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萜烯诱导盐酸普萘洛尔经皮吸收的增强及其机制。

Enhancement and mechanism of transdermal absorption of terpene-induced propranolol hydrochloride.

机构信息

Department of Pharmacy, Medical College of Chinese People's Armed Police Force, Tianjin 300162, China.

出版信息

Arch Pharm Res. 2011 Sep;34(9):1477-85. doi: 10.1007/s12272-011-0909-2. Epub 2011 Oct 6.

Abstract

For the purpose of efficient and safe transdermal administration of propranolol hydrochloride (PHCl), effects of (+)-borneol, (+)-camphor, and α-bisabolol (5 w/v%) in 66.6% ethanol solution on transdermal permeation across rat skin in vitro and their enhancement mechanism was investigated with fourier transform infrared spectroscopy, differential scanning calorimetry, and PHCl-stratum corneum binding studies. Each of (+)-borneol, (+)-camphor, and α-bisabolol significantly increased the transdermal flux of PHCl through rat skin in comparison to the control. The enhancement mechanism of the terpenes is involved with disruption of the lipid bilayer and increase of PHCl partitioning coefficient to the stratum corneum. As for α-bisabolol, the protect effect of skin from dehydration and an important reason of irritation incident were observed with differential scanning calorimetry for the first time.

摘要

为了实现盐酸普萘洛尔(PHCl)的高效、安全经皮给药,考察了(+)-龙脑、(+)-樟脑和 α- 红没药醇(5w/v%)在 66.6%乙醇溶液中的作用,通过傅里叶变换红外光谱、差示扫描量热法和 PHCl-角质层结合研究,探讨了它们对体外透皮的影响及其增强机制。与对照组相比,(+)-龙脑、(+)-樟脑和 α- 红没药醇均显著增加了 PHCl 经大鼠皮肤的透皮通量。萜类化合物的增强机制涉及到破坏脂质双层和增加 PHCl 分配系数至角质层。对于 α- 红没药醇,首次通过差示扫描量热法观察到其对皮肤脱水的保护作用和一个重要的刺激性事件的原因。

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