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Intestinal drug absorption enhancers: synergistic effects of combinations.

作者信息

Enslin Gill M, Hamman Josias H, Kotze Awie F

机构信息

Department of Pharmaceutical Sciences, Tshwane University of Technology, Pretoria, South Africa.

出版信息

Drug Dev Ind Pharm. 2008 Dec;34(12):1343-9. doi: 10.1080/03639040802098185.

DOI:10.1080/03639040802098185
PMID:18686089
Abstract

Although many absorption enhancers have been investigated, very few are used clinically. A need exists therefore for more effective absorption enhancers. The drug-absorption-enhancing effects of combinations of N-trimethyl chitosan chloride (TMC) with degrees of quaternization of 48 and 64%, dicarboxymethyl chitosan oligosaccharide, and chitosan lactate oligomer with monocaprin and melittin were compared to their individual performances using the in vitro Caco-2 cell model. Combining the absorption enhancers showed synergism in both the reduction of the transepithelial electrical resistance (TEER) and the enhancement of the transport of a macromolecular model compound across this intestinal epithelial cell layer. Lower concentrations of the absorption enhancers in the combination groups exhibited greater effects on the epithelial cells compared with the individual absorption enhancers.

摘要

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