Houston J B, Levy G
J Pharm Sci. 1976 Aug;65(8):1218-21. doi: 10.1002/jps.2600650822.
Oral administration of 3 g of ascorbic acid 1.5 hr after an oral dose of 1 g of acetaminophen caused a rapid and pronounced decrease in the excretion rate of acetaminophen sulfate in five healthy adult volunteers. There was a statistically significant increase in the fractions of the dose of acetaminophen excreted as such as as acetaminophen glucuronide but a decrease in the fraction excreted as acetaminophen sulfate. The apparent biological half-life of acetaminophen increased from 2.3 +/- 0.2 (mean +/- SD) to 3.1 +/- 0.5 hr. Concomitant administration of sodium sulfate prevented these effects. Ascorbic acid, which itself is metabolized in part to the sulfate, inhibits the conjugation of acetaminophen with sulfate by competing for available sulfate in the body.
在口服1克对乙酰氨基酚1.5小时后口服3克抗坏血酸，导致5名健康成年志愿者中对乙酰氨基酚硫酸盐的排泄率迅速且显著降低。以对乙酰氨基酚葡萄糖醛酸苷形式排泄的对乙酰氨基酚剂量分数有统计学意义的增加，但以对乙酰氨基酚硫酸盐形式排泄的分数减少。对乙酰氨基酚的表观生物半衰期从2.3±0.2（平均值±标准差）小时增加到3.1±0.5小时。同时给予硫酸钠可防止这些影响。抗坏血酸本身部分代谢为硫酸盐，通过竞争体内可用的硫酸盐来抑制对乙酰氨基酚与硫酸盐的结合。
