Department of Gastroenterology, First Affiliated Hospital of Anhui Medical University, Key Laboratory of Gastroenterology of Anhui Province, Hefei 230032, China.
Acta Pharmacol Sin. 2010 Apr;31(4):501-8. doi: 10.1038/aps.2009.191. Epub 2010 Mar 22.
To investigate the distribution of amoxicillin in the gastric juice and gastric mucosa of rats and to investigate the effects of proton pump inhibitor rabeprazole on amoxicillin concentrations in various compartments.
One hundred and sixty anesthetized rats were divided into five groups, and given intravenously different doses of amoxicillin or amoxicillin and rabeprazole. The pH value and volume of gastric juice was aspirated were measured and separated gastric mucosa was homogenized. The concentrations of amoxicillin in the plasma, gastric juice and gastric mucosa were measured by high performance liquid chromatography (HPLC).
The maximum concentrations of amoxicillin in gastric juice and gastric mucosa were significantly lower than those in plasma (P<0.001). Concentrations in the glandular stomach mucosa were higher than those in the forestomach mucosa. Rabeprazole did not significantly change the pharmacokinetic parameters of amoxicillin in the plasma and did not alter gastric antibiotic clearance or the gastric transfer fraction of amoxicillin in gastric juice. However, rabeprazole did increase the amoxicillin concentration and pH value in gastric juice and reduced the volume of the gastric juice.
Amoxicillin could penetrate the gastric mucosa and achieve therapeutic concentrations at the target site after transfer from the blood to the stomach. Rabeprazole increased the amoxicillin concentration in gastric juice by decreasing the gastric juice volume but did not affect its concentration in blood or gastric mucosa.
研究阿莫西林在大鼠胃液和胃黏膜中的分布，并探讨质子泵抑制剂雷贝拉唑对各部位阿莫西林浓度的影响。
将 160 只麻醉大鼠分为 5 组，分别静脉给予不同剂量的阿莫西林或阿莫西林和雷贝拉唑。测定胃液的 pH 值和体积，并抽吸胃黏膜，匀浆。采用高效液相色谱法（HPLC）测定血浆、胃液和胃黏膜中阿莫西林的浓度。
胃液和胃黏膜中阿莫西林的最高浓度明显低于血浆（P<0.001）。胃腺黏膜中的浓度高于贲门黏膜中的浓度。雷贝拉唑对阿莫西林在血浆中的药代动力学参数无显著影响，也不改变胃内抗生素清除率或阿莫西林在胃液中的胃转移分数。然而，雷贝拉唑确实增加了胃液中的阿莫西林浓度和 pH 值，减少了胃液的体积。
阿莫西林从血液转移到胃后，可穿透胃黏膜并在靶部位达到治疗浓度。雷贝拉唑通过减少胃液量来增加胃液中的阿莫西林浓度，但不影响其在血液或胃黏膜中的浓度。
