吴争;高建青;陈海靓;胡英;梁文权;
WU Zheng1,GAO Jian-qing1,CHEN Hai-liang1,HU Ying1,2,LIANG Wen-quan(1.Institute of pharmaceutics,Zhe jiang University,Hangzhou 310058,China;2.Zhejiang Pharmaceutical College,Ningbo 315100,China)

• 1:浙江大学药学院生物技术药物制剂研究所
• 2:浙江大学药学院生物技术药物制剂研究所
• 3:浙江大学药学院生物技术药物制剂研究所
• 4:浙江大学药学院生物技术药物制剂研究所

摘要(Abstract)：

目的:制备α-细辛醚储库型贴片,考察其体外释药特性和离体皮肤经皮渗透性,筛选有效的透皮吸收促进剂,提高α-细辛醚的透皮吸收速率。方法:以1%的HPMC的醇性溶液为储库介质,以EVA膜为控释膜,制备α-细辛醚的储库型透皮贴片。用改良Franz扩散池进行人离体皮肤渗透实验,筛选透皮吸收促进剂,用HPLC测定α-细辛醚的含量并计算其透皮速率。结果:α-细辛醚的释放速率接近零级。30%乙醇和1%肉豆蔻酸异丙酯协同对α-细辛醚贴片的促渗效果最佳,透皮速率达到(20.67±1.33)μg.cm-2.h-1。结论:含乙醇和肉豆蔻酸异丙酯的α-细辛醚储库型贴片有较好的经皮渗透速率,可满足临床治疗要求。
Objective: To prepare the α-asarone reservoir patch and investigate its release and transdermal absorption characteristics in vitro.The efficient enhancers were chosen to improve the drug's permeation rate.Method: The α-asarone reservoir patch was prepared using 1%hydroxypropyl methylcellulose(HPMC) of ethanol solution as medium and ethylene vinyl acetate(EVA) membrane to control the release of drug.The Franz diffusion cel1s were used and several permeation enhancers were evaluated.High performance liquid chromatorgraphy(HPLC) was used to determine α-asarone's content and permeation rate.Result: The release mechanisms of α K-asarone patch in vitro coincided with zero-order kinetic.30% ethanol cooperates with 1% Isopropyl Myristate(IPM) have the best effect on permeation of the patch.The permeation rate reaches(20.67±1.33) μg·cm-2·h-1.Conclusion: Ethanol combined with IPM is good permeation enhancer,which facilitated the permeation of α K-asarone to fit the clinical requirements.However,the further studies of the skin's stimulation and bioavailability are needed.

关键词(KeyWords)： α-细辛醚;经皮渗透;促渗剂;储库型;贴片;HPLC
α-asarone;transdermal;permeation enhancers;reservoir;patch;HPLC

Abstract:

Keywords:

基金项目(Foundation):

作者(Authors): 吴争;高建青;陈海靓;胡英;梁文权;
WU Zheng1,GAO Jian-qing1,CHEN Hai-liang1,HU Ying1,2,LIANG Wen-quan(1.Institute of pharmaceutics,Zhe jiang University,Hangzhou 310058,China;2.Zhejiang Pharmaceutical College,Ningbo 315100,China)

参考文献(References)：

• [1]刘宇,王东凯.α-细辛脑-β-环糊精包合物的制备及体外溶出度测定[J].中国药剂学杂志,2003,1(4):150.
• [2]刘立东,凌树森.α-细辛醚透皮吸收研究[J].中国药房,1994,5(3):12.
• [3]柯雪红,方永奇.RP-HPLC测定石菖蒲、水菖蒲药材中β-细辛醚、α-细辛醚的含量[J].中国中药杂志,2004,29(3):279.
• [4]马福家.双氯芬酸钾HPMC骨架片体外释药影响因素研究[J].上海医药,2005,26(6):271.
• [5]MK Kim,HZhao,CHLee,et al.Formulation of a reservoir-typetestosterone transdermal delivery system[J].Int J Pharm,2001,219(1-2):51.
• [6]姜晓虹,金一.倍他米松骨架型缓释贴片的处方筛选[J].中国医药工业杂志,2003,34(8):393.
• [7]李国锋,权英淑.皮肤不同层对脂溶性药物经皮渗透的影响[J].中国药学杂志,2002,37(11):833.
• [8]陆彬.药物新剂型和新技术[M].北京:人民卫生出版社,2003:302.