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治疗性超声对人体角质层中分配系数和扩散系数的影响。

Effect of therapeutic ultrasound on partition and diffusion coefficients in human stratum corneum.

作者信息

Mitragotri S

机构信息

Department of Chemical Engineering, University of California, Santa Barbara, CA 93106, USA.

出版信息

J Control Release. 2001 Mar 12;71(1):23-9. doi: 10.1016/s0168-3659(00)00344-8.

Abstract

Application of various enhancers including ultrasound and chemicals has been shown to enhance transdermal drug transport. Most of these enhancers increase transdermal transport by increasing either partition or diffusion coefficients in lipid bilayers. Although the effect of such enhancers on skin permeability has been measured in many cases, the effect of the same enhancers on solute partition and diffusion coefficients has not been measured since such measurements are difficult. In this paper, we describe application of a new method that can be used to determine the effect of enhancers on partition and diffusion coefficients. This method is based on two independent measurements of the transport properties of the SC and a theoretical model. This method was tested for five solutes including estradiol, napthol, aldosterone, lidocaine, and testosterone. Measurements based on our method showed that the primary effect of therapeutic ultrasound (1 MHz) is on diffusion coefficient and not partition coefficient. Specifically, ultrasound enhanced diffusion coefficients of these solutes by up to 15-fold. However, it did not significantly enhance partition coefficients. The method described in this paper is quite general and can be used to measure the effect of various enhancers on partition and diffusion coefficients.

摘要

包括超声和化学物质在内的各种促进剂已被证明可增强经皮药物转运。这些促进剂大多通过增加脂质双层中的分配系数或扩散系数来提高经皮转运。尽管在许多情况下已测量了此类促进剂对皮肤渗透性的影响,但由于此类测量困难,尚未测量相同促进剂对溶质分配系数和扩散系数的影响。在本文中,我们描述了一种可用于确定促进剂对分配系数和扩散系数影响的新方法的应用。该方法基于对表皮角质层(SC)转运特性的两项独立测量以及一个理论模型。该方法针对包括雌二醇、萘酚、醛固酮、利多卡因和睾酮在内的五种溶质进行了测试。基于我们方法的测量表明,治疗性超声(1兆赫)的主要作用是对扩散系数而非分配系数。具体而言,超声使这些溶质的扩散系数提高了多达15倍。然而,它并未显著提高分配系数。本文所述方法具有广泛适用性,可用于测量各种促进剂对分配系数和扩散系数的影响。

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