Department of Pharmaceutical Sciences, College of Pharmacy and Health Sciences, Butler University, IN 46208, USA.
Gastroenterology and Hepatology Unit, Department of Medical Sciences, Uppsala University, Uppsala University Hospital, Uppsala SE-75185, Sweden.
Int J Pharm. 2022 Sep 25;625:122069. doi: 10.1016/j.ijpharm.2022.122069. Epub 2022 Jul 30.
Food can alter drug bioavailability through gastric pH changes. Time spent at gastric pH ranges is reported here, including variability data following ingestion of a light, mixed, 260 kcal meal. pH data was obtained for 20 healthy subjects undergoing SmartPill™ wireless motility capsule investigations on three separate visits. Gastric phase pH was sorted into pH < 2, 2-3, 3-4, 4-5 and > 5. All visits and all subjects were pooled to determine median time (25-75th percentiles) in minutes. Gastric emptying time was 176 (137-205) min with the majority of time, 111 (67 - 163), spent at pH < 2. Times spent at pH 2-3 and 3-4 were similar: 17 (5.7 - 35.6) and 18 (7.2-29.3). Time spent at pH 4-5 was 9 (1.3-20.6) and at pH > 5 was 0.7 (0-4.4). Intra-subject variability as determined by robust coefficient of variation (RCV)% was 30 % for pH < 2, 57 % for pH 2-3, 71 % for pH 3-4, 106 % for pH 4-5 and 144 % for pH > 5. Inter-subject variability RCV% was 49 % for pH < 2, 89 % for pH 2-3, 54 % for pH 3-4, 97 % for pH 4-5 and 148 % for pH > 5. Inter-subject variability can be up to approximately twofold higher than intra-subject variability at the lower pH ranges.
食物可通过改变胃内 pH 值来影响药物的生物利用度。本研究报告了不同时间内胃内 pH 值的范围，包括摄入 260 卡路里轻食后出现的变异性数据。对 20 名健康受试者进行了 SmartPill™无线动力胶囊研究，在 3 次不同访问中获得了 pH 值数据。胃期 pH 值被分为 pH 值<2、2-3、3-4、4-5 和>5。将所有访问和所有受试者进行汇总，以确定分钟中位数（25-75 百分位数）。胃排空时间为 176（137-205）min，大部分时间（111（67-163））在 pH 值<2 时。pH 值为 2-3 和 3-4 的时间相似：17（5.7-35.6）和 18（7.2-29.3）。pH 值为 4-5 的时间为 9（1.3-20.6），pH 值>5 的时间为 0.7（0-4.4）。通过稳健变异系数（RCV）%确定的个体内变异性为 pH 值<2 时为 30%，pH 值为 2-3 时为 57%，pH 值为 3-4 时为 71%，pH 值为 4-5 时为 106%，pH 值>5 时为 144%。个体间变异性 RCV%为 pH 值<2 时为 49%，pH 值为 2-3 时为 89%，pH 值为 3-4 时为 54%，pH 值为 4-5 时为 97%，pH 值>5 时为 148%。个体间变异性在较低的 pH 值范围内可能是个体内变异性的两倍左右。
