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链烷酸的经皮吸收II:正规溶液理论的应用。

Percutaneous absorption of alkanoic acids II: Application of regular solution theory.

作者信息

Liron Z, Cohen S

出版信息

J Pharm Sci. 1984 Apr;73(4):538-42. doi: 10.1002/jps.2600730426.

DOI:10.1002/jps.2600730426
PMID:6726640
Abstract

The permeability coefficient, Kp, of pure unbranched alkanoic acids (C2-C7) applied to isolated porcine skin, reached a maximum in the solubility parameter (delta 2) range of 9.7-10 cal1 /2/cm3/2. When these and other penetrants were delivered from a solvent vehicle, the following linear relationships could be demonstrated: (a) between log Kp and the molar attraction constant of the penetrant [delta 2v2 or (-Ev)1/2] for six unbranched and six branched acids delivered from 1 M solution in n-heptane; (b) between Kp and the partial molal volume difference in n-heptane (-v2-v02) for the unbranched acids; and (c) between Kp and (-v2-v02) for propionic acid delivered from 1 M solutions in nine solvents having delta 1 values in the range 7.4-12.7 cal1 /2/cm3/2. Drug penetrability in a given series could be assessed from knowledge of the excess free energy of the penetrant in the delivery system used.

摘要

将纯的直链烷酸(C2 - C7)应用于离体猪皮时,其渗透系数Kp在溶解度参数(δ2)为9.7 - 10 cal1/2/cm3/2的范围内达到最大值。当这些及其他渗透剂从溶剂载体中递送时,可以证明以下线性关系:(a)对于从正庚烷中的1M溶液递送的六种直链酸和六种支链酸,log Kp与渗透剂的摩尔吸引常数[δ2v2或(-Ev)1/2]之间的关系;(b)对于直链酸,Kp与正庚烷中的偏摩尔体积差(-v2 - v02)之间的关系;以及(c)对于从δ1值在7.4 - 12.7 cal1/2/cm3/2范围内的九种溶剂中的1M溶液递送的丙酸,Kp与(-v2 - v02)之间的关系。给定系列中的药物渗透性可以通过了解所用递送系统中渗透剂的过剩自由能来评估。

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