Hedenström H, Alm C, Kraft M, Grahnén A
Department of Clinical Physiology, University Hospital, Uppsala, Sweden.
Aliment Pharmacol Ther. 1997 Dec;11(6):1137-41. doi: 10.1046/j.1365-2036.1997.00264.x.
The therapeutic effect of drugs inhibiting acid production on acid-related discomforts is related to both the onset and duration of action of the drug. The effects on gastric pH by single oral doses of some acid-inhibiting drugs were investigated by measuring daytime (morning to lunch) intragastric pH in healthy volunteers.
This randomized, single-dose, 4-way crossover study included 15 healthy fasting subjects. Effervescent ranitidine tablets 150 and 300 mg, fast-dissolving famotidine tablets 20 mg and capsules of omeprazole 20 mg were administered. Measurements of intragastric pH were performed every 4 s for 10 min prior to drug administration and during the following 4 h.
The effervescent ranitidine tablets (150 or 300 mg) produced similar changes in intragastric pH: following an immediate increase to about pH 5, intragastric pH decreased slightly over the next 10-20 min. Thereafter pH increased steadily, reaching pH 4 after 20-40 min and pH 6 after about 70 min. After famotidine, pH 4 was reached after 80 min, significantly slower than ranitidine. After omeprazole, pH 3 was never reached. Ranitidine 150 and 300 mg showed significantly larger integrated pH responses over the 4-h observation period, compared to famotidine (P = 0.0288 and 0.0074) or omeprazole (P < 0.001).
After single-dose administration to healthy fasting volunteers), ranitidine effervescent tablets showed a significantly more rapid onset of action and a significantly larger integrated pH response compared to either famotidine 20 mg fast-dissolving tablets or omeprazole 20 mg capsules.
抑制胃酸分泌的药物对酸相关性不适的治疗效果与药物的起效时间和作用持续时间均有关。通过测量健康志愿者白天(上午至午餐时间)的胃内pH值,研究了单次口服某些抑酸药物对胃pH值的影响。
这项随机、单剂量、四交叉研究纳入了15名健康的空腹受试者。给予150毫克和300毫克的泡腾雷尼替丁片、20毫克的速溶法莫替丁片以及20毫克的奥美拉唑胶囊。在给药前10分钟及给药后的4小时内,每4秒测量一次胃内pH值。
泡腾雷尼替丁片(150毫克或300毫克)引起的胃内pH值变化相似:胃内pH值立即升至约5,随后在接下来的10 - 20分钟内略有下降。此后pH值稳步上升,20 - 40分钟后达到pH 4,约70分钟后达到pH 6。服用法莫替丁后,80分钟后达到pH 4,明显慢于雷尼替丁。服用奥美拉唑后,从未达到pH 3。在4小时的观察期内,150毫克和300毫克的雷尼替丁的累计pH反应明显大于法莫替丁(P = 0.0288和0.0074)或奥美拉唑(P < 0.001)。
在对健康空腹志愿者进行单剂量给药后,与20毫克速溶法莫替丁片或20毫克奥美拉唑胶囊相比,泡腾雷尼替丁片起效明显更快,累计pH反应明显更大。