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首页> 外文OA文献 >The effect of pH and organic ester penetration enhancers on skin permeation kinetics of terbutaline sulfate from pseudolatex-type transdermal delivery systems through mouse and human cadaver skins
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The effect of pH and organic ester penetration enhancers on skin permeation kinetics of terbutaline sulfate from pseudolatex-type transdermal delivery systems through mouse and human cadaver skins

机译：pH和有机酯渗透促进剂对假乳胶型透皮给药系统通过小鼠和人尸体皮肤的硫酸特布他林的皮肤渗透动力学的影响

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摘要

The purpose of this research was to prepare a pseudolatex transdermal delivery system for terbutaline sulfate and to evaluate the effect of pH and organic ester penetration enhancers on permeation kinetics of terbutaline sulfate through mice abdominal skin and human cadaver skin. An increase in the permeation flux by increasing pH was observed. The distribution coefficient of terbutaline sulfate between 1-octanol and buffers of different pH values was also pH-dependent. Furthermore, the change of the permeability coefficient with pH correlated well with the distribution coefficient by a 2-degree polynomial equation. The permeation profile and related kinetic parameters of terbutaline sulfate was determined in presence of 3 estertype permeation enhancers incorporated in the films, viz methyl laureate, isopropyl lanolate, and isopropyl myristate. Among the 3, the more pronounced enhancing effect was obtained with isopropyl myristate, regarding the permeatin flux, permeability coefficient, and diffusion coefficient. This was attributed to solubility parameter of isopropyl myristate being closer to the solubility parameter of human skin, and such a pronounced enhancing effect was probably caused by its passage across the skin barrier through the lipid pathway.
机译：这项研究的目的是为硫酸特布他林制备一种伪乳胶透皮递送系统，并评估pH和有机酯渗透促进剂对硫酸特布他林通过小鼠腹部皮肤和人尸体皮肤渗透动力学的影响。观察到通过增加pH值可以增加渗透通量。硫酸特布他林在1-辛醇和不同pH值的缓冲液之间的分配系数也与pH有关。此外，通过2多项式方程，渗透系数随pH的变化与分布系数密切相关。在存在于膜中的3种酯型渗透增强剂，即月桂酸甲酯，月桂酸异丙酯和肉豆蔻酸异丙酯的存在下，测定硫酸特布他林的渗透曲线和相关的动力学参数。在三者中，肉豆蔻酸异丙酯在渗透素通量，渗透系数和扩散系数方面获得了更明显的增强效果。这归因于肉豆蔻酸异丙酯的溶解度参数更接近人皮肤的溶解度参数，并且这种显着的增强作用可能是由于其穿过脂质屏障穿过皮肤屏障而引起的。

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