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含利多卡因的单层透皮贴剂:使用中子散射法测定水和利多卡因的迁移率。

Single layer transdermal film containing lidocaine: water and lidocaine mobility determined using neutron scattering.

机构信息

Dipartimento Farmaceutico, Università di Parma, 43100 Parma, Italy.

出版信息

J Pharm Sci. 2010 Oct;99(10):4277-84. doi: 10.1002/jps.22152.

Abstract

The diffusivity of lidocaine through a polymer film developed for transdermal drug administration has been characterized by macroscopic permeation experiments and by neutron quasielastic spectroscopy that provides information on microscopic diffusivity parameters. It turns out that film hydration plays a key role on the performance and efficiency of the investigated system. Diffusion of lidocaine, at the microscopic level, is triggered by the presence of "mobile water." At hydration levels below 15% (weight water/weight hydrated film) neither lidocaine nor water show any appreciable long-range diffusion. At higher hydration levels, the onset of water long-range diffusion triggers diffusion of lidocaine through the film. The use of neutron quasielastic scattering makes it possible to measure lidocaine mobility within the film without the need of any additional physical barrier.

摘要

通过宏观渗透实验和提供微观扩散参数信息的中子准弹性光谱学对用于经皮给药的聚合物膜中利多卡因的扩散率进行了表征。结果表明,膜水合作用对所研究系统的性能和效率起着关键作用。在微观水平上,利多卡因的扩散是由“可移动水”的存在引发的。在水合水平低于 15%(水的重量/水合膜的重量)时,利多卡因和水都没有表现出任何明显的长程扩散。在更高的水合水平下,水的长程扩散的开始引发了利多卡因通过膜的扩散。使用中子准弹性散射使得可以在不使用任何其他物理屏障的情况下测量膜内利多卡因的迁移率。

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