Levine R A, Petokas S, Czarny L, Schwartz G J, Bynum L
Prostaglandins Leukot Med. 1986 Oct;24(2-3):219-25. doi: 10.1016/0262-1746(86)90129-0.
We evaluated the degree of acid suppression that occurred when enprostil, a dehydro-prostaglandin E2 (PGE2) methyl ester analog, was administered before (anti-cibum AC) or after a meal (post-cibum PC). A double-blind, randomized, single-dose, parallel-group design compared enprostil, 35 mcg, 25 min AC or 5 min PC, with placebo AC or PC in 30 healthy adults. Enprostil or placebo was administered at time 0 and a standard beef test meal was ingested at 25 min, followed 5 min later by enprostil or placebo. A second test meal was consumed at 210 min. Intragastric titration was performed from 30 to 390 min. Subjects receiving enprostil-AC or enprostil-PC secreted less (P less than 0.05) acid compared to placebo; however, the antisecretory effects of enprostil-AC or enprostil-PC were similar throughout the duration of study. Minor adverse reactions were present in 13/30 subjects and confined to those receiving enprostil. In contrast to the previously reported potentiation of trimoprostil, a trimethyl-desoxy-PGE2 analog, antisecretory activity by food, enprostil-PC did not result in more prominent or prolonged suppression of gastric acid secretion than enprostil-AC. There is an apparent specificity of different oral PGE2 analogs with regard to their antisecretory activity in the presence or absence of food.
我们评估了在餐前（抗食AC）或餐后（食后PC）给予地诺前列素（一种脱氢前列腺素E2（PGE2）甲酯类似物）时发生的胃酸抑制程度。一项双盲、随机、单剂量、平行组设计将35微克地诺前列素在餐前25分钟（AC）或餐后5分钟（PC）给药与安慰剂AC或PC在30名健康成年人中进行了比较。地诺前列素或安慰剂在0时刻给药，在25分钟时摄入标准牛肉试验餐，5分钟后再给予地诺前列素或安慰剂。在210分钟时食用第二顿试验餐。在30至390分钟进行胃内滴定。与安慰剂相比，接受地诺前列素-AC或地诺前列素-PC的受试者分泌的胃酸较少（P<0.05）；然而，在整个研究期间，地诺前列素-AC或地诺前列素-PC的抗分泌作用相似。13/30的受试者出现轻微不良反应，且仅限于接受地诺前列素的受试者。与先前报道的三甲基去氧-PGE2类似物曲莫前列素的食物增强抗分泌活性相反，地诺前列素-PC对胃酸分泌的抑制作用并不比地诺前列素-AC更显著或持久。不同的口服PGE2类似物在有或没有食物的情况下其抗分泌活性存在明显的特异性。
