Miwa M, Tani N, Miwa T
Int J Clin Pharmacol Ther Toxicol. 1984 Apr;22(4):214-7.
Oral administration of YM-11170 (5-20 mg) inhibited both basal and tetragastrin-induced gastric secretion of acid and pepsin in healthy volunteers. YM-11170 was at least 20 times more potent than cimetidine in inhibiting stimulated acid secretion. The area under the plasma concentration of YM-11170 vs time curve correlated positively to both dose and percent inhibition of acid output in response to tetragastrin. YM-11170 significantly inhibited basal and stimulated acid secretion even 10 h after a 20-mg dose. A plasma level of YM-11170 required for 50% inhibition of stimulated acid secretion was found to be 13 ng/ml. These results indicate that YM-11170 is a very potent inhibitor of gastric acid secretion and that twice daily medication of 20 mg YM-11170 is recommendable for further antisecretory studies with ulcer patients.
在健康志愿者中,口服YM - 11170(5 - 20毫克)可抑制基础胃酸分泌以及由促胃液素诱导的胃酸和胃蛋白酶分泌。在抑制刺激后的胃酸分泌方面,YM - 11170的效力至少是西咪替丁的20倍。YM - 11170血药浓度-时间曲线下面积与剂量以及对促胃液素反应的胃酸分泌抑制百分比呈正相关。即使在服用20毫克剂量的YM - 11170 10小时后,它仍能显著抑制基础胃酸分泌和刺激后的胃酸分泌。发现抑制50%刺激后胃酸分泌所需的YM - 11170血浆水平为13纳克/毫升。这些结果表明,YM - 11170是一种非常有效的胃酸分泌抑制剂,对于溃疡患者的进一步抗分泌研究,建议每日两次服用20毫克YM - 11170。