Vatier J, Lionnet F, Vitre M T
INSERM U10, Hôpital Bichat, Paris.
Gastroenterol Clin Biol. 1987 Nov;11(11):758-63.
Antacid capacity of two aluminium containing-antacid drugs was evaluated in vitro; the first drug contained aluminium hydroxide (Alternagel), the second, aluminium phosphate (Phosphalugel). The antacid evaluation was performed 1) in a closed system by measuring antacid activity by down titration, 2) by a dynamic evaluation simulating acid secretion and gastric emptying. The results were reported both to the recommended therapeutical dose and to 100 mg aluminium. In static conditions, without gastric emptying, it was shown that aluminium hydroxide and phosphate acted by their buffer capacity in pH range less than or equal to pH 1.5. The therapeutical dose of aluminium phosphate displayed greater antacid activity than aluminium hydroxide, this fact being due to the empiric choice of the doses. With regard to aluminium content, aluminium phosphate activity remained greater than that of aluminium hydroxide although the difference decreased with decreasing pH values. The antacid capacities were related to the emptying outputs. Antacid activity corresponding to 100 mg aluminium was similar in both antacids less than pH 1.5. This effect was dependent on emptying rates. It can be suggested that Al was responsible for antacid activity in both preparations, and that the buffering capacity was supported by the change of aluminium cation in hydrolysis intermediary compounds.
在体外评估了两种含铝抗酸药物的抗酸能力；第一种药物含有氢氧化铝（胃舒平），第二种含有磷酸铝（磷酸铝凝胶）。抗酸评估通过以下方式进行：1）在封闭系统中通过向下滴定测量抗酸活性；2）通过模拟胃酸分泌和胃排空进行动态评估。结果以推荐治疗剂量和100毫克铝为基础进行报告。在无胃排空的静态条件下，结果表明氢氧化铝和磷酸铝在pH值小于或等于1.5的范围内通过其缓冲能力发挥作用。磷酸铝的治疗剂量显示出比氢氧化铝更大的抗酸活性，这一事实归因于剂量的经验性选择。就铝含量而言，尽管随着pH值降低差异减小，但磷酸铝的活性仍大于氢氧化铝。抗酸能力与排空量相关。在pH值小于1.5时，两种抗酸剂中相当于100毫克铝的抗酸活性相似。这种效应取决于排空速率。可以认为，铝在两种制剂中均对抗酸活性起作用，并且缓冲能力由水解中间化合物中铝阳离子的变化所支持。
