活血止痛膏体外经皮渗透成分的确定与研究

Determination and Study of Transdermal Permeable Components of Huoxue Zhitong Ointment in Vitro

目的:建立透皮接收液中丁香酚、丹皮酚及水杨酸甲酯的含量测定方法并对活血止痛膏体外经皮渗透成分进行确定与研究。方法:采用Franz扩散池法考察活血止痛膏体外透皮成分及规律;利用UPLC及气相色谱法确定透皮成分,测定透皮接收液中丁香酚、丹皮酚及水杨酸甲酯的透过量;以24 h透过成分的累积透过量、测定成分经皮渗透量平行性及皮肤组织微观结构为指标,比较四种不同的透皮接收液,对接收液进行优选。结果与结论:活血止痛膏中可经皮渗透成分为丹皮酚、丁香酚及水杨酸甲酯;丁香酚、丹皮酚及水杨酸甲酯的累积透过量均较乙醇-0.9%NaCl注射液3∶7、聚乙二醇-0.9%NaCl注射液2∶8作为接收液高,有效成分经皮渗透量平行性及实验皮肤组织微观结构较乙醇-丙二醇-0.9%NaCl注射液(2∶2∶6)作为接收液好,因此选定乙醇-聚乙二醇-0.9%NaCl注射液(2∶2∶6)作为透皮接收液。

Objective:To establish a method for the determination of eugenol, paeonol and methyl salicylate in transdermal receiving fluid, and to determine and study the in vitro transdermal permeable components of Huoxue Zhitong ointment. Methods: Franz diffusion cell method was used to investigate the transdermal components and regularity of Huoxue Zhitong ointment in vitro. The transdermal components were determined by UPLC and gas chromatography, and the transdermal transmittance of eugenol, paeonol and methyl salicylate in the transdermal receiving fluid was determined. Four different transdermal receiving solutions were compared according to the cumulative transmittance of the components in 24 hours, the parallelism of the measured components and the microstructure of the skin tissue. Results & Conclusion: The transdermal components of Huoxue Zhitong ointment are paeonol, eugenol and methyl salicylate. The cumulative permeability of eugenol, paeonol and methyl salicylate is higher than that of ethanol 0.9% NaCl solution 3∶7, polyethylene glycol 0.9% NaCl solution 2∶8 and as the receiving solution. The parallelism of the percutaneous permeability of effective components and the microstructure of experimental skin tissue are better than that of ethanol propylene glycol 0.9% NaCl solution(2∶2∶6). Therefore, ethanol polyethylene glycol 0.9% NaCl solution(2∶2∶6) is selected as the receiving solution.