Evaluation of Anti-Ulcer Effect among Various Anti-Peptic Ulcer Agents in Experimental Animal Models

Abstract

A retrospective bibliographical review was carried out to evaluate objectively the antipepticulcer activity of various agents in experimental animal models. In the present study, we selected benexate, cetraxate, clebopride, plaunotol, sofalcone, teprenone, and troxipide, which have been approved in Japan from 1979 to 1988, as enhancers of mucosal defense.Relationship between ulcer inhibition rate (UIR) and pharmacological effective oral dosewas examined in rats, as regards eight experimental peptic ulcer models. Most of theagents inhibited stress-, indomethacin-, and acetic acid-induced ulcer. It was found thatthe dose exhibiting the, pharmacological effect was remarkably different .among agents ineach model or among models in each agent. Therefore, the dose for UIR 50%, UIR_50% (or UIR_30% in acetic acid ulcer), which was calculated by the least-squares linear regressionanalysis of UIR versus logarithm of dose, was used as an index for the evaluation of eachinhibitory activity against ulceration. It was found that cetraxate was relatively. effectivein ethanol ulcer, plaunotol in stress and aspirin ulcer, and teprenone in indomethacin andethanol ulcer. Clebopride and plaunotol showed smaller UIR_50% againststress ulcer, andteprenone and troxipide showed smaller UIR_50% against indomethacin ulcer. Smaller UIR50% for ethanol ulcer was found with sofalcone and teprenone, and smaller .UIR_30%for acetic acid ulcer was found with sofalcone. It is suggested that UIR_50% (or UIR_30%) may be a useful index for evaluating the preclinical anti-ulcer property and its rank orderamong various agents even in the absence of well-designed comparative studies.