Lu Yang, Du Shouying, Yao Zongling, Zhai Yongsong
School of Chinese Pharmacy, Beijing University of Chinese Medicine, Beijing 100102, China.
Zhongguo Zhong Yao Za Zhi. 2009 Feb;34(3):272-4.
To study the factors that affect mucosal absorption of gardenia extract.
Take vitro frog skin as a model to study the vitro mucosal permeation. The impacts of the osmotic pressure and the pH value of permeation medium on the Papp of the Jasminoidin were studied, and the effect of frog skin on the stability of Jasminoidin was investigated also.
The Papp of Jasminoidin were (0.53 +/- 0.01), (0.21 +/- 0.05), (0.44 +/- 0.12), (0.42 +/- 0.13), (0.26 +/- 0.03) cm x min(-1) by using the normal saline (pH 6.88), pure water, 1.8 % NaCl solution, normal saline (pH 4.05) and normal saline (pH 10.05) as permeation medium for each. The accumulated permeation rate was (55.69 +/- 9.81)% by 12 h, using normal saline as permeation medium respectively, and there was no obvious time lag. Jasminoidin began to degrade around 8 h by affectedof frog skin, the constant of degradation rate (K) was 1.999, and the t1/2 was 0.347 h.
The mucosal permeability of gardenia extract by using the vitro model of frog skin is good, and consistent with zero level absorption process. The osmotic pressure and pH value significantly affected the permeation and the isotonic and partial neutral permeation medium are more conducive to the permeation and absorption of Jasminoidin. The degradation effect of frog skin to the Jasminoidin will not affect mucosal permeation research. In vitro model of frog skin is a suitable way to simulate mucosal permeation process of the gardenia extract.
研究影响栀子提取物黏膜吸收的因素。
以离体蛙皮为模型研究体外黏膜渗透。考察渗透介质的渗透压和pH值对栀子苷表观渗透系数(Papp)的影响,同时研究蛙皮对栀子苷稳定性的影响。
分别以生理盐水(pH 6.88)、纯水、1.8%氯化钠溶液、生理盐水(pH 4.05)和生理盐水(pH 10.05)为渗透介质时,栀子苷的Papp分别为(0.53±0.01)、(0.21±0.05)、(0.44±0.12)、(0.42±0.13)、(0.26±0.03)cm·min⁻¹。以生理盐水为渗透介质时,12 h累积渗透率为(55.69±9.81)%,且无明显时滞。栀子苷受蛙皮影响约8 h开始降解,降解速率常数(K)为1.999,半衰期(t1/2)为0.347 h。
采用离体蛙皮模型,栀子提取物的黏膜透过性良好,符合零级吸收过程。渗透压和pH值显著影响渗透,等渗且偏中性的渗透介质更有利于栀子苷的渗透和吸收。蛙皮对栀子苷的降解作用不影响黏膜渗透研究。离体蛙皮模型是模拟栀子提取物黏膜渗透过程的适宜方法。