Halter F
Z Gastroenterol. 1983 Mar;21 Suppl:33-40.
Observations made during intragastric titration studies performed with antacids that have an identical neutralizing capacity but differ in their chemical compositions suggested that aluminum hydroxide loses a large portion of its neutralizing capacity when applied postprandially. To further elucidate the mechanism involved in-vitro studies were performed whereby the reactivity of magnesium hydroxide, aluminum hydroxide, and calcium carbonate was estimated either in aliquots of 10 ml of water or 10 ml of 5% oxo solution. The effectively available neutralizing capacity of the respective antacids was measured for the pH range of 1 to 5. The results revealed that magnesium hydroxide as well as calcium carbonate can fully react with acid whereby their theoretically available neutralizing capacity is fully available for the pH of 1 to 4.5, this in water as well as in 5% oxo solution. In contrast, aluminum hydroxide loses a large proportion of the theoretically available neutralizing capacity already in water but especially in oxo solution in a pH dependent manner. The loss far exceeds that calculated when one takes into account the pKa dependent hydrolysis of aluminum hydroxide. This loss of reactivity increased from 20% at pH 1 in a near linear fashion up to above 80% at pH 3.5. A food induced decrease of aluminum hydroxide solubility as well as stabilisation of the macromolecular aluminum hydroxide complexes through anions and organic acids are likely to be responsible for this loss of reactivity.
在用具有相同中和能力但化学成分不同的抗酸剂进行的胃内滴定研究中观察到,氢氧化铝在餐后使用时会损失很大一部分中和能力。为了进一步阐明其中涉及的机制,进行了体外研究,在10毫升水或10毫升5%含氧溶液的等分试样中评估氢氧化镁、氢氧化铝和碳酸钙的反应性。在pH值为1至5的范围内测量了各抗酸剂的有效可用中和能力。结果表明,氢氧化镁和碳酸钙都能与酸充分反应,因此它们理论上可用的中和能力在水和5%含氧溶液中对于pH值为1至4.5时都能完全发挥作用。相比之下,氢氧化铝在水中就已经损失了很大一部分理论上可用的中和能力,而在含氧溶液中尤其如此,且呈pH依赖性。这种损失远远超过在考虑氢氧化铝的pKa依赖性水解时所计算出的损失。这种反应性的损失在pH值为1时从20%开始以近似线性的方式增加,在pH值为3.5时达到80%以上。食物引起的氢氧化铝溶解度降低以及阴离子和有机酸对大分子氢氧化铝络合物的稳定作用可能是造成这种反应性损失的原因。