Document Detail


Correlation between the systemic clearance of drugs and their food effects in humans.
MedLine Citation:
PMID:  21692649     Owner:  NLM     Status:  Publisher    
Abstract/OtherAbstract:
Context: Food effects were defined as positive, when coadministration of food causes an increase in the extent of absorption (AUC(0-∞)) of a drug when compared with fasted state drug administration and no effect when coadministration of food causes no change in AUC(0-∞). In general, low solubility drugs exhibit positive food effects due to improved solubility in fed state administration. But, certain high-solubility and high-permeability drugs that undergo extensive presystemic metabolism exhibit positive food effects because of the increased splanchnic hepatic blood flow in the fed state presumably causing a fraction of drug to bypass first-pass metabolism during absorption. Objective: In this study, systemic clearance (Cl) of structurally diverse high-permeability and high-solubility drugs was correlated to their food effects to explore whether drugs undergoing low clearance exhibited no food effects and drugs undergoing high clearance exhibited positive food effects. Methods: Six drugs exhibiting positive food effects and nine drugs exhibiting no food effects (for comparison) were selected for linear regression analysis. Results: Regression analysis of the selected drugs indicated that percent food effects correlated linearly to Cl and fitted the equation: percent food effects = 0.9163 × Cl - 6.4789. The R(2), p-value and power of the regression model were >0.88, 0.9999, respectively indicating the direct correlation between Cl and food effects of the selected model drugs; other statistical tests validated the model. Conclusion: The model indicated that high-solubility and high-permeability drugs undergoing Cl of more than 27 L/h may exhibit statistically significant positive food effects.
Authors:
Venugopal P Marasanapalle; Ramesh R Boinpally; Haijian Jim Zhu; Andreas Grill; Fuxing Tang
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Publication Detail:
Type:  JOURNAL ARTICLE     Date:  2011-6-21
Journal Detail:
Title:  Drug development and industrial pharmacy     Volume:  -     ISSN:  1520-5762     ISO Abbreviation:  -     Publication Date:  2011 Jun 
Date Detail:
Created Date:  2011-6-22     Completed Date:  -     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  7802620     Medline TA:  Drug Dev Ind Pharm     Country:  -    
Other Details:
Languages:  ENG     Pagination:  -     Citation Subset:  -    
Affiliation:
Exploratory Pharmaceutics, Forest Research Institute, Farmingdale, NY, USA.
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