共轭亚油酸及其乙酯的体外透皮实验研究

An Experimental Study on in Vitro Percutaneous Absorption of Conjugated Linoleic Acid and Its Ethyl Ester

目的:考察共轭亚油酸及其乙酯的体外透皮和皮肤摄取特性。方法:通过气相色谱-质谱法分析共轭亚油酸及其乙酯试样的成分;用紫外分光光度法确定测定波长为233nm,并且制备标准曲线;选择30%乙醇溶液作为接受液,采用改进的Franz透皮扩散仪对用试样配制的各扩散液进行裸鼠皮肤体外渗透实验。结果:共轭亚油酸及其乙酯在各扩散介质中于10小时内可导致显著的皮内摄取,并且共轭亚油酸的皮内摄取量大于其乙酯;以丙二醇作溶剂,共轭亚油酸可以透过皮肤,而其乙酯几乎无透过;氮酮能抑制共轭亚油酸的透皮吸收,但可促进其皮内摄取。以2%共轭亚油酸或其乙酯软膏作为扩散物,至3小时便几乎致皮内摄取达饱和,且24小时内共轭亚油酸的皮内摄取量小于其乙酯。结论:共轭亚油酸及其乙酯可用于局部制剂。

Objective： To investigate the in vitro percutaneous absorption and skin-intake of conjugated linoleic acid（CLA） and its ethyl ester（ CLAE）. Methods： The components of CLA and CLAE samples were analyzed by GC-MS, detecting wavelength of 233 nm was confirmed by UV, where the standard curve was prepared, 30% alcohol solution was used as receiving solution and an improved Franz diffusion cell was adopted to test the in vitro permeability of CLA and CLAE solutions through nude mouse skin. Results： After l0 h the skin-intakes of CLA and CLAE in varied diffusion mediums were obvious, and the intake of CLA was more than that of CLAE under the same conditions. When PG used as diffusion medium, a few CLA permeated the skin, but CLAE had hardly permeation. Azone restrained the permeation of CLA while enhanced the skin- intake of CLA. The skin-intakes of the 2%CLA and 2%CLAE oinmaents almost reached saturation in 3 h and the skin-intake of CLA in 24 h was less than that of CLAE. Conclusion： It is suggested that CLA and CLAE could be used for topical preparations.