Smout A J, Jonkman J H, Peeters P A, De Bruin H
Department of Gastroenterology, University Hospital Utrecht, The Netherlands.
Aliment Pharmacol Ther. 1995 Feb;9(1):51-6. doi: 10.1111/j.1365-2036.1995.tb00351.x.
To compare the effects on intragastric acidity of a single evening dose of either standard or effervescent formulations of ranitidine (300 mg) or cimetidine (800 mg).
Twelve healthy subjects were studied, using a four-period randomized cross-over design and an ambulatory intragastric pH monitoring technique. The subjects received a standard evening meal at 17.00 hours and one of the H2-receptor antagonist formulations was given at 23.00 hours.
Both effervescent formulations caused a transient rapid increase in intragastric pH, reaching a maximum at about 3 min after ingestion. After both effervescent formulations a significantly higher pH was measured during the first 45 min after ingestion (P < 0.05), compared to the regular formulations. The onset of action of the H2-receptor antagonists was similar for both formulations of ranitidine and the effervescent cimetidine, but tended to be slower for the regular cimetidine (P = 0.06). Nocturnal intragastric pH was significantly increased by all four formulations, but more effectively so by the two ranitidine formulations. The duration of action (taken as time with pH > 4) of both ranitidine formulations was longer than that of both cimetidine formulations (P < 0.002).
A single evening dose of 300 mg ranitidine produces a stronger decrease of nocturnal gastric acid secretion than 800 mg cimetidine. The effervescent formulations of both drugs offer the advantage of a rapid decrease (within minutes) of intragastric acidity, with preservation of the sustained systemic effect.
比较单次晚间服用300毫克雷尼替丁或800毫克西咪替丁的标准剂型与泡腾剂型对胃内酸度的影响。
采用四周期随机交叉设计和动态胃内pH监测技术对12名健康受试者进行研究。受试者于17:00进食标准晚餐,并于23:00服用一种H2受体拮抗剂剂型。
两种泡腾剂型均可使胃内pH值短暂快速升高,服药后约3分钟达到峰值。与常规剂型相比,两种泡腾剂型在服药后的前45分钟内测得的pH值显著更高(P<0.05)。雷尼替丁的两种剂型和泡腾型西咪替丁的H2受体拮抗剂起效时间相似,但常规西咪替丁起效较慢(P=0.06)。所有四种剂型均可使夜间胃内pH值显著升高,但雷尼替丁的两种剂型效果更佳。两种雷尼替丁剂型的作用持续时间(以pH>4的时间计)均长于两种西咪替丁剂型(P<0.002)。
单次晚间服用300毫克雷尼替丁比800毫克西咪替丁更能有效降低夜间胃酸分泌。两种药物的泡腾剂型均具有胃内酸度在数分钟内快速下降的优点,同时保持了持续的全身效应。