کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
2481725 1556246 2010 11 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Determination of permeation resistance distribution in in vitro cell monolayer permeation experiments
موضوعات مرتبط
علوم پزشکی و سلامت داروسازی، سم شناسی و علوم دارویی اکتشاف دارویی
پیش نمایش صفحه اول مقاله
Determination of permeation resistance distribution in in vitro cell monolayer permeation experiments
چکیده انگلیسی

The results of cell monolayer permeation experiments are often affected by concentration dependent cellular processes, such as active transport and metabolism. The rigorous analysis of the concentration dependence of these processes is often limited by the lack of knowledge of the actual concentration at the site of action because the measurement of the local concentration is seldom feasible. However, the local concentrations can be estimated if the rates into and out of a particular location are known. Thus, an insight into the distribution of the permeation resistance in the in vitro cell monolayer permeation experiments would enable the estimation of local concentrations during the permeation experiments and, consequently, a more thorough analysis of the concentration dependent processes involved in the transepithelial transfer of compounds. In this study, a compartmental model was constructed applicable for dissecting the roles of apical and basal side aqueous boundary layers and the cell membranes in the total permeation barrier for weakly acidic and basic compounds. The model was applied for the analysis of the Caco-2 permeation data of three high permeability compounds, propranolol, metoprolol and ibuprofen. Furthermore, the effects of extracellular pH and the agitation conditions on the local concentrations of these compounds were evaluated.

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: European Journal of Pharmaceutical Sciences - Volume 40, Issue 2, 12 May 2010, Pages 132–142
نویسندگان
, , ,