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温度对阿夫唑嗪渗透模式的影响:基于 DOE 的研究。

Temperature influencing permeation pattern of alfuzosin: an investigation using DoE.

机构信息

Talla Padmavathi College of Pharmacy, Orus, Warangal, India.

Talla Padmavathi College of Pharmacy, Orus, Warangal, India.

出版信息

Medicina (Kaunas). 2015;51(4):253-61. doi: 10.1016/j.medici.2015.07.002. Epub 2015 Jul 30.

DOI:10.1016/j.medici.2015.07.002
PMID:26424191
Abstract

BACKGROUND AND OBJECTIVE

There has been relatively little investigation of the effect of temperature on skin permeation compared to other methods of penetration enhancement. A principal physicochemical factor which controls the passive diffusion of a solute from a vehicle into the skin arises from the skin temperature. The aim of this ex vivo study was to probe into the effect of heat on transdermal absorption of alfuzosin hydrochloride from ethyl cellulose-polyvinyl pyrrolidone (EC-PVP) based transdermal systems.

MATERIALS AND METHODS

Principles of design of experiment (DoE) were used to systematically study the influence of temperature on transdermal permeation of alfuzosin. Ex vivo transdermal permeation studies were carried out at varied donor compartment temperatures. Permeation data analysis was carried out and activation energy for transdermal permeation was estimated.

RESULTS

Temperature found to enhance ex vivo permeation parameters of alfuzosin hydrochloride from its transdermal systems. It was also noted that chemical permeation enhancers potentiate permeation enhancing effect of temperature. The permeation flux values approximately doubled after exposure to 45°C. The activation energy for transdermal permeation was found lower for the runs with chemical permeation enhancers indicating existence of a lower energy barrier in the presence of chemical permeation enhancers.

CONCLUSION

The method reported here is a simple and useful tool for studying the effect of heat on percutaneous absorption. Such temperature dependent enhancement of flux can be more pronounced at skin surface temperatures >45°C.

摘要

背景与目的

与其他渗透增强方法相比,人们对温度对皮肤渗透的影响的研究相对较少。控制溶质从载体向皮肤被动扩散的主要物理化学因素源于皮肤温度。本离体研究旨在探讨加热对盐酸阿夫唑嗪从乙基纤维素-聚乙烯吡咯烷酮(EC-PVP)基透皮系统中经皮吸收的影响。

材料与方法

采用实验设计(DoE)原理系统研究温度对盐酸阿夫唑嗪经皮渗透的影响。在不同供体腔室温度下进行离体透皮渗透研究。对渗透数据进行分析,并估算经皮渗透的活化能。

结果

发现温度可增强盐酸阿夫唑嗪从其透皮系统中的离体渗透参数。还注意到化学渗透增强剂增强了温度对渗透增强的作用。暴露于 45°C 后,渗透通量值增加了约一倍。对于含有化学渗透增强剂的运行,经皮渗透的活化能较低,这表明在存在化学渗透增强剂的情况下,存在较低的能量障碍。

结论

这里报道的方法是研究热对经皮吸收影响的简单而有用的工具。在皮肤表面温度>45°C 时,这种依赖于温度的通量增强可能更为明显。

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