Ishimori A, Kawamura T, Koizumi F
Department of Clinical and Laboratory Medicine, Tohoku University School of Medicine, Sendai, Japan.
Arzneimittelforschung. 1988 Jun;38(6):833-9.
The effect of trimoprostil, an analogue of prostaglandin E2, on gastric secretion was studied in healthy volunteers in comparison with that of cimetidine. Graded doses of 50, 250, 500 and 750 micrograms were given p.o. for trimoprostil and 200 mg for cimetidine. Basal secretion was significantly depressed at doses larger than 500 micrograms of trimoprostil but not by 200 mg of cimetidine probably due to the method of gastric analysis adopted in the study. In amyl-oxy-carbonyl (AOC)-tetragastrin stimulated gastric secretion, 500 micrograms of trimoprostil depressed acid output significantly, but did not affect pepsin output which was depressed, however, at 750 micrograms. On the other hand cimetidine markedly inhibited AOC-tetragastrin stimulated acid and pepsin secretion. Some difference was also recognized between trimoprostil and cimetidine concerning the mechanism of inhibitory action. Serum concentration of trimoprostil measured at 60 min after oral administration varied dose-dependently and antisecretory effects were also found to be dose-related. Serum gastrin and pepsinogen I were not affected either by trimoprostil or cimetidine. These results indicate that trimoprostil showed inhibitory effect on gastric secretion at doses larger than 500 micrograms for acid, and at doses larger than 750 micrograms for pepsin.
在健康志愿者中研究了前列腺素E2类似物曲莫前列素对胃液分泌的影响，并与西咪替丁进行了比较。曲莫前列素口服给予50、250、500和750微克的分级剂量，西咪替丁给予200毫克。剂量大于500微克的曲莫前列素可显著抑制基础分泌，但200毫克西咪替丁则无此作用，这可能是由于该研究采用的胃液分析方法所致。在淀粉氧羰基（AOC）-四胃泌素刺激的胃液分泌中，500微克曲莫前列素可显著降低胃酸分泌量，但不影响胃蛋白酶分泌量，然而，750微克时胃蛋白酶分泌量降低。另一方面，西咪替丁可显著抑制AOC-四胃泌素刺激的胃酸和胃蛋白酶分泌。曲莫前列素和西咪替丁在抑制作用机制方面也存在一些差异。口服给药60分钟后测得的曲莫前列素血清浓度呈剂量依赖性变化，其抗分泌作用也呈剂量相关性。曲莫前列素和西咪替丁均未影响血清胃泌素和胃蛋白酶原I。这些结果表明，曲莫前列素在剂量大于500微克时对胃酸分泌有抑制作用，在剂量大于750微克时对胃蛋白酶分泌有抑制作用。
