Konturek S J, Kwiecien N, Obtulowicz W, Maczka J, Hebzda Z, Oleksy J
Institute of Physiology, Academy of Medicine, Cracow, Poland.
Scand J Gastroenterol. 1991 Nov;26(11):1145-51. doi: 10.3109/00365529108998606.
Previous studies in animals and humans demonstrated that nocloprost, a stable prostaglandin E2 analogue, shows very high gastroprotective potency, relatively weak gastric inhibitory activity, and low systemic bioavailability after oral administration. In this study the effects of nocloprost on gastric acid secretion and intraluminal pH and on gastric emptying and plasma gastrin levels were determined in humans. Nocloprost at doses of 50 and 100 micrograms was ineffective, but at a dose of 200 micrograms it reduced the response to pentagastrin significantly and that to a peptone meal by 30-50% and abolished plasma gastrin response without affecting the rate of gastric emptying. Nocloprost given at a dose of 100 micrograms three times daily 30 min before the major meals (breakfast, lunch, and dinner) did not affect intragastric pH significantly as monitored by continuous intraluminal pH-metry. We conclude that nocloprost does not affect gastric acid secretion or intraluminal pH when applied at a dose (50-100 micrograms) that is gastroprotective and that is proposed for peptic ulcer therapy. A higher dose (200 micrograms) of nocloprost causes moderate gastric acid inhibition and suppression of plasma gastrin release without affecting gastric emptying or causing any side effects.
先前在动物和人体中的研究表明，诺克洛前列素是一种稳定的前列腺素E2类似物，具有很高的胃保护效力、相对较弱的胃抑制活性，口服后全身生物利用度较低。在本研究中，测定了诺克洛前列素对人体胃酸分泌、腔内pH值、胃排空及血浆胃泌素水平的影响。50微克和100微克剂量的诺克洛前列素无效，但200微克剂量时可显著降低对五肽胃泌素的反应，并使对蛋白胨餐的反应降低30%-50%，且消除血浆胃泌素反应，而不影响胃排空速率。在主餐（早餐、午餐和晚餐）前30分钟每日三次给予100微克剂量的诺克洛前列素，通过连续腔内pH测量监测，并未显著影响胃内pH值。我们得出结论，当以具有胃保护作用且拟用于消化性溃疡治疗的剂量（50-100微克）应用时，诺克洛前列素不影响胃酸分泌或腔内pH值。更高剂量（200微克）的诺克洛前列素可引起适度的胃酸抑制并抑制血浆胃泌素释放，而不影响胃排空或引起任何副作用。
