Täuber U, Weiss C, Krause W, Acksteiner B, Matthes H
Eur J Drug Metab Pharmacokinet. 1985 Jan-Mar;10(1):41-53. doi: 10.1007/BF03189696.
The absorption, disposition, biotransformation and excretion of the nonsteroidal anti-inflammatory drug pirazolac were investigated in 6 volunteers (3 males, 3 females, age 50 greater than years) after intravenous and oral administration of 50 mg 14C-pirazolac as an aqueous solution of the sodium salt. Pirazolac was very rapidly and completely absorbed and bioavailable when orally administered in a dose of 50 mg in solution. Maximum pirazolac levels in plasma of 6 micrograms/ml (30% of dose in total plasma volume) were already reached after approx. 20 minutes. No metabolites were detectable in the plasma. Pirazolac was eliminated from the plasma in two phases with half-lives of 3 hours and 16 hours, respectively, regardless of administration route. After intravenous and oral administration approximately 80% of the dose was excreted with the urine and approximately 15% with the feces within 7 days, indicating a complete excretion of 14C-radioactivity. In urine, approximately 10% of the dose was identified as unchanged pirazolac and 70% as pirazolac ester glucuronide.
在6名志愿者（3名男性，3名女性，年龄大于50岁）中，静脉注射和口服50mg 14C-吡唑酸（以钠盐的水溶液形式）后，对非甾体抗炎药吡唑酸的吸收、分布、生物转化和排泄进行了研究。当以50mg溶液口服给药时，吡唑酸吸收非常迅速且完全，具有生物利用度。约20分钟后，血浆中吡唑酸的最高水平达到6微克/毫升（占总血浆体积中剂量的30%）。血浆中未检测到代谢产物。无论给药途径如何，吡唑酸从血浆中消除分两个阶段，半衰期分别为3小时和16小时。静脉注射和口服给药后，约80%的剂量在7天内随尿液排出，约15%随粪便排出，表明14C放射性完全排出。在尿液中，约10%的剂量被鉴定为未变化的吡唑酸，70%为吡唑酸酯葡萄糖醛酸。
