Characteristics of the gastrointestinal absorption of morphine in rats.
Characteristics of the gastrointestinal absorption of morphine in rats.
复制标题
吗啡在大鼠胃肠道吸收的特点。
DOI：
10.1248/cpb.37.168
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发表时间：
1989
影响因子：
1.7
通讯作者：
H. Yoshimura
中科院分区：
文献类型：
--
作者：
T. Tan;M. Kuramoto;T. Takahashi;H. Nakamura;Y. Nakanishi;Y. Imasato;H. Yoshimura
利用大鼠胃肠道研究吗啡的吸收特性。分别通过原位环法和体外翻转囊法进行吸收和运输实验。刷状缘膜囊泡（BBMV）用于摄取实验。采用高效液相色谱 (HPLC) 结合紫外 (UV) 检测和电化学检测同时测定生物样品中的吗啡及其代谢物吗啡-3-葡萄糖醛酸 (M-3-G) 和吗啡-6-葡萄糖醛酸 (M-6-G)。在原位环法中，吗啡以空肠部位大于十二指肠部位大于回肠部位大于中肠部位大于直肠部位的顺序吸收良好，但从胃吸收较差。在每个外翻的十二指肠囊和空肠囊中，代谢抑制剂2,4-二硝基苯酚抑制吗啡从粘膜侧向浆膜侧的转运。此外，HgCl2 预处理减少了十二指肠和空肠环对吗啡的吸收。在 H+ 梯度（内部 pH 7.5 和外部 pH 5.0）存在下刺激 BBMV 对吗啡的初始摄取，并观察到过冲现象。初始吸收显示出浓度依赖性，即，它是饱和的。本研究获得的结果表明，尽管吗啡是从其他位点被动吸收的，但 H+ 梯度刺激的载体介导的运输部分参与了吗啡的十二指肠空肠吸收。
The absorption characteristics of morphine were investigated by using rat gastrointestine. Absorption and transport experiments were carried out by the in situ loop and the in vitro everted sac methods, respectively. Brush border membrane vesicles (BBMVs) were used for uptake experiments. Morphine and its metabolites, morphine-3-glucuronide (M-3-G), and morphine-6-glucuronide (M-6-G), in biological samples were simultaneously determined by high-performance liquid chromatography (HPLC) with ultraviolet (UV) detection and electrochemical detection. In the in situ loop method, morphine was well absorbed in the order of jejunal site greater than duodenal site greater than ileal site greater than middle intestinal site greater than rectal site, but it was poorly absorbed from the stomach. In each of the everted duodenal and jejunal sacs, 2,4-dinitrophenol, a metabolic inhibitor, inhibited the transport of morphine from the mucosal side to the serosal side. Further, HgCl2 pretreatment reduced the absorption of morphine from the duodenal and the jejunal loops. The initial uptake of morphine by BBMVs was stimulated in the presence of an H+ gradient (inner pH 7.5 and outer pH 5.0) and an overshoot phenomenon was observed. The initial uptake showed concentration dependence, i.e., it was saturable. Results obtained in this study indicate that carrier-mediated transport stimulated by the H+ gradient is partly involved in the duodeno-jejunal absorption of morphine, although morphine is passively absorbed from other sites.