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β-内酰胺类抗生素的胃肠道吸收。III:大鼠小肠中一元青霉素和头孢唑林离子化形式原位吸收的动力学证据及结构-吸收速率关系

GI absorption of beta-lactam antibiotics. III: Kinetic evidence for in situ absorption of ionized species of monobasic penicillins and cefazolin from the rat small intestine and structure-absorption rate relationships.

作者信息

Tsuji A, Miyamoto E, Kubo O, Yamana T

出版信息

J Pharm Sci. 1979 Jul;68(7):812-6. doi: 10.1002/jps.2600680706.

Abstract

Absorption rates of monobasic beta-lactam antibiotics were measured as a function of lumen solution pH between 4 and 9 by utilizing the rat intestinal recirculating method in situ. Between pH 6.5 and 9, the absorption rate constants of ionized antibiotics were almost identical; but, at pH 4, the unionized species were highly absorbed, depending on their lipophilicity through the GI membrane lipoidal barrier. The structure-absorption rate relationship was established with the unstirred layer model.

摘要

采用大鼠肠道原位再循环法,测定了一价β-内酰胺类抗生素在管腔溶液pH值为4至9时的吸收速率。在pH值6.5至9之间,离子化抗生素的吸收速率常数几乎相同;但在pH值为4时,非离子化形式的抗生素吸收程度很高,这取决于它们通过胃肠道膜脂质屏障的亲脂性。利用未搅拌层模型建立了结构-吸收速率关系。

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