论文部分内容阅读
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 the solubility of dehydro-silybin (DHS) and investigate the absorption kinetics of DHS in the small intestine. Methods: The content of DHS was determined by HPLC. The mobile phase consisted of methanol-0.2% formic acid solution (60:40) and the detection wavelength was 255 nm. The absorption characteristics of DHS in the duodenum, jejunum and ileum of rats were investigated using the rat model of intestinal circulation. Results: The solubility of DHS at 20 and 37 ℃ for 24 h were 0.46 and 1.23 mg · L -1, respectively. The absorption rate of DHS in duodenum, jejunum and ileum were (17.81 ± 6.37)%, (8.41 ± 2.43)%, (12.95 ± 5.06)%, and the absorption rate The values of K a were (0.176 ± 0.069), (0.089 ± 0.053) and (0.158 ± 0.058) h-1, respectively. The K a of DHS in the duodenum remained unchanged with the increase of drug concentration. Conclusion: The temperature has some influence on the solubility of DHS. DHS in the duodenum, jejunum, ileum are absorbed in the duodenum section absorption and K a significantly higher than the jejunum segment. The absorption mechanism of DHS in the small intestine is mainly passive diffusion.