Grimm Michael, Rump Adrian, Meilicke Lisa, Feldmüller Maximilian, Keßler Rebecca, Scheuch Eberhard, Tzvetkov Mladen Vassilev, Weitschies Werner
Department of Biopharmaceutics and Pharmaceutical Technology, University of Greifswald, 17489 Greifswald, Germany.
Department of Clinical Pharmacology, Bayer AG Pharmaceuticals, 13353 Berlin, Germany.
Pharmaceutics. 2023 Jan 18;15(2):328. doi: 10.3390/pharmaceutics15020328.
Gastric water emptying as a critical parameter for oral drug absorption can be investigated by several imaging techniques or by the interpretation of pharmacokinetics of appropriate substances. Recently introduced salivary caffeine kinetics is a valuable tool, but the required caffeine abstinence limits its applicability. To avoid the caffeine abstinence, stable isotope-labeled caffeine might be used, but the representability and transferability of kinetics for evaluation of gastric emptying must be demonstrated. Thus, salivary caffeine pharmacokinetics were compared for naturally occurring C-caffeine and C-caffeine after the administration of water under fasting conditions in six healthy young subjects. For this purpose, an ice capsule containing the two caffeine species was administered with 50 mL tap water. Gastric water emptying was simultaneously quantified using magnetic resonance imaging (MRI). Gastric emptying of 50 mL of water could be successfully evaluated. The salivary caffeine kinetics of C- and C-caffeine were nearly congruent and showed good linear correlations in all subjects, with a mean correlation coefficient of 0.96 in pooled data. Thus, the substitution of natural C caffeine with stable isotope-labeled C-caffeine offers the opportunity for broader application of the salivary caffeine gastric emptying technique and increases the robustness of the method against environmental contamination with caffeine.
胃排空作为口服药物吸收的关键参数,可以通过多种成像技术或通过对合适物质的药代动力学进行解释来研究。最近引入的唾液咖啡因动力学是一种有价值的工具,但所需的咖啡因戒断限制了其适用性。为避免咖啡因戒断,可以使用稳定同位素标记的咖啡因,但必须证明其动力学在评估胃排空方面的代表性和可转移性。因此,在六名健康年轻受试者禁食条件下饮水后,比较了天然存在的¹²C-咖啡因和¹³C-咖啡因的唾液咖啡因药代动力学。为此,将含有两种咖啡因的冰胶囊与50 mL自来水一起服用。同时使用磁共振成像(MRI)对胃排空进行定量。50 mL水的胃排空可以成功评估。¹²C-和¹³C-咖啡因的唾液咖啡因动力学几乎一致,并且在所有受试者中均显示出良好的线性相关性,汇总数据中的平均相关系数为0.96。因此,用稳定同位素标记的¹³C-咖啡因替代天然¹²C-咖啡因,为唾液咖啡因胃排空技术的更广泛应用提供了机会,并提高了该方法对咖啡因环境污染的稳健性。