Laxative and anti-diarrheal activity of polycarbophil in mice and rats
Laxative and anti-diarrheal activity of polycarbophil in mice and rats
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DOI：
10.1254/jjp.89.133
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发表时间：
2002-06-01
期刊：
影响因子：
--
通讯作者：
Kato, H
中科院分区：
文献类型：
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作者：
Saito, T;Mizutani, F;Kato, H
我们研究了聚碳酸酯的泻药和止泻活性，并与其他用于治疗功能性肠病(FBD)的药物进行了比较。在幼鼠中，多聚碳酸盐(500 mg/kg)增加了粪便重量和水分含量，而不会引起腹泻。羧甲基纤维素(CMC)对大鼠的排便无明显影响。硫代吡咯烷胺、曲美布汀和格拉司琼均能明显引起小鼠腹泻，并呈剂量依赖关系。大鼠氯哌丁胺和可乐定可引起便秘，表现为粪便重量减少。多聚碳酸盐(500 mg/kg)和CMC增加了粪便重量，没有腹泻。相反，曲美布汀进一步降低了便秘大鼠的粪便重量。聚碳酸酯(500 mg/kg)可抑制蓖麻油引起的腹泻，250-500 mg/kg可使前列腺素E-2、5-羟色胺或卡巴胆碱引起的小鼠粪便呈异形。多聚碳酸盐(500 mg/kg)还可减少大鼠的粪便排泄量，并可增加束缚应激(WRS)所致的排泄量。除卡巴胆碱引起的腹泻和WRS诱导的排泄外，思爱在腹泻模型中没有作用。除卡巴胆碱引起的腹泻外，洛哌丁胺、曲美布汀和格拉司琼均可抑制腹泻的产生和WRS诱导的排空。结果表明，与其他药物不同的是，聚碳酸酯可以预防便秘和腹泻，而不会引起腹泻或便秘。聚碳酸酯等亲水性聚合物将成为治疗FBD的有前途的药物。
We investigated the laxative and anti-diarrheal activity of polycarbophil, an insoluble hydrophilic polymer, in comparison with other agents used for treating functional bowel disorder (FBD). In naive rats, polycarbophil (500 mg/kg) increased fecal weight and water contents without producing diarrhea. Carboxymethylcellulose (CMC) did not produce evident changes in bowel movement. Picosulfate markedly produced diarrhea, Loperamide, trimebutine and granisetron decreased stool output dose-dependently. Constipation, indicated by decrease in fecal weight, was produced by loperamide and clonidine in rats. Polycarbophil (500 mg/kg) and CMC increased fecal weight without diarrhea. Conversely trimebutine further decreased fecal weight in constipated rats. Polycarbophil (500 mg/kg) suppressed diarrhea induced by castor oil, and at 250 - 500 mg/kg, it produced shaped stools in animals with stools loosened by prostaglandin E-2, serotonin or carbachol in mice. Polycarbophil (500 mg/kg) also reduced stools in rats with stool output increased by wrap restraint stress (WRS). CIVIC had no effect in the diarrhea models, except for carbachol-induced diarrhea, and WRS-induced evacuation. Loperamide, trimebutine and granisetron inhibited diarrhea production and WRS-induced evacuation, except for carbachol-induced diarrhea. The results show that polycarbophil prevents constipation and diarrhea without inducing diarrhea or constipation, which is different from the other agents. Hydrophilic polymers such as polycarbophil will be promising agents for the treatment of FBD.