Channer K S, Roberts C J
Br J Clin Pharmacol. 1984 Aug;18(2):250-3. doi: 10.1111/j.1365-2125.1984.tb02464.x.
Twenty fasted patients were given hard gelatin capsules containing antipyrine and barium, and in ten patients the capsule arrested and disintegrated in the oesophagus. Plasma antipyrine was assayed at 10 min intervals for 1 h, then 30 min intervals for a further 3 h. The plasma concentration-time curves for the patients in whom the capsule entered the stomach rapidly, and for those in whom the capsule lodged in the oesophagus, were compared. The absorption in the first hour was calculated from the area under the plasma concentration-time curve and found to be significantly lower if the capsule disintegrated in the oesophagus (P less than 0.0005). The time to peak plasma concentration was delayed by an average of 46 min (P less than 0.01) and the peak plasma concentration was significantly lower (P less than 0.05) if delayed capsule transit occurred. Delayed capsule transit through the oesophagus significantly changed the pharmacokinetic profile of antipyrine.
给20名空腹患者服用含有安替比林和钡的硬明胶胶囊，其中10名患者的胶囊在食管内滞留并崩解。每隔10分钟测定一次血浆安替比林浓度，持续1小时，然后每隔30分钟再测定3小时。比较了胶囊迅速进入胃内的患者和胶囊滞留在食管内的患者的血浆浓度-时间曲线。根据血浆浓度-时间曲线下的面积计算第一小时的吸收量，发现如果胶囊在食管内崩解，吸收量显著降低（P小于0.0005）。如果出现胶囊转运延迟，血浆浓度达峰时间平均延迟46分钟（P小于0.01），且血浆峰浓度显著降低（P小于0.05）。胶囊在食管内的转运延迟显著改变了安替比林的药代动力学特征。
