Food, Acid Supplementation and Drug Absorption – a Complicated Gastric Mix: a Randomized Control Trial

Abstract

Purpose The purpose of this study was to determine the impact of food on gastric pH and the ability of over the counter betaine hydrochloride (BHCl) acid to reacidify gastric pH after food-induced elevations in gastric pH. Methods This open-label cross over clinical study (NCT02758015) included 9 subjects who were randomly assigned to one of 16 possible, 4-period cross-over sequences to determine the impact and relationship of food and gastric pH with acid supplementation. Subjects were administered various doses (1500 mg, 3000 mg and 4500 mg) of betaine hydrochloride (BHCl) to determine the ability of acid supplementation to reacidify gastric pH after the elevation of gastric pH caused by the ingestion of food. Results Following the administration of food and the resulting elevation in gastric pH, time to return to baseline gastric pH levels without acid supplementation was 49.7 ± 14.0 min. Administering 4500 mg of BHCl acid in capsules was able to reacidify gastric pH levels back to baseline following the administration of food in approximately 17.3 ± 5.9 min. AUC pH of each treatment were similar and not statistically different. Mean max pH following the administration of food was 3.20 ± 0.55. Conclusion The ability of food to elevate and maintain gastric pH levels in the presence of acid supplementation was made evident throughout the study. A 4500 mg dose of BHCl was required to reacidify gastric pH after the administration of food. This study details the difficulty faced by clinicians in dosing a poorly soluble, weakly basic drug to patients receiving acid reducing agents where administration with food is recommended to avoid gastric side effects. Trial Registration: https://clinicaltrials.gov/ct2/show/ NCT02758015 KEY WORDS betaine hydrochloride . gastric pH . gastric reacidification . meal effects ABBREVIATIONS ARA Acid reducing agent BHCl Betaine hydrochloride GERD Gastroesophageal reflux disease PPI Proton pump inhibitor

Creating a Framework for Treating Autoimmune Gastritis—The Case for Replacing Lost Acid

“…Only the 4500 mg dose of BHCL (six capsules) was able to return the pH to its pre-meal baseline faster, in 17 min. The subjects experienced no adverse effects from either the Heidelberg capsule or the BHCL, despite the high dosages [ 67 ]. Surofchy’s study suggests that BHCL does not improve acidification in a healthy stomach except in high amounts and that BHCL is well tolerated even in high amounts.…”