Wilson D E, Quadros E, Rajapaksa T, Adams A, Noar M
Dig Dis Sci. 1986 Feb;31(2 Suppl):126S-129S. doi: 10.1007/BF01309336.
Misoprostol, a synthetic prostaglandin E1 analog, at doses of 200, 400, or 800 micrograms, and placebo were administered orally in random fashion to eight healthy male volunteers. The effects on basal and pentagastrin (0.6 microgram/kg/hr)-stimulated acid and mucus (N-acetylneuraminic acid measurement) secretion were then determined. Misoprostol in 200-, 400-, and 800-micrograms doses reduced basal acid secretion by 91%, 93%, and 93%, respectively. Mean 2-hr acid secretion was reduced by 27%, 33% (P less than 0.01), and 51% (P less than 0.01), respectively. Reductions in secretory volumes paralleled acid changes. Mucus secretion increased by 37%, 82%, and 95% during the basal period following misoprostol doses of 200, 400, and 800 micrograms, respectively. Increase in mucus of 27%, 31%, and 38% was observed during maximal acid inhibition (1-30 min) by misoprostol in 200-, 400-, and 800-micrograms doses. The concentration of gastric juice mucus was significantly increased. Subjects experienced no significant side effects during the study, and there were no significant changes in hematological or chemical blood studies. Misoprostol, a potent inhibitor of gastric acid secretion, also stimulates mucus secretion. This mucogenic effect may be important in the mucosal protective action of misoprostol and its antiulcer efficacy in man.
米索前列醇是一种合成的前列腺素E1类似物,以200、400或800微克的剂量与安慰剂一起随机口服给予8名健康男性志愿者。然后测定其对基础胃酸分泌以及五肽胃泌素(0.6微克/千克/小时)刺激的胃酸和黏液(通过测量N - 乙酰神经氨酸)分泌的影响。200微克、400微克和800微克剂量的米索前列醇分别使基础胃酸分泌减少了91%、93%和93%。平均2小时胃酸分泌分别减少了27%、33%(P<0.01)和51%(P<0.01)。分泌量的减少与胃酸变化平行。在给予200微克、400微克和800微克米索前列醇后的基础期,黏液分泌分别增加了37%、82%和95%。在200微克、400微克和800微克剂量的米索前列醇最大程度抑制胃酸分泌期间(1 - 30分钟),黏液分别增加了27%、31%和38%。胃液黏液浓度显著增加。在研究过程中,受试者未出现明显副作用,血液学或血液化学检查也无显著变化。米索前列醇是一种强效胃酸分泌抑制剂,还能刺激黏液分泌。这种促黏液分泌作用可能在米索前列醇的黏膜保护作用及其对人类的抗溃疡疗效中起重要作用。