焦谷氨酸油醇酯作为经皮渗透促进剂及其促渗机理  

Oleyl pyroglutamate for use as transdermal enhancer and its enhancing mechanism

作　　者：成志毅[1] 陈浩凡[1] 

机构地区：[1]中山大学药学院,广东广州510080

出　　处：《药学学报》2003年第5期384-387,共4页Acta Pharmaceutica Sinica

摘　　要：目的　研究焦谷氨酸油醇酯作为经皮渗透促进剂 ,试验其促渗活性和促渗机理。方法　考察焦谷氨酸油醇酯、油醇和油酸对咖啡因、替硝唑和醋酸可的松经皮渗透促渗效果 ;通过衰减全反射 傅立叶变换红外光谱 (ATR FTIR)法分析焦谷氨酸油醇酯的促渗机理。结果　焦谷氨酸油醇酯使 3种不同类型药物经皮渗透的累积渗透量有明显提高 ,增渗倍数分别为 7 9,41 8和 2 8。作用后的人体皮肤ATR FTIR谱图上 2 80 0～ 2 950cm-1 和酰胺I吸收峰随角质层的逐步剥离出现不同的位移变化。结论　焦谷氨酸油醇酯对药物有较好的促渗效果 ,其促渗机理除了使角质层中的脂质变得无序外可能还使角质蛋白的二级结构发生改变。Aim To test the enhancing activity and the mechanism of oleyl pyroglutamate used as transdermal enhancer. Methods The penetration enhancing effects of oleyl pyroglutamate, oleyl alcohol and oleic acid on the three drugs (caffeine, tinidazole and cortisone) were observed; the transdermal enhancing mechanism of oleyl pyroglutamate was studied with the attenuated total reflectance Fourier transfer infrared spectroscopy(ATR FTIR) of the human stratum corneum in vivo . Results The penetration enhancing...

关 键 词：经皮给药系统 经皮渗透促进剂 促渗透机理 焦谷氨酸油醇酯 

分 类 号：R94[医药卫生—药剂学]