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研究双环单萜促透剂(冰片与樟脑)对川芎嗪透皮吸收的影响及其作用机制。分别采用傅里叶红外光谱法、扫描电镜法和体外透皮动力学法研究促透剂对角质层的生物物理变化、猪皮表面的变化及川芎嗪体外透过量的影响,并采用表观密度评价角质鳞片脱落的程度。红外光谱结果表明,以冰片为促透剂使角质层脂质中的对称与不对称峰的峰位移及峰面积降低值均高于樟脑;扫描电镜结果表明,角质层的形态学变化与采用的促透剂有关,冰片与樟脑对角质层脂质的抽提作用导致角质层的破裂及角质鳞片的脱落;川芎嗪的体外透过量结果显示,以冰片为促透剂的透过量大于樟脑。双环单萜促透剂对川芎嗪的促透机制包括对脂质的抽提和扰动作用,这些作用与C-H伸缩震动的位移变化及促透剂与神经酰胺的氢键作用相关;双环单萜促透剂(冰片与樟脑)中羟基的促透能力较酮基的促透能力强。
To study the effect of bicyclic monoterpene enhancer (borneol and camphor) on transdermal absorption of ligustrazine and its mechanism. The effects of enhancing agent on the biophysical changes of stratum corneum, the surface changes of pigskin and the in vitro permeation of ligustrazine were studied respectively by Fourier transform infrared spectroscopy, scanning electron microscopy and in vitro transdermal kinetics. The apparent density Evaluation of keratin flake shedding extent. Infrared spectroscopy results showed that with the borneol as a penetration enhancer, the peak shift and peak area reduction of the symmetrical and asymmetric peaks in the stratum corneum lipid were higher than that of the camphor. The scanning electron microscopy results showed that the morphological changes of the stratum corneum and the Increasing agent, borneol and camphor extract of the stratum corneum lead to the breakdown of the stratum corneum and sclera scales shed; in vitro transmission of ligustrazine results show that the borneol penetration enhancer penetration greater than camphor. The mechanism of promoting the permeation of tetramethylpyrazine by bicyclic monoterpene enhancer includes the extraction and perturbation of lipids, which are related to the change of the displacement of CH stretching vibration and the hydrogen bonding effect between enhancer and ceramide. Permeability of the hydroxyl groups in the penetrating agents (borneol and camphor) is stronger than that of the keto group.