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单剂量和多剂量噻洛芬酸在老年关节炎患者中的药代动力学。

The pharmacokinetics of single and multiple doses of tiaprofenic acid in elderly patients with arthritis.

作者信息

Hosie J, Hosie G A

出版信息

Eur J Clin Pharmacol. 1987;32(1):93-5. doi: 10.1007/BF00609965.

DOI:10.1007/BF00609965
PMID:3582474
Abstract

We have studied the single dose and steady-state pharmacokinetic of tiaprofenic acid in ten elderly arthritic patients living in the community (5 men and 5 women) taking 200 mg tid for 8 days. The mean area under the plasma concentration-time curves to 8 h (AUC (0-8)) did not alter significantly from day 1 to day 8 (77.25 to 79.61 micrograms X ml-1 X h). The mean terminal phase half-life (t1/2) was 2.05 h and 2.25 h on Days 1 and 8 respectively in patients in whom the calculations were possible (7 patients on Day 1 and 6 patients on Day 8). The median observed time of maximum concentration (tmax) and the mean observed maximum plasma concentration (Cmax) of 100 min and 21.3 micrograms X ml-1 respectively on Day 1 were not significantly different from the values obtained on Day 8 (tmax 120 min; Cmax 20.7 micrograms X ml-1). The kinetic data suggest that there should be no significant accumulation of tiaprofenic acid in elderly ambulant people suffering from arthritis.

摘要

我们研究了10名社区老年关节炎患者(5名男性和5名女性)单剂量及稳态下的替诺昔康药代动力学,这些患者每日3次服用200mg,共服用8天。血浆浓度-时间曲线下至8小时的平均面积(AUC(0 - 8))从第1天到第8天无显著变化(77.25至79.61微克·毫升⁻¹·小时)。在可进行计算的患者中(第1天7名患者,第8天6名患者),平均终末相半衰期(t1/2)在第1天和第8天分别为2.05小时和2.25小时。第1天观察到的最大浓度中位时间(tmax)为100分钟,平均观察到的最大血浆浓度(Cmax)为21.3微克·毫升⁻¹,与第8天获得的值(tmax 120分钟;Cmax 20.7微克·毫升⁻¹)无显著差异。动力学数据表明,替诺昔康在老年活动期关节炎患者中不应有显著蓄积。

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本文引用的文献

1
The pharmacokinetics of benoxaprofen in elderly subjects.老年人中苯恶洛芬的药代动力学。
Eur J Rheumatol Inflamm. 1982;5(2):69-75.
2
Tiaprofenic acid (surgam) in the treatment of osteoarthritis of the knee and hip.噻洛芬酸(苏灵大)治疗膝和髋骨关节炎
Rheumatol Rehabil. 1981 Aug;20(3):177-80. doi: 10.1093/rheumatology/20.3.177.
3
Short-term efficacy and tolerance of tiaprofenic acid ('Surgam') in rheumatoid arthritis and osteoarthritis: multi-centre, placebo-controlled trials.
Curr Med Res Opin. 1982;8(4):215-23. doi: 10.1185/03007998209109770.
4
Treatment of osteoarthritis: a 3-month comparison between tiaprofenic acid and indomethacin.骨关节炎的治疗:噻洛芬酸与吲哚美辛的3个月比较
Curr Med Res Opin. 1983;8(5):295-301. doi: 10.1185/03007998309112387.
5
A controlled trial of tiaprofenic acid versus ibuprofen in rheumatoid arthritis.噻洛芬酸与布洛芬治疗类风湿性关节炎的对照试验。
Rheumatol Rehabil. 1979 Nov;18(4):257-60. doi: 10.1093/rheumatology/18.4.257.