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吡罗昔康多次给药后的吡罗昔康和5'-羟基吡罗昔康动力学

Piroxicam and 5'-hydroxypiroxicam kinetics following multiple dose administration of piroxicam.

作者信息

Richardson C J, Blocka K L, Ross S G, Verbeeck R K

出版信息

Eur J Clin Pharmacol. 1987;32(1):89-91. doi: 10.1007/BF00609964.

DOI:10.1007/BF00609964
PMID:3582473
Abstract

Piroxicam (20 mg once daily) was administered orally to six healthy young volunteers for 15 days. Trough steady-state levels of piroxicam and 5'-hydroxypiroxicam were 5.5 and 1.2 micrograms/ml, respectively. Piroxicam's plasma half-life (54.9 h) was significantly shorter than that of 5'-hydroxypiroxicam (70.5 h). Percent unbound piroxicam and 5'-hydroxypiroxicam in plasma at steady-state averaged 1.10 and 8.07 respectively. An average of 25.2% of the dose was recovered in urine as 5'-hydroxypiroxicam; approximately two-thirds (17.2%) in the form of the glucuronide conjugate. Average steady-state plasma levels (Css) of piroxicam (7.0 micrograms/ml) were significantly higher than predicted from a previously reported single dose study (5.3 micrograms/ml).

摘要

对6名健康年轻志愿者口服吡罗昔康(每日1次,每次20毫克),持续15天。吡罗昔康和5'-羟基吡罗昔康的谷稳态水平分别为5.5和1.2微克/毫升。吡罗昔康的血浆半衰期(54.9小时)明显短于5'-羟基吡罗昔康(70.5小时)。稳态时血浆中未结合的吡罗昔康和5'-羟基吡罗昔康的百分比平均分别为1.10和8.07。平均25.2%的剂量以5'-羟基吡罗昔康的形式在尿液中回收;约三分之二(17.2%)为葡萄糖醛酸结合物形式。吡罗昔康的平均稳态血浆水平(Css)为7.0微克/毫升,明显高于先前报道的单剂量研究预测值(5.3微克/毫升)。

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本文引用的文献

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Synthesis and antiinflammatory activity of metabolites of piroxicam.吡罗昔康代谢产物的合成与抗炎活性
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Piroxicam. A reappraisal of its pharmacology and therapeutic efficacy.吡罗昔康。对其药理学和治疗效果的重新评估。
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Clinical pharmacokinetics of non-steroidal anti-inflammatory drugs.非甾体抗炎药的临床药代动力学
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The pharmacokinetics of piroxicam in elderly persons with and without renal impairment.吡罗昔康在有和没有肾功能损害的老年人中的药代动力学。
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Clinical pharmacokinetics of tenoxicam.替诺昔康的临床药代动力学
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Methotrexate disposition following concomitant administration of ketoprofen, piroxicam and flurbiprofen in patients with rheumatoid arthritis.类风湿性关节炎患者同时服用酮洛芬、吡罗昔康和氟比洛芬后甲氨蝶呤的处置情况。
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Oral bioavailability of CHF1194, an inclusion complex of piroxicam and beta-cyclodextrin, in healthy subjects under single dose and steady-state conditions.吡罗昔康与β-环糊精包合物CHF1194在健康受试者单剂量和稳态条件下的口服生物利用度。
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Plasma tenoxicam concentrations after single and multiple oral doses.
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Steady state pharmacokinetics of piroxicam in children with rheumatic diseases.吡罗昔康在风湿性疾病患儿中的稳态药代动力学。
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Single-dose and steady-state pharmacokinetics of piroxicam in elderly vs young adults.吡罗昔康在老年人与年轻人中的单剂量及稳态药代动力学
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Clin Pharmacol Ther. 1985 Jan;37(1):13-8. doi: 10.1038/clpt.1985.4.
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High-performance liquid chromatographic analysis of piroxicam and its major metabolite 5'-hydroxypiroxicam in human plasma and urine.人血浆和尿液中吡罗昔康及其主要代谢物5'-羟基吡罗昔康的高效液相色谱分析
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