). In conclusion, fenofibric acid is well absorbed throughout the GI tract and has greater bioavailability than fenofibrate in all GI regions.
Authors:
Tong Zhu; Jean-Claude Ansquer; Maureen T Kelly; Darryl J Sleep; Rajendra S Pradhan
Publication Detail:
Type:  Comparative Study; Journal Article; Randomized Controlled Trial; Research Support, Non-U.S. Gov't     Date:  2010-02-09
Journal Detail:
Title:  Journal of clinical pharmacology     Volume:  50     ISSN:  1552-4604     ISO Abbreviation:  J Clin Pharmacol     Publication Date:  2010 Aug 
Date Detail:
Created Date:  2010-07-20     Completed Date:  2010-11-08     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  0366372     Medline TA:  J Clin Pharmacol     Country:  United States    
Other Details:
Languages:  eng     Pagination:  914-21     Citation Subset:  IM    
Affiliation:
100 Abbott Park Road, Dept R4PK, Bldg AP13A-3, Abbott Park, IL 60064-6104, USA. tong.zhu@abbott.com
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MeSH Terms
Descriptor/Qualifier:
Administration, Oral
Adolescent
Adult
Antilipemic Agents / administration & dosage,  pharmacokinetics*
Area Under Curve
Biological Availability
Drug Delivery Systems
Half-Life
Humans
Injections, Intravenous
Intestinal Absorption
Male
Metabolic Clearance Rate
Middle Aged
Procetofen / administration & dosage,  analogs & derivatives*,  pharmacokinetics
Young Adult
Chemical
Reg. No./Substance:
0/Antilipemic Agents; 26129-32-8/fenofibric acid; 49562-28-9/Procetofen

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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