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第二种增溶剂对药物在胶束溶液中的分配系数及其跨人工膜渗透速率的影响。

Effect of a second solubilizate on the partition coefficient of drugs in micellar solution and their permeation rate across an artificial membrane.

作者信息

Alhaique F, Giacchetti D, Marchetti M, Riccieri F M

出版信息

J Pharm Pharmacol. 1977 Jul;29(7):401-6. doi: 10.1111/j.2042-7158.1977.tb11353.x.

DOI:10.1111/j.2042-7158.1977.tb11353.x
PMID:19577
Abstract

The distribution of a solubilizate between micelles and the aqueous phase does not obey a simple partition law when a second solubilizate species is present. Alterations of the apparent partition coefficient cannot be explained in terms of a simple displacement mechanism, following the interaction of both solubilizates with the same site of the micelle. A non linear increase in solubilizate association to micelles following an increase in surfactant concentration is observed in the presence of a second solubilizate. A depression in the cloud point temperature follows the addition of a second species and is such that cannot be interpreted as a simple additive effect. Alteration of the apparent partition coefficient in a miscellar solution has an effect on the permeation rate of the solubilizate across an artificial membrane. Biopharmaceutical implications are discussed.

摘要

当存在第二种增溶物质时,增溶物在胶束和水相之间的分布并不遵循简单的分配定律。表观分配系数的变化不能用简单的置换机制来解释,即两种增溶物与胶束的同一部位相互作用。在存在第二种增溶物的情况下,随着表面活性剂浓度的增加,观察到增溶物与胶束的缔合呈非线性增加。加入第二种物质后会出现浊点温度降低的情况,且这种降低不能解释为简单的加和效应。胶束溶液中表观分配系数的变化会影响增溶物通过人工膜的渗透速率。本文讨论了其生物药剂学意义。

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