脱氢水飞蓟宾的溶解度及大鼠在体肠吸收特性考察  

Investigation of Solubility of Dehydrosilybin and Its in situ Intestinal Absorption Characteristics in Rats

作　　者：许颖[1] 金雪锋[2] 童珊珊[1] 陈美[1] 徐希明[1] 

机构地区：[1]江苏大学药学院,江苏镇江212013 [2]江苏奥赛康药业股份有限公司,南京211100

出　　处：《中国实验方剂学杂志》2013年第24期165-168,共4页Chinese Journal of Experimental Traditional Medical Formulae

基　　金：国家自然科学基金项目(81202930);江苏省高校自然科学研究面上项目(12KJB350002);江苏大学高级人才科研启动基金(11JDG122)

摘　　要：目的:测定脱氢水飞蓟宾(DHS)的溶解度并探讨DHS在小肠的吸收动力学特征。方法:采用HPLC测定DHS含量,流动相甲醇-0.2%甲酸水溶液(60∶40),检测波长255 nm。应用大鼠在体肠循环模型考察DHS在大鼠十二指肠、空肠、回肠的吸收特性。结果:DHS于20,37℃振荡24 h的溶解度分别为0.46,1.23 mg·L-1。DHS在十二指肠、空肠及回肠中单位时间吸收率(n=3,x珋±s)分别为(17.81±6.37)%,(8.41±2.43)%,(12.95±5.06)%,吸收速率常数(K a)依次为(0.176±0.069),(0.089±0.053),(0.158±0.058)h-1;DHS在十二指肠的K a随药物质量浓度的增加基本保持不变。结论:温度对DHS溶解度存在一定影响。DHS在十二指肠、空肠、回肠均有吸收,在十二指肠段吸收量和K a显著高于空肠段。DHS在小肠的吸收机制以被动扩散为主。Objective： To determine solubility of dehydrosilybin（DHS） and investigate its intestinal absorption kinetics characteristics. Method： HPLC was adopted to determine solubility of DHS with mobile phase of methanol-0.2% formic acid solution（60：40） and detection wavelength of 255 nm.Absorption characteristics of DHS in duodenum,jejunum and ileum was investigated by in situ intestinal circulation model in rats. Result： Solubility of DHS were 0.46,1.23 mg·L-1 oscillated at 20,37℃ for 24 h,respectively.Absorption rate per unit time of DHS in duodenum,jejunum and ileum were （17.81±6.37）%,（8.41±2.43）%,（12.95±5.06）%,absorption rate constant（Ka）of them were （0.176±0.069）,（0.089±0.053）,（0.158±0.058） h-1,respectively;Ka of DHS in duodenum generally kept unchanged with drug concentration increased. Conclusion： Temperature had a certain influence on solubility of DHS.DHS had absorption in duodenum,jejunum and ileum,but absorption amount and Ka in duodenum were significantly higher than them in jejunum.Absorption mechanism of DHS in small intestine was based on passive diffusion.

关 键 词：脱氢水飞蓟宾 溶解度 在体肠吸收特性 高效液相色谱 酚红 

分 类 号：R945[医药卫生—微生物与生化药学]