Channer K S, Roberts C J
Clin Pharmacol Ther. 1985 Jan;37(1):72-6. doi: 10.1038/clpt.1985.14.
Twenty patients awaiting cardiac catheterization swallowed a single tablet containing acetaminophen and barium sulfate. The first 11 subjects swallowed the tablet while supine; its progress down the esophagus was followed by fluoroscopy. In 10 of these subjects, transit of the tablet was delayed in the esophagus. The other nine subjects swallowed the tablet while standing; it entered the stomach immediately. The plasma concentration profile of acetaminophen was measured in all subjects. When there was delayed esophageal transit of tablets, the initial absorption of acetaminophen (measured as the AUC over the first 60 min) was lower than that after normal esophageal transit of tablets. The peak plasma acetaminophen concentration was also lower and occurred on average 70 min later when transit was delayed. These kinetic changes decrease the effectiveness of acetaminophen as an analgesic. We recommend that, to ensure rapid and complete drug absorption, patients be advised to swallow tablets with a large amount of water while standing.
20名等待心脏导管插入术的患者吞服了一片含有对乙酰氨基酚和硫酸钡的药片。前11名受试者仰卧位吞服该片；通过荧光透视观察其在食管中的下行过程。在这些受试者中，有10名的药片在食管中的传输延迟。另外9名受试者站立位吞服该片；它立即进入了胃。对所有受试者测量了对乙酰氨基酚的血浆浓度曲线。当药片在食管传输延迟时，对乙酰氨基酚的初始吸收（以最初60分钟的药时曲线下面积测量）低于药片在食管正常传输后的吸收。血浆对乙酰氨基酚的峰值浓度也较低，并且在传输延迟时平均延迟70分钟出现。这些动力学变化降低了对乙酰氨基酚作为镇痛药的有效性。我们建议，为确保药物快速和完全吸收，应建议患者站立位用大量水吞服药片。
