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目的应用乙醇(E)-肉豆蔻酸异丙酯(IPM)2组分溶液系统,研究在EI系统中有机胺对酮洛芬(KP)的经皮渗透的影响,初步探讨其作用机理。方法用水平扩散池,以离体大鼠皮肤作为渗透屏障进行体外渗透实验。用HPLC测定样品中KP浓度。结果除二乙胺(DEtA)和三乙胺外,当EI系统[m(乙醇)∶m(肉豆蔻酸异丙酯)=90∶10]中加入乙醇胺、二乙醇胺、三乙醇胺、和N-(2-羟乙基)吡啶时,KP在溶液系统中溶解度均略有降低。所有加入有机胺的EI溶液系统均对KP产生明显的渗透促进作用。此外,在DEtA-EI系统中,KP的流量与DEtA的浓度成正比,而E的渗透流量恒定,与KP流量变化无关。结论结果表明,EI系统中有机胺对KP的经皮渗透有促进作用。这种渗透促进作用可能依赖于KP与胺之间所形成的离子对组成。
Objective To study the effect of organic amines on the transdermal permeation of ketoprofen (KP) in EI system by using the solution system of ethanol (E) -isopropyl myristate (IPM) 2 components and to explore its mechanism. Methods In vitro diffusion experiments were performed with a horizontal diffusion cell using the isolated rat skin as an osmotic barrier. The KP concentration in the sample was measured by HPLC. Results Ethanolamine, diethanolamine, triethanolamine, and N- (2-hydroxyethyl) amine were added to the EI system [m (ethanol): m (isopropyl myristate) = 90:10] except diethylamine (DEtA) and triethylamine. (2-hydroxyethyl) pyridine, KP solubility in the solution system were slightly lower. All of the EI-added organic amine systems gave a significant permeation-promoting effect on KP. In addition, in the DEtA-EI system, the KP flow rate is proportional to the DEtA concentration, while the E permeate flow rate is constant, independent of the KP flow rate change. Conclusion The results show that the organic amine in EI system can promote the transdermal penetration of KP. This penetration enhancement may depend on the composition of the ion pairs formed between KP and the amine.