Dammann H G, Müller P, Kather H, Simon B
Arzneimittelforschung. 1982;32(5):550-2.
The effect of graded oral doses of 16,16-dimethyl-prostaglandin E2 (PG E2) on basal acid secretion in healthy volunteers was tested over a time period of 6 h. In addition, studies were conducted to determine whether pretreatment with this methylated PG-analog could prevent the characteristic fall in human gastric potential difference (PD) associated with intragastric instillation of 50 ml of 4 mmol/l Na-taurocholate. Basal acid output was reduced by 80--90% after 0.5 microgram/kg b.w. 16,16-dimethyl-PG E2. Half maximum inhibition was achieved by 0.1 microgram/kg b.w., whereas a 10 fold lower dose of 16,16-dimethyl-PG E2 (0.01 microgram/kg b.w.) effectively protected human gastric mucosa against the injurious effects of Na-taurocholate. In analogy to findings in animals it is, therefore, concluded that 16,16-dimethyl-PG E2 has two distinct properties in human stomach, antisecretory and protective ones, which were independent of each other.
在6小时的时间段内,测试了不同口服剂量的16,16 - 二甲基前列腺素E2(PG E2)对健康志愿者基础胃酸分泌的影响。此外,还进行了研究以确定用这种甲基化的PG类似物进行预处理是否可以预防与胃内滴注50 ml 4 mmol/l牛磺胆酸钠相关的人体胃电位差(PD)的特征性下降。在给予0.5微克/千克体重的16,16 - 二甲基 - PG E2后,基础胃酸分泌量降低了80% - 90%。0.1微克/千克体重可达到半数最大抑制作用,而剂量降低10倍的16,16 - 二甲基 - PG E2(0.01微克/千克体重)可有效保护人体胃黏膜免受牛磺胆酸钠的损伤作用。因此,与动物实验结果类似,得出结论:16,16 - 二甲基 - PG E2在人胃中有两种不同的特性,即抑制胃酸分泌和保护胃黏膜,且这两种特性相互独立。