中药肠吸收动力学的研究——灯盏花素肠吸收动力学的研究

【作者】 唐灿；

【导师】 王一涛； 杨奎；

【作者基本信息】 成都中医药大学 ， 中药学， 2004， 博士

【摘要】 本研究首次运用外翻肠囊法、在体肠循环灌流法和Caco-2细胞模型法研究了灯盏花素的肠吸收动力学。 外翻肠囊法研究结果表明，灯盏花素在肠道的吸收方式属于被动扩散吸收，最大吸收率从13.1％～16.9％。 在体肠循环灌流法研究结果表明，灯盏花素在肠道的吸收方式同样属于被动扩散吸收，最大吸收率从15.14％～16.38％，吸收速率常数0.0329～0.0358h^-1，每小时吸收分数为0.0507～0.0546，表观扩散系数为1.137×10^-7～1.240×10^-7，吸收半衰期为19.45h～21.70h，肠道菌群对吸收无影响。 Caco-2细胞模型法研究结果表明，灯盏花素跨肠上皮细胞的运动属被动扩散，最大扩散率从16.78％～17.11％，扩散速率常数0.04～0.042h^-1，每小时扩散分数为0.0833～0.0856，表观扩散系数为23.59×10^-7～24.76×10^-7，扩散半衰期为16.5h～17.33h，排泌试验显示灯盏花素无逆向排泌现象。 结果显示，三种实验方法具有良好的相关性，灯盏花素在肠道的吸收方式属被动扩散吸收，吸收半衰期长，吸收较差。结合文献研究表明灯盏花素的体内过程相对复杂。肠吸收动力学研究为深入研究其体内过程及新的口服给药系统提供了研究思路。更多还原

【Abstract】 This reserch was studied on the Breviscapine intestinal absorption dynamics first-time with 3 methods : everted sac technique, body circulatory perfusion technique and Caco-2 cell method.The result of everted sac technique test showed the way of Breviscapine intestinal absorbtion is passive transport mechanism and maximum absorptivity varied from 13.1% to 16.9%.The result of body circulatory perfusion technique test showed the same absorption mechanism with Breviscapine .Maximum absorptivity varied from 15.41% to 16.38%, the absorption Ka was 0.0329~0.0358h-1,absorption-fraction per hour was0.0507~0.0546,Papp was 1.137x10-7~1.240x10-7, absorption t1/2 was 19.45h~21.70h and with no influence on intestinal bacterial flora.The result of Caco-2 cellular model manifested the transenterocyte movement of Breviscapine was passive diffusion,maximum diffusibility changed from 16.78% to 17.11%, diffusion -fraction per hour was 0.0833-0.0856, diffusion Ka was 23.59 x 10-7~24.76 x 10-7,diffusion t1/2 was 16.5h~17.33h.. Efflux test demonstrated no adverse efflux.Those results showed there were satisfied correlation among the three experiment tests. The absorption mechanism of Breviscapine was passive diffusion, characterized by long absorption t1/2 and poor absorption. Relative documents and reserches illustrated complicated process in vivo of Breviscapine. Intestinal absorption dynamics provided a method for profound study on the process in vivo and new oral druges development.更多还原