促渗剂对白头翁素体外经皮渗透的影响Influence of permeation enhancers on transdermal permeation of anemonin
宁玉明;饶跃峰;梁文权;
NING Yu-ming1,2,RAO Yue-feng1,LIANG Wen-quan1(1.School of Pharmaceutical Sciences,Zhejiang University,Hangzhou 310031,China;2.Fuyang Women and Children Hospital,Fuyang 311400,China)
摘要(Abstract):
目的:考察几种常用促渗剂对白头翁素体外经皮渗透性能的影响,为白头翁素经皮给药系统的开发提供参考。方法:采用TK-6A型透皮扩散仪,供应室加含不同促进剂的白头翁素样品,用人皮进行体外经皮渗透实验;以HPLC测定一定时间点接受室中药物浓度,求算累积渗透量及稳态透皮速率。结果:白头翁素饱和水溶液的稳态渗透速率为(1.17±0.03)μg.cm-2.h-1,含30%、50%乙醇和3%月桂氮酮-5%聚山梨酯20、30%乙醇-3%月桂氮酮-5%聚山梨酯20的白头翁素溶液稳态渗透速率为(9.30±0.32),(18.56±0.58),(7.29±0.35),(13.77±0.16)μg.cm-2.h-1,分别使白头翁素的经皮渗透速率提高了7.9,15.9,6.2,11.8倍。结论:乙醇和月桂氮酮能显著促进白头翁素的经皮渗透,白头翁素有望开发成经皮给药制剂。
Objective: To investigate the effect of different permeation enhancer on transdermal permeation of anemonin through human skin.Method: The permeation experiments were performed using human skin on modified Franz diffusion cells in vitro.The concentrations of anemonin in receptor compartment at specified time points were determined by HPLC.The steady flux and the cumulative quantity of anemonin through skin were calculated.Result: The flux of anemonin permeating through human skin from 30% ethanol,50% ethanol solution and a combination of 3 % laurocapm-5% polysorbate 20 and 30 % ethanol-3 % laurocapm-5% polysorbate 20 of anemonin was(9.30±0.32),(18.56±0.58),(7.29±0.35),(13.77±0.16) μg·cm-2·h-1 and 7.9,15.9,6.2,11.8 times higher than from saturated water solution respectively.Conclusion: Ethanol and laurocapm can remarkably improve the transdermal permeation of anemonin and the anemonin have the potential to be developed to new transdermal preparation.
关键词(KeyWords):
白头翁素;透皮吸收;促渗剂;乙醇;月桂氮酮
anemonin;transdermal permeation;permeation enhancer;ethanol;laurocapm
基金项目(Foundation):
作者(Authors):
宁玉明;饶跃峰;梁文权;
NING Yu-ming1,2,RAO Yue-feng1,LIANG Wen-quan1(1.School of Pharmaceutical Sciences,Zhejiang University,Hangzhou 310031,China;2.Fuyang Women and Children Hospital,Fuyang 311400,China)
参考文献(References):
- [1]吕丹.威灵仙的药学研究[J].海峡药学,1999,11(4):7.
- [2]柯铭清.中草药有效成分理化与药理特性[M].修订本.长沙:湖南科学技术出版社,1982:7.
- [3]国家医药管理局中草药情报中心站.植物药有效成分手册[M].北京:人民卫生出版社,1994:1407.
- [4]NIAID-Division of AIDS[DB/OL].http://apps1.niaid.nih.gov/struct_search/all/url_search.asp?aids_no=012179.
- [5]Rathbone M J,Hadgraft J,Roberts M S.Modified-release drugdelivery technology[M].New York:Marcel Dekker,2003:488.
- [6]Janoff A S.Liposomes rational design[M].New York:MarcelDekker,1999:292.
- [7]陆彬.药物新剂型和新技术[M].2版.北京:人民卫生出版社,2005:353.
- 宁玉明
- 饶跃峰
- 梁文权
NING Yu-ming1- 2
- RAO Yue-feng1
- LIANG Wen-quan1(1.School of Pharmaceutical Sciences
- Zhejiang University
- Hangzhou 310031
- China
- 2.Fuyang Women and Children Hospital
- Fuyang 311400
- China)
- 宁玉明
- 饶跃峰
- 梁文权
NING Yu-ming1- 2
- RAO Yue-feng1
- LIANG Wen-quan1(1.School of Pharmaceutical Sciences
- Zhejiang University
- Hangzhou 310031
- China
- 2.Fuyang Women and Children Hospital
- Fuyang 311400
- China)