[Pharmacokinetic and pharmacological studies on cetraxate, an anti-ulcer agent].
Cetraxate hydrochloride was administered either orally or intravenously to rabbits, and its concentration in body fluids was determined by using the HPLC method. Cetraxate was easily hydrolyzed in the gastrointestinal tract and blood, and it was metabolized to p-hydroxyphenylpropionic acid (PHPA) and a new metabolite, p-hydroxybenzoic acid (PHBA). After oral administration of cetraxate hydrochloride, a large amount of unchanged drug was distributed to the gastric wall. PHPA was distributed in all the organs examined, excluding the brain. To determine whether or not the anti-ulcer action of cetraxate hydrochloride was due to the unchanged drug, PHPA, or tranexamic acid, studies with aspirin and water-immersion -induced gastric ulcers in rats were performed. As a result, it was found that tranexamic acid had an anti-ulcer action similar to that of cetraxate hydrochloride.
D000818:Animals; D000897:Anti-Ulcer Agents / Q000378:metabolism*; D002851:Chromatography, High Pressure Liquid; D003509:Cyclohexanecarboxylic Acids / Q000378:metabolism*; D062385:Hydroxybenzoates / Q000032:analysis; D007700:Kinetics; D008196:Lymph / Q000032:analysis; D008297:Male; D010666:Phenylpropionates / Q000032:analysis; D011817:Rabbits; D051381:Rats; D011919:Rats, Inbred Strains; D013276:Stomach Ulcer / Q000188:drug therapy*; D014018:Tissue Distribution; D014148:Tranexamic Acid / Q000031:analogs & derivatives / Q000134:cerebrospinal fluid / Q000378:metabolism* / Q000627:therapeutic use
D000897:Anti-Ulcer Agents; D003509:Cyclohexanecarboxylic Acids; D062385:Hydroxybenzoates; D010666:Phenylpropionates; C032948:3-hydroxybenzoic acid; C000665:cetraxate; C008869:phloretic acid; D014148:Tranexamic Acid