在体单向灌流法研究ZYS-01的大鼠肠吸收特性
发布时间：2019-05-24 03:08
【摘要】：目的研究ZYS-01在大鼠小肠各段的吸收特性,并对其吸收机制进行探讨。方法建立大鼠在体单向肠灌流模型,通过HPLC测定肠灌流液中ZYS-01的浓度,采用重量法对灌流液体积进行校正,考察不同剂量组的ZYS-01在十二指肠、空肠、回肠的吸收情况,以及P-糖蛋白(P-gp)抑制剂对ZYS-01吸收的影响。结果 ZYS-01为全小肠段吸收的药物,其吸收速率与肠段部位和灌流液浓度有关,全肠段Peff值均大于0.2×10~(-4)cm·s~(-1)。P-gp抑制剂的加入可显著提高ZYS-01在不同小肠段的吸收。结论 ZYS-01为高渗透性药物,在小肠全段均有吸收,其吸收速率最快的部位是十二指肠;在低浓度时吸收速率最快,并有随浓度增加而降低的趋势;ZYS-01吸收机制可能为主动转运;ZYS-01可能是Pgp的底物。
[Abstract]:Objective to study the absorption characteristics of ZYS-01 in each segment of rat small intestine and to explore its absorption mechanism. Methods the rat model of in vivo single intestinal perfusion was established. The concentration of ZYS-01 in intestinal perfusion fluid was determined by HPLC. The volume of perfusion solution was corrected by gravimetric method. The absorption of ZYS-01 in duodenum, Jejunum and ileum in different dose groups was investigated. And the effect of P-glycoprotein (P-gp) inhibitor on ZYS-01 absorption. Results ZYS-01 was a drug absorbed by whole intestinal segment, and its absorption rate was related to the location of intestinal segment and the concentration of perfusion solution. The Peffvalue of whole intestinal segment was more than 0.2 脳 10 ~ (- 4) cm 路s ~ (- 1). The addition of P-gp inhibitor could significantly increase the absorption of ZYS-01 in different intestinal segments. Conclusion ZYS-01 is a highly permeable drug, which is absorbed in the whole small intestine, and the fastest absorption rate is in the duodenum, and the absorption rate is the fastest at low concentration and tends to decrease with the increase of concentration. The absorption mechanism of ZYS-01 may be active transport, and ZYS-01 may be the substrate of Pgp.
【作者单位】： 天津中医药大学;中国中医科学院中药研究所;
【分类号】：R965
[Abstract]:Objective to study the absorption characteristics of ZYS-01 in each segment of rat small intestine and to explore its absorption mechanism. Methods the rat model of in vivo single intestinal perfusion was established. The concentration of ZYS-01 in intestinal perfusion fluid was determined by HPLC. The volume of perfusion solution was corrected by gravimetric method. The absorption of ZYS-01 in duodenum, Jejunum and ileum in different dose groups was investigated. And the effect of P-glycoprotein (P-gp) inhibitor on ZYS-01 absorption. Results ZYS-01 was a drug absorbed by whole intestinal segment, and its absorption rate was related to the location of intestinal segment and the concentration of perfusion solution. The Peffvalue of whole intestinal segment was more than 0.2 脳 10 ~ (- 4) cm 路s ~ (- 1). The addition of P-gp inhibitor could significantly increase the absorption of ZYS-01 in different intestinal segments. Conclusion ZYS-01 is a highly permeable drug, which is absorbed in the whole small intestine, and the fastest absorption rate is in the duodenum, and the absorption rate is the fastest at low concentration and tends to decrease with the increase of concentration. The absorption mechanism of ZYS-01 may be active transport, and ZYS-01 may be the substrate of Pgp.
【作者单位】： 天津中医药大学;中国中医科学院中药研究所;
【分类号】：R965
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