[Antacid activity of citrate-bicarbonate complex of effervescent formulations of ranitidine. In vitro analysis using...

Antacid activity supported by citrate-bicarbonate complex of four effervescent ranitidine forms has been assessed in vitro using an 'artificial stomach-duodenum' model controlled by microcomputer. This model allows (i) maintenance of constant the rates of the fluxes throughout the experiments or (ii) simulation of gastroduodenal flux regulation, in the normal subject (NS) or in the duodenal ulcer patient (DU) situation. The four forms developed a theoretical maximal antacid capacity between 61 and 81 mmol with a maximum intragastric pH between 3.2 and 4.8. In the gastroduodenal flux regulation simulation, antacid activity duration was rapid and included between 85 and 118 min in NS situation (50 to 56 mmol H+ consumed) and between 75 and 93 min in DU situation (43 to 47 mmol H+ consumed). The reduction of acid load penetrating into the duodenum was contained between 36 and 50 per cent. Effervescent compounds exerted a neutralising activity and a buffering capacity close to pH 6.0 (5 per cent of total antacid capacity), related to antacid potency.