【摘要】：目的研究ZYS-01在大鼠小腸各段的吸收特性,并對(duì)其吸收機(jī)制進(jìn)行探討。方法建立大鼠在體單向腸灌流模型,通過(guò)HPLC測(cè)定腸灌流液中ZYS-01的濃度,采用重量法對(duì)灌流液體積進(jìn)行校正,考察不同劑量組的ZYS-01在十二指腸、空腸、回腸的吸收情況,以及P-糖蛋白(P-gp)抑制劑對(duì)ZYS-01吸收的影響。結(jié)果 ZYS-01為全小腸段吸收的藥物,其吸收速率與腸段部位和灌流液濃度有關(guān),全腸段Peff值均大于0.2×10~(-4)cm·s~(-1)。P-gp抑制劑的加入可顯著提高ZYS-01在不同小腸段的吸收。結(jié)論 ZYS-01為高滲透性藥物,在小腸全段均有吸收,其吸收速率最快的部位是十二指腸;在低濃度時(shí)吸收速率最快,并有隨濃度增加而降低的趨勢(shì);ZYS-01吸收機(jī)制可能為主動(dòng)轉(zhuǎn)運(yùn);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.
【作者單位】： 天津中醫(yī)藥大學(xué);中國(guó)中醫(yī)科學(xué)院中藥研究所;
【分類號(hào)】：R965

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