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[口服阿明洛芬(米那芬)在老年类风湿性关节炎和变形性脊柱炎患者中的药代动力学]

[Pharmacokinetics of oral alminoprofen (Minalfen) in elderly patients with rheumatoid arthritis and spondylosis deformans].

作者信息

Shin K, Takasaki M, Katsunuma H, Sato K, Shibuya T, Sato S, Hirayama H

机构信息

Department of Geriatric Medicine, Tokyo Medical College.

出版信息

Nihon Ronen Igakkai Zasshi. 1992 Nov;29(11):881-7. doi: 10.3143/geriatrics.29.881.

DOI:10.3143/geriatrics.29.881
PMID:1491485
Abstract

The pharmacokinetics of oral Alminoprofen, a nonsteroidal anti-inflammatory drug, were studied in five elderly patients with rheumatoid arthritis and spondylosis deformans after 200 mg (three times a day) repeated dose for 5 days. The pharmacokinetic parameters after oral administration of Alminoprofen were analyzed by the one-compartment open model method. The maximum plasma concentrations (Cmax) were 16.1 +/- 2.5 micrograms/ml, after dosing on day 1, 25.2 +/- 1.6 micrograms/ml on day 3 and 21.6 +/- 2.7 micrograms/ml on day 5. The maximum time (Tmax) were about 2 hours after the medication in al cases. The area under the curve in drug concentration in plasma versus time (AUC) were 58.5 +/- 6.3 micrograms hr/ml on day 1, 58.5 +/- 3.1 micrograms hr/ml on day 3 and 58.1 +/- 8.5 micrograms hr/ml on day 5. The biological half-lives (t1/2) were 2.45 +/- 0.35, 2.09 +/- 0.82 and 2.49 +/- 0.63 hours, after dosing on day 1, day 3 and day 5, respectively. The analysis of moment in pharmacokinetics revealed that the mean residence time (MRT) on day 1, day 3 and day 5 observed were 2.31 +/- 0.03, 2.15 +/- 0.09 and 2.15 +/- 0.07 hours, respectively. The variance residence times (VRT) observed were 0.95 +/- 0.05 hour2 on day 1, 0.88 +/- 0.09 hour2 on day 3 and 1.06 +/- 0.07 hour2 on day 5. The ratios of accumulation calculated were 1.16 +/- 0.05 in both the morning medication on day 3 day 5, and it therefore appears that the steady-state equilibrium is established within 3 days after commencement of dosage.(ABSTRACT TRUNCATED AT 250 WORDS)

摘要

对5例类风湿性关节炎和变形性脊柱炎老年患者,在重复给予200毫克(每日3次)的阿明洛芬5天后,研究了其口服后的药代动力学。采用单室开放模型方法分析阿明洛芬口服给药后的药代动力学参数。第1天给药后,血浆最大浓度(Cmax)为16.1±2.5微克/毫升,第3天为25.2±1.6微克/毫升,第5天为21.6±2.7微克/毫升。所有病例用药后最大时间(Tmax)约为2小时。血浆药物浓度-时间曲线下面积(AUC)在第1天为58.5±6.3微克·小时/毫升,第3天为58.5±3.1微克·小时/毫升,第5天为58.1±8.5微克·小时/毫升。第1天、第3天和第5天给药后的生物半衰期(t1/2)分别为2.45±0.35、2.09±0.82和2.49±0.63小时。药代动力学矩分析显示,第1天、第3天和第5天观察到的平均驻留时间(MRT)分别为2.31±0.03、2.15±0.09和2.15±0.07小时。观察到的变异驻留时间(VRT)在第1天为0.95±0.05小时²,第3天为0.88±0.09小时²,第5天为1.06±0.07小时²。第3天和第5天早晨用药时计算的蓄积比均为1.16±0.05,因此似乎在开始给药后3天内达到稳态平衡。(摘要截取自250字)

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