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Human oral drugs absorption is correlated to theirin vitrouptake by brush border membrane vesicles

Authors
Journal
International Journal of Pharmaceutics
0378-5173
Publisher
Elsevier
Publication Date
Volume
336
Issue
1
Identifiers
DOI: 10.1016/j.ijpharm.2006.11.045
Keywords
  • Absorption
  • Transport
  • Bbmv
  • In Vivo–In Vitrocorrelation
Disciplines
  • Biology

Abstract

Abstract Brush border membrane vesicles (BBMV) were prepared from the rabbit small intestine for testing drug absorption potency through the enterocyte's apical membrane, which is an important compartment for drug oral absorption. Some modifications have been made to the traditional vesicle assay for adapting it to the 96-well plate format. The accumulation of 23 reference drugs was measured, and the data showed a good correlation with human oral absorption with a correlation coefficient R = 0.853 ( P < 0.001), with the exception of a few false positive results. As the measured drug absorption may contain a membrane/protein binding component as well as drug uptake into vesicles, these two fractions can be discriminated by changing extravesicular osmolarity using different mannitol concentrations. This model can be applied for evaluating drug absorption rate/mechanisms, and helping drug selection in early drug research and development.

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