Abstract

Alginates are used as the active pharmaceutical ingredients (API) in anti-reflux formulations for many years for the treatment of the symptoms of gastroesophageal reflux disease (GERD). After the consumption of such formulation a swollen gel layer (raft) is formed in the stomach of the patient. This raft is further floated to the upper part of the stomach, where its traps and neutralizes the acid content of the stomach away from the gastroesophageal junction and preventing damage to the esophageal mucosa. The characterization of such raft is mainly performed according to the so-called raft strength, where a L-hook is moved through the formed raft mass and the corresponding force is recorded. The drawbacks of this method are discussed in this contribution, which lead to high standard deviations in the results. Alternatively, a new method for the characterization of the raft is introduced, which is based on a forward extrusion process. This new method showed improved reproducibility and decreased standard deviations. As further shown in this article. the performance of the anti-reflux formulation is mainly influenced by the chemical structure of the alginate, which are used in these formulations. Alginates are a copolymer build up from 1,4-α-L-guluronic (G) and 1,4-β-D-mannuronic (M) units. Based on the modelling of this G / M ratios to the raft performance attributes, new structure property relationships could be achieved, which allow a deeper understanding of the functional related characteristics (FRC).

Keywords

gastroesophageal reflux disease