Document Detail


Effect of food on the relative bioavailability of a hypolipidemic agent (CGP 43371) in healthy subjects.
MedLine Citation:
PMID:  8169802     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
The relative bioavailability of a capsule formulation and the effects of food on the pharmacokinetics of a hypolipidemic agent (CGP 43371) in 12 healthy subjects were examined. Each subject randomly received a single dose of 800 mg of CGP 43371, either as a dispersion formulation under fasting conditions or as a capsule formulation under fasting and fed conditions in a three-way crossover design with a washout period of 2 weeks between each treatment. Serial blood samples were collected at frequent intervals up to 96 h after each treatment. The concentrations of CGP 43371 in plasma were determined by a normal-phase HPLC method. Similar mean pharmacokinetic data (peak plasma drug concentration, 0.16 versus 0.18 micrograms/mL; area under the plasma drug concentration-time curve from time zero to infinity, 4.56 versus 4.22 micrograms.h/mL; time to the peak plasma drug concentration, 10.3 versus 10.2 h; lag time, 3.7 versus 3.8 h; and terminal elimination half-life, 17.8 versus 15.0 h) for the dispersion and capsule formulations under fasting conditions indicated that both formulations were bioequivalent with respect to the rate and extent of absorption. In contrast, the mean peak plasma drug concentration (2.01 micrograms/mL) and area under the curve from time zero to infinity (57.35 micrograms.h/mL) for the capsule formulation with food were enhanced approximately 11- and 14-fold, respectively, when compared with that without food. The corresponding mean lag time (2.1 h) was decreased approximately 50%. These differences in pharmacokinetic parameters were statistically significant, on the basis of an analysis of variance.(ABSTRACT TRUNCATED AT 250 WORDS)
Authors:
J X Sun; A Cipriano; K Chan; M Klibaner; V A John
Publication Detail:
Type:  Clinical Trial; Journal Article; Randomized Controlled Trial    
Journal Detail:
Title:  Journal of pharmaceutical sciences     Volume:  83     ISSN:  0022-3549     ISO Abbreviation:  J Pharm Sci     Publication Date:  1994 Feb 
Date Detail:
Created Date:  1994-06-01     Completed Date:  1994-06-01     Revised Date:  2004-11-17    
Medline Journal Info:
Nlm Unique ID:  2985195R     Medline TA:  J Pharm Sci     Country:  UNITED STATES    
Other Details:
Languages:  eng     Pagination:  264-6     Citation Subset:  IM    
Affiliation:
Drug Development Department, CIBA-GEIGY Corp., Ardsley, NY 10502.
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MeSH Terms
Descriptor/Qualifier:
Anticholesteremic Agents / adverse effects,  pharmacokinetics*
Biological Availability
Capsules
Chromatography, High Pressure Liquid
Emulsions
Food*
Half-Life
Humans
Intestinal Absorption
Male
Rifampin / adverse effects,  analogs & derivatives*,  pharmacokinetics
Chemical
Reg. No./Substance:
0/Anticholesteremic Agents; 0/Capsules; 0/Emulsions; 123036-23-7/CGP 43371; 13292-46-1/Rifampin

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


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