[Physicochemical and pharmacological characteristic and clinical efficacy of an anti-irritable bowel syndrome agent, polycarbophil calcium (Polyful)].
Irritable bowel syndrome (IBS) is a functional bowel disorder characterized by abdominal pain or discomfort and abnormal defecation. Polycarbophil calcium, a water-absorbing polymer, is expected to improve stool consistency. Polycarbophil calcium decalcified under the acidic condition and then absorbed 70 times its weight of water under the neutral condition. In in situ experiments using rat jejunum and colon, polycarbophil decreased water absorption by the intestine without affecting water secretion. Polycarbophil inhibited prostaglandin E2-, 5-hydroxy-L-tryptophan- and castor oil-induced diarrhea in mice or rats. Polycarbophil calcium also inhibited sennoside-induced diarrhea in dogs. Polycarbophil increased the weight of feces in naive or low-fiber diet feeding rats. In naive dogs, polycarbophil calcium increased stool frequency, stool weight and moisture. Polycarbophil was not absorbed from the gastrointestine, not metabolized and eliminated into feces in rats and dogs. Polycarbophil calcium did not affect the absorption of coadministered drugs in dogs. In the dose-finding clinical study for IBS, polycarbophil calcium was effective both in diarrhea and constipation. In the Phase III study, polycarbophil calcium was superior to trimebutine maleate in efficacy and equal in safety. Emesis/vomiting and thirst were observed, but episodes of diarrhea or constipation by excessive action were few. Polycarbophil calcium seems promising as an anti-IBS agent.
Iwanaga
Yuji
Y
Laboratory of Pharmacology,  Research Division, Hokuriku Seiyaku Co., Ltd., 37-1-1 Inokuchi, Katsuyama City, Fukui 911-8555, Japan. yuji.iwanaga@abbott.com
D000180:Acrylic Resins / Q000493:pharmacokinetics / Q000494:pharmacology* / Q000627:therapeutic use*; D000818:Animals; D000930:Antidiarrheals / Q000493:pharmacokinetics / Q000494:pharmacology* / Q000627:therapeutic use*; D002400:Cathartics / Q000493:pharmacokinetics / Q000494:pharmacology* / Q000627:therapeutic use*; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D002986:Clinical Trials as Topic; D003109:Colonic Diseases, Functional / Q000188:drug therapy*; D003672:Defecation / Q000187:drug effects; D004195:Disease Models, Animal; D004285:Dogs; D005243:Feces / Q000737:chemistry; D006801:Humans; D051379:Mice; D051381:Rats
D000180:Acrylic Resins; D000930:Antidiarrheals; D002400:Cathartics; C030312:calcium polycarbophil