Arimori K, Deshimaru M, Furukawa E, Nakano M
Department of Pharmacy, Kumamoto University Hospital, Japan.
J Pharm Pharmacol. 1992 Dec;44(12):977-80. doi: 10.1111/j.2042-7158.1992.tb07077.x.
Transport of paraquat and mexiletine from the blood into the intestinal lumen and the peritoneal cavity was examined after their intravenous administration (paraquat: 20 mg kg-1, mexiletine: 10 mg kg-1) to rats. The average amounts of paraquat transferred into the intestinal lumen and the peritoneal cavity were 1.39 and 22.8% of the dose in 120 min, respectively. The average amounts of mexiletine transferred into the intestinal lumen and the peritoneal cavity were 6.1 and 2.5% of the dose in 120 min, respectively. The transfer rate of 3H2O into the peritoneal cavity after intravenous administration (1.85 MBq) was greater than that into the intestinal lumen. In view of the hydrophilic nature of paraquat cation, a solvent drag effect due to movement of water might contribute to transport of paraquat from the blood to the peritoneal cavity. Differences in transport behaviour across the two membranes could be due to differences in the geometrical factors such as the surface area and the distribution of blood vessels. Differences might also be due to differences in physicochemistry and pharmacological effects of both substances.
给大鼠静脉注射百草枯（20毫克/千克）和美西律（10毫克/千克）后，检测了它们从血液到肠腔和腹腔的转运情况。120分钟内，转运至肠腔和腹腔的百草枯平均量分别为给药剂量的1.39%和22.8%。120分钟内，转运至肠腔和腹腔的美西律平均量分别为给药剂量的6.1%和2.5%。静脉注射（1.85兆贝可）后，3H2O进入腹腔的转运速率大于进入肠腔的转运速率。鉴于百草枯阳离子的亲水性，水的移动产生的溶剂拖曳效应可能有助于百草枯从血液转运至腹腔。跨两种膜的转运行为差异可能归因于几何因素的差异，如表面积和血管分布。差异也可能是由于两种物质的物理化学和药理作用不同。
