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标题：SOLVENT DRAG EFFECT IN DRUG INTESTINAL ABSORPTION. I. STUDIES ON DRUG AND D2O ABSORPTION CLEARANCES
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作者：AKIRA KARINO ; MASAHIRO HAYASHI ; TOSHIHARU HORIE 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：6
页码：410-417
DOI：10.1248/bpb1978.5.410
出版社：The Pharmaceutical Society of Japan
摘要：It was shown that the intestinal absorption clearance of D₂O (CL_D₂O) could be a more appropriate index to study the solvent drag effect than water volume flow which was the difference between water influx and outflux in the intestinal lumen. Then, the correlation between the intestinal abosrption clearances of drugs (CL_drug) and CL_D₂O were studied using the in situ recirculating method in the rat small intestine. The drugs used were low molecular drugs, that is, benzoic acid, salicylic acid, p-hydroxybenzoic acid and antipyrine, and comparably high molecular drugs, that is, cephalexin (CEX), cefroxadine (CXD) and cephalothin (CET). CL_drug and CL_D₂O were obtained in hypertonic, isotonic and hypotonic perfused solution adjusted with sodium chloride. Consequently, the correlations for all drugs except CET were significant and high solvent drag effects were observed. CL_drug of benzoic acid, salicylic acid and antipyrine were approximately equal to CL_D₂O, suggesting that the intestinal mucosa could not distinguish these lower molecular drugs from water. For the high molecular drugs such as cephalosporins, however, some extent of reflection from the membrane was certainly found in CEX and CXD, and the extent in CET was assumed much larger than CEX and CXD, resulting that the contribution of solvent drag in CET could not be found. Consequently, it was suggested that the solvent drag had some important role in the intestinal absorption of cephalosporins.
关键词：absorption clearance