摘要
目的:探讨天然冰片(艾片)、合成冰片对栀子提取物黏膜促渗作用并进行比较。方法:以离体蛙皮为模型进行体外黏膜渗透试验,研究艾片、合成冰片对栀子提取物指标成分栀子苷表观渗透系数Papp的影响,考察艾片及合成冰片对栀子苷稳定性影响,比较各组10 h累积渗透率。以效应面法研究提取物浓度、艾片浓度及渗透转速对Papp的影响。结果:艾片组和合成冰片组的Papp分别是对照组的1.44,1.77倍,均具有极显著性差异(P<0.01),两促渗组间也具有显著性差异(P<0.05)。在蛙皮作用下,对照组和合成冰片组栀子苷8 h左右开始降解,艾片组12 h内未发生降解。艾片组及合成冰片组10 h累计渗透率相当,约为对照组1.3倍。效应面试验设计结果表明,艾片浓度对Papp具有极显著性影响(P<0.01),渗透转速则对渗透时滞(time-lag)作用明显(P<0.01)。结论:艾片和合成冰片均能促进栀子苷的渗透,合成冰片的促渗作用更强。艾片及合成冰片均能降低蛙皮对栀子苷降解作用,艾片的保护作用更佳。艾片对黏膜屏障的作用较合成冰片弱,但保护作用更强,使用较高浓度的艾片可以提高栀子提取物的黏膜吸收,降低时滞,同时保护栀子苷不易被生物内源性物质破坏。
Objective： To observe the influence of natural borneol and synthetic borneol on mucosal permeability of Gardenia extract. Method： Taken frog skin as a vitro model to study the vitro mucosal permeation the impacts of the natural borneols and synthetic borneols on the Papp of the Jasminoidin were studied, and the effect of different borneols on the stability of Jasminoidin were investigated. Compared the 10 h accumulated infiltration rate of each group the effects of influence factors, such as CGe , CR and rotation speed on Papp were investigated by using response surface method. Result： The Papp, of Jasminoidin of natural borneol and synthetic borneol group were 1.44 fold and 1.77 fold of control group （P 〈 0.01 ）. For two borneol groups, the results also showed a significant difference too （ P 〈 0. 05 ）. Jasminoidin began to degrade about 8 h after the effect of frog skin for control group and synthetic borneol group, but was stable within 12 h for natural borneol group. The accumulated permeation rate of 10 h was same for different borneol groups, It was about 1.3 fold of control group. The CGe had a salinence influence on the Papp （ P 〈 0. 01 ） and CR had a salience influence on time-lag （P 〈 0. O1 ）. Conclusion： Both the natural borneol and synthetic borneol can accelerate the permeation of Jasminoidin and the synthetic horneol has stronger effect on the Papp. Both two different borneol can reduce the degradation effect of frog skin to Jasminoidin, hut the natural borneol has a better protect effect on it. By using more natural borneol, the mucosal permeability of Gardenia extract can be increased, the time-lag can be reduced, and Jasminoidin has better stability.
出处
《中国中药杂志》
CAS
CSCD
北大核心
2009年第10期1207-1210,共4页
China Journal of Chinese Materia Medica
基金
国家"十一五"科技支撑计划(2006BA106A17)
关键词
天然冰片
合成冰片
栀子提取物
黏膜渗透
稳定性
natural borneol
synthetic borneol
gardenia extract
mucosal permeability
stability
作者简介
陆洋，在读博士，主要从事中药经鼻给药系统研究，E—mail：landocean28@163．com.
[通信作者]杜守颖，博士，教授，博士生导师。研究方向：中药新剂型与新技术。Tel：（010）84738645．E-mail：dushouying@263．net
