氟比洛芬对映体在类风湿性关节炎患者中的药代动力学。
The pharmacokinetics of the enantiomers of flurbiprofen in patients with rheumatoid arthritis.
作者信息
Young M A, Aarons L, Toon S
机构信息
Department of Pharmacy, University of Manchester.
出版信息
Br J Clin Pharmacol. 1991 Jan;31(1):102-4. doi: 10.1111/j.1365-2125.1991.tb03865.x.
Plasma and synovial fluid concentrations of the enantiomers of flurbiprofen were measured in 15 rheumatoid patients receiving 100 mg racemic flurbiprofen twice daily. Pharmacokinetic parameters showed considerable variability within the group of patients, although differences in S(+)/R(-) plasma concentration ratios were small. The average values (+/- s.d.) of oral plasma clearance, volume of distribution and elimination half-life for R(-)-flurbiprofen were 0.075 (+/- 0.066) l min-1, 12.47 (+/- 5.79) l and 138 (+/- 61) min, respectively. The average values (+/- s.d.) of oral plasma clearance, volume of distribution and elimination half-life for S(+)-flurbiprofen were 0.057 (+/- 0.035) l min-1, 12.81 (+/- 4.43) l and 155 (+/- 49) min, respectively. S(+)/R(-) ratios (+/- s.d.) rose from 1.06 (+/- 0.12) to 1.75 (+/- 0.61) at the end of the 12 h interval in plasma and from 1.18 (+/- 0.13) to 1.47 (+/- 0.24) over the measured time course in synovial fluid. Increases in S(+)/R(-) ratios may be clinically important as they demonstrate accumulation of the pharmacologically active species.
对15名每日两次服用100mg消旋氟比洛芬的类风湿性关节炎患者的血浆和滑液中氟比洛芬对映体的浓度进行了测定。药代动力学参数在患者组内显示出相当大的变异性，尽管S(+)/R(-)血浆浓度比的差异很小。R(-)-氟比洛芬的口服血浆清除率、分布容积和消除半衰期的平均值（±标准差）分别为0.075（±0.066）l min-1、12.47（±5.79）l和138（±61）min。S(+)-氟比洛芬的口服血浆清除率、分布容积和消除半衰期的平均值（±标准差）分别为0.057（±0.035）l min-1、12.81（±4.43）l和155（±49）min。在12小时间隔结束时，血浆中S(+)/R(-)比值（±标准差）从1.06（±0.12）升至1.75（±0.61），滑液中在所测时间过程中从1.18（±0.13）升至1.47（±0.24）。S(+)/R(-)比值的升高可能具有临床重要性，因为它们表明了药理活性物质的蓄积。
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