School of Pharmacy, University of California San Francisco, San Francisco, CA, USA.
School of Medicine, University of California San Francisco, San Francisco, CA, USA.
Pharm Res. 2019 Sep 4;36(11):155. doi: 10.1007/s11095-019-2693-5.
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.
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.
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 of each treatment were similar and not statistically different. Mean max pH following the administration of food was 3.20 ± 0.55.
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.
本研究旨在确定食物对胃 pH 值的影响，以及在食物引起胃 pH 值升高后，非处方盐酸甜菜碱（BHCl）酸重新酸化胃 pH 值的能力。
这是一项开放标签的交叉临床试验研究（NCT02758015），纳入了 9 名受试者，他们被随机分配到 16 种可能的 4 期交叉序列中的 1 种，以确定食物和胃 pH 值与酸补充之间的影响和关系。受试者接受了不同剂量（1500mg、3000mg 和 4500mg）的盐酸甜菜碱（BHCl）补充剂，以确定在摄入食物引起胃 pH 值升高后，酸补充剂重新酸化胃 pH 值的能力。
在给予食物并导致胃 pH 值升高后，不给予酸补充剂恢复到基线胃 pH 值水平的时间为 49.7±14.0 分钟。给予 4500mg 的 BHCl 酸胶囊能够在大约 17.3±5.9 分钟内使胃 pH 值水平恢复到基线。每种治疗方法的 AUC 相似，且无统计学差异。给予食物后的平均最大 pH 值为 3.20±0.55。
在酸补充剂存在的情况下，食物升高和维持胃 pH 值的能力在整个研究中得到了证实。在给予食物后，需要给予 4500mg 的 BHCl 酸才能使胃 pH 值重新酸化。本研究详细说明了临床医生在给接受胃酸减少剂的患者用药时所面临的困难，因为建议与食物一起给药以避免胃副作用。
