中国中药杂志

2014, v.39(11) 2131-2135

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微透析技术基于丹皮酚前非离子体软膏的皮肤药代动力学研究
Preparation of paeonol transdermal delivery systems based on proniosomes-based ointment and its pharmacokinetics characters

江晓;刘莉;李沙沙;张斌;李雪玲;刘志刚;刘强;
JIANG Xiao;LIU Li;LI Sha-sha;ZHANG Bin;LI Xue-ling;LIU Zhi-gang;LIU Qiang;Guangzhou Xiangxue Pharmaceutical Corporation Limited;School of Traditional Chinese Medicine,Southern Medical University;

摘要(Abstract):

以大鼠为动物模型,分别给予丹皮酚前非离子体软膏及其普通软膏1 g,以生理盐水为灌流液,灌流速度为5mL·L-1,每隔20 min收集1次,共收集12 h,采用HPLC法测定丹皮酚的含量,研究丹皮酚前非离子体软膏及其普通软膏在大鼠皮下组织液及血液中药物浓度随时间的变化过程,并对其药代动力学参数进行比较分析。结果表明探针体外回收率Rin vitro为(54.80±1.50)%,体内回收率Rin vivo为(54.58±4.61)%;皮肤药代动力学结果表明丹皮酚前非离子体软膏与普通软膏相比,显著提高了药物在皮肤组织液中的浓度,起到了缓释、长效作用。血液药代动力学结果表明丹皮酚前非离子体软膏与普通软膏相比,丹皮酚较少的进入血液中,药物浓度平稳。故该研究所构建的丹皮酚前非离子体软膏有望为皮肤湿疹的治疗提供一种新的制剂。
The paeonol proniosomes ointment and ordinary ointment were administered to rats.Physiological saline served as perfused solution.The perfusion rate was 5 mL·L-1and the microdialysis samples were collected every 20 min intervals.The paeonol concentration in perfused solution was determined by HPLC.Investigation of the pharmacokinetics of paeonol proniosomes ointment and ordinary ointment by the skin-blood synchronous microdialysis coupled with HPLC is reported in this study.The results show that the recovery was(54.80 ± 1.50)% in vitro and(54.58 ± 4.61)% in vivo.The results showed that paeonol proniosomes ointment significantly raised the drug concentrations in skin more than the paeonol ordinary ointment.The paeono proniosomes ointment has less drugs into the blood as the ordinary ointments in blood,but its blood drug concentrations were steadier.The paeonol proniosomes ointment may be developed into a new preparation.

关键词(KeyWords): 丹皮酚;前非离子体;微透析;经皮给药;药代动力学
paeonol;proniosomes;microdialysis;transdermal delivery system;pharmacokinetics

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基金项目(Foundation): 广东省高校中药化妆品工程中心建设项目(GCZX-A1007);; 广州市白云区科技计划项目(2010-KZ-28);; 广州白云区科技计划重点项目(2011-KQ-17)

作者(Author): 江晓;刘莉;李沙沙;张斌;李雪玲;刘志刚;刘强;
JIANG Xiao;LIU Li;LI Sha-sha;ZHANG Bin;LI Xue-ling;LIU Zhi-gang;LIU Qiang;Guangzhou Xiangxue Pharmaceutical Corporation Limited;School of Traditional Chinese Medicine,Southern Medical University;

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