活血止痛膏有效成分经皮渗透性研究

Transdermal permeation of effective components in Huoxue Zhitong patch

建立透皮接收液中丹皮酚、丁香酚及胡椒碱的含量测定方法并对活血止痛橡胶膏剂经皮渗透性进行研究。利用HPLC测定透皮接收液中丹皮酚、丁香酚及胡椒碱的含量;以24 h累积透过量、经皮渗透速率及皮肤刺激性为指标,优选透皮接收液;采用Franz扩散池法考察活血止痛橡胶膏剂体外透皮特征及规律。结果表明,以聚乙二醇-乙醇-生理盐水3∶3∶4为透皮接收液,丹皮酚、丁香酚及胡椒碱的累积透过量和经皮渗透速率均较丙二醇-乙醇-生理盐水3∶3∶4和乙醇-生理盐水3∶7作为接收液高,皮肤刺激性较丙二醇-乙醇-生理盐水3∶3∶4作为接收液小;活血止痛橡胶膏剂中丹皮酚、丁香酚及胡椒碱24 h累积透过量分别为2.84,19.9,0.753μg·cm^(-2),三者经皮渗透速率分别为0.18,1.22,0.02μg·cm^(-2)·h^(-1)。由此,活血止痛橡胶膏剂中丹皮酚、丁香酚及胡椒碱的透皮过程与其在膏中含量无关,且这一过程为扩散过程。

To establish a determination method for the contents of paeonol, eugenol and piperine in receptor liquid and to research the transdermal permeability of Huoxue Zhitong patch.The contents of paeonol, eugenol and piperine in receptor liquid were determined by high pressure liquid chromatography（HPLC）;and the receptor liquid was optimized by taking accumulative amount penetrated within 24 hours, percutaneous permeation rate and skin irritation as indexes.In vitro Franz diffusion experiment was applied to assess the percutaneous penetration characteristics and regularity of Huoxue Zhitong patch.The results showed that the accumulative penetration amount and penetration rate by using PEG 400-ethanol-normal saline 3∶3∶4 as receptor liquid were higher than those by using propylene glycol∶ethanol∶normal saline 3∶3∶4 and ethanol-normal saline 3∶7, the and skin irritation of PEG 400-ethanol-normal saline 3∶3∶4 was smaller than propylene glycol：ethanol： normal saline 3∶3∶4.Results of percutaneous permeability experiments displayed that the accumulative amount penetrated of paeonol, eugenol and piperine within 24 hours was 2.84, 19.9, and 0.753 μg＆#183;cm-2 respectively in Huoxue Zhitong patch and the penetration rate was 0.18, 1.22, and 0.02 μg＆#183;cm-2＆#183;h-1 respectively.Thus, the permeation of paeonol, eugenol and piperine through the skin was a diffusion process, which was irrelevant to their content in patch.