Smyth R D, Herczeg T, Wheatley T A, Hause W, Reavey-Cantwell N H
J Pharm Sci. 1976 Jul;65(7):1045-7. doi: 10.1002/jps.2600650722.
The rate and extent of acid consumption of an antacid suspension and tablet were evaluated by in vitro and in vivo techniques. Four different test procedures were used to estimate in vitro antacid reactivity. In vivo effects were determined in the fasted and postcibal states in normal human subjects by a radiotelemetry procedure. The duration of elevation of intragastric pH greater than 3 was in agreement with in vitro estimates of total acid consumption of the antacid. There was also good correlation between onset, extent, and duration of in vivo antacid activity and a modified in vitro Beekman antacid test procedure. There was no significant difference in antacid activity of the tablet or suspension in either in vitro or in vivo test procedures. A wide variation in antacid activity was observed between subjects and also in the fasted versus postcibal states. These studies emphasize the requirements for standardization of antacid products by comparactive in vitro and in vivo evaluations to facilitate individualized dose titration of the antacid in each patient and correlation of the acid secretion rate in various types of GI disease with the antacid dose.
通过体外和体内技术评估了抗酸混悬液和片剂的酸消耗速率及程度。采用四种不同的测试程序来估计体外抗酸反应性。通过无线电遥测程序在正常人类受试者的空腹和餐后状态下测定体内效应。胃内pH值大于3的升高持续时间与抗酸剂总酸消耗的体外估计值一致。体内抗酸活性的起始、程度和持续时间与改良的体外贝克曼抗酸试验程序之间也有良好的相关性。在体外或体内测试程序中，片剂或混悬液的抗酸活性均无显著差异。在受试者之间以及空腹与餐后状态下均观察到抗酸活性存在很大差异。这些研究强调了通过比较体外和体内评估来对抗酸产品进行标准化的必要性，以便于对每位患者进行抗酸剂的个体化剂量滴定，并将各种类型胃肠道疾病中的酸分泌速率与抗酸剂剂量相关联。
