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标题：SOLVENT DRAG EFFECT IN DRUG INTESTINAL ABSORPTION. II. STUDIES ON DRUG ABSORPTION CLEARANCE AND WATER INFLUX
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作者：AKIRA KARINO ; MASAHIRO HAYASHI ; SHOJI AWAZU 等
期刊名称：Biological and Pharmaceutical Bulletin
印刷版ISSN：0918-6158
电子版ISSN：1347-5215
出版年度：1982
卷号：5
期号：9
页码：670-677
DOI：10.1248/bpb1978.5.670
出版社：The Pharmaceutical Society of Japan
摘要：In order to study the solvent drag effect, it was shown that back flux of absorbed drug from blood to intestinal lumen can be ignored but the back flux of water cannot. Then, apparent water influx was calculated as a new measure of solvent drag based on the model in which the back flux of D₂O from blood to lumen was considered during absorption. Consequently, the correlation between drug absorption clearance (CL_drug) and apparent water influx was highly significant for benzoic acid, salicylic acid, p-hydroxybenzoic acid, antipyrine, cephalexin (CEX) and cefroxadine (CXD), resulting the high solvent drag effects were detected. The mean values of the slopes in the regression lines of CL_drug versus apparent water influx, i.e., sieving coefficients, were smaller than one for benzoic acid and salicylic acid, but the values were not significantly different from one. The sieving coefficients of the other drugs were significantly smaller than one. From these results, the molecular size dependence in the reflection from the intestinal membrane during absorption was clearly shown. And the intercepts of the regression lines including diffusive permeabilities were found to be significantly different from zero in CEX and CXD. On the basis of the sieving coefficients and intercept values obtained in such ways, the appropriateness of this model was discussed.
关键词：absorption clearance