Tanaka H, Naito S
Nihon Yakurigaku Zasshi. 1985 May;85(5):357-66. doi: 10.1254/fpj.85.357.
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.
将盐酸西曲酸酯经口或静脉给予兔子，并采用高效液相色谱法测定其在体液中的浓度。西曲酸酯在胃肠道和血液中易于水解，并代谢为对羟基苯丙酸（PHPA）和一种新的代谢产物对羟基苯甲酸（PHBA）。口服盐酸西曲酸酯后，大量未变化的药物分布于胃壁。PHPA分布于除脑以外的所有检测器官中。为了确定盐酸西曲酸酯的抗溃疡作用是否归因于未变化的药物、PHPA或氨甲环酸，对大鼠进行了阿司匹林和水浸诱导的胃溃疡研究。结果发现，氨甲环酸具有与盐酸西曲酸酯相似的抗溃疡作用。
