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[活血止痛贴中有效成分的透皮渗透]

[Transdermal permeation of effective components in Huoxue Zhitong patch].

作者信息

Yang Chang, Du Shou-Ying, Bai Jie, Li Peng-Yue, Cui Ya-Hua, Yang Bing

机构信息

Beijing University of Chinese Medicine, Beijing 100102, China.

出版信息

Zhongguo Zhong Yao Za Zhi. 2017 Apr;42(8):1597-1602. doi: 10.19540/j.cnki.cjcmm.20170224.020.

Abstract

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•cm⁻² respectively in Huoxue Zhitong patch and the penetration rate was 0.18, 1.22, and 0.02 μg•cm⁻²•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.

摘要

建立受体液中丹皮酚、丁香酚和胡椒碱含量的测定方法,并研究活血止痛贴的透皮渗透性。采用高效液相色谱法(HPLC)测定受体液中丹皮酚、丁香酚和胡椒碱的含量;以24小时内累积渗透量、经皮渗透速率和皮肤刺激性为指标对受体液进行优化。应用体外Franz扩散实验评价活血止痛贴的经皮渗透特性和规律。结果表明,以聚乙二醇400 - 乙醇 - 生理盐水3∶3∶4为受体液时的累积渗透量和渗透速率高于以丙二醇∶乙醇∶生理盐水3∶3∶4和乙醇 - 生理盐水3∶7为受体液时,且聚乙二醇400 - 乙醇 - 生理盐水3∶3∶4对皮肤的刺激性小于丙二醇∶乙醇∶生理盐水3∶3∶4。经皮渗透实验结果显示,活血止痛贴中丹皮酚、丁香酚和胡椒碱24小时内的累积渗透量分别为2.84、19.9和0.753 μg•cm⁻²,渗透速率分别为0.18、1.22和0.02 μg•cm⁻²•h⁻¹。因此,丹皮酚、丁香酚和胡椒碱透过皮肤的过程为扩散过程,这与它们在贴剂中的含量无关。

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