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阴道给药的系统方法V:1-链烷酸的原位阴道吸收

Systems approach to vaginal delivery of drugs V: in situ vaginal absorption of 1-alkanoic acids.

作者信息

Hwang S, Owada E, Suhardja L, Ho N F, Flynn G L, Higuchi W I

出版信息

J Pharm Sci. 1977 Jun;66(6):781-4. doi: 10.1002/jps.2600660609.

Abstract

The vaginal absorption of a homologous series of ionizable compounds, the 1-alkanoic acids, was studied using a perfusion method with a rib-cage cell surgically implanted in the rabbit vagina. The absorption rates of these compounds followed first-order kinetics. The physical model previously used for the 1-alkanols, but accounting for the pKa and pH effects in the present case was employed in the analysis of the carboxylic acid data. The aqueous diffusion layer thickness was 0.031 cm. The permeability coefficient for the lipoidal pathway increased 3.5-fold per methylene group. Both values agree reasonably well with those obtained in the alcohol study.

摘要

使用外科手术植入兔阴道的肋骨笼细胞灌注法,研究了一系列可电离化合物(1-链烷酸)的阴道吸收情况。这些化合物的吸收速率符合一级动力学。分析羧酸数据时采用了先前用于1-链烷醇的物理模型,但考虑了本案例中的pKa和pH效应。水扩散层厚度为0.031厘米。脂类途径的渗透系数每增加一个亚甲基就增加3.5倍。这两个值与在醇类研究中获得的值相当吻合。

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