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布洛芬对映体在健康人体的药动学研究 被引量:4

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摘要 目的研究健康自愿者单次和多次口服布洛芬缓释胶囊后布洛芬对映体〔S-(+)-布洛芬(S-IBP)和R-(-)-布洛芬(R-IBP)〕的药动学。方法8名健康志愿者单次和多次口服300 mg布洛芬缓释胶囊后,测定布洛芬对映体的血药浓度。绘制药-时曲线并用DAS 2.0药动学程序进行室模型的拟合,求出药动学参数,比较单次给药和多次给药后布洛芬消旋体、S-IBP和R-IBP间各药动学参数的差异。结果8名健康志愿者单次和多次口服300 mg布洛芬缓释胶囊后,布洛芬消旋体及其对映体的体内过程均符合一室开放模型,权重系数为1/C2。健康人单次口服布洛芬消旋体后,体内S-IBP的药时曲线下面积(AUC0-t)和Cmax均较R-IBP大,消除率(CL/F)较R-IBP低,其他参数差异均无统计学意义。结论布洛芬对映体体内代谢过程存在立体选择性。
出处 《四川大学学报(医学版)》 CAS CSCD 北大核心 2010年第1期176-178,共3页 Journal of Sichuan University(Medical Sciences)
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  • 1Fornasini G, Monti N, Brogin G, et al. Preliminary pharmacokinetic study of ibuprofen enantiomers after administration of a new oral formulation (ibuprofen arginine) to healthy male volunteers. Chirality, 1997 . 9(3) :297-302.
  • 2Gabard B, Nirnberger G, Schiel H, et al. Comparison of the bioavailability of dexibuprofen administered alone or as part of racemic ibuprofen. Eur J Clin Pharmacol, 1995.48(6) : 505-516.
  • 3Lotsch J, Muth-Selbach U, Tegeder I, et al. Simultaneous fitting of R- and S-ibuprofen plasma concentrations after oral administration of the racemate. Br J Clin Pharmacol, 2001; 52 (4) :387-398.
  • 4Lee EJ, Williams K, Day R, etal. Stereoselective disposition of ibuprofen enantiomers in man. Br J Clin Pharmacol, 2004. 58 (7) :S759-764.
  • 5Jamali F, Singh NN, Pasutto FM, et al. Pharmacokinetics of ibuprofen enantiomers in humans following oral administration of tablets with different absorption rates. Pharm Res, 1988; 5 (1) :40-43.
  • 6向瑾,余勤,梁茂植,秦永平,南峰.柱切换高效液相色谱法测定人血浆中布洛芬对映体浓度[J].分析化学,2008,36(3):311-315. 被引量:8
  • 7林文辉,崔福德,吴斌,早川达,柳本ひとみ,猪爪信夫.布洛芬离体肝代谢中对映体间的相互作用[J].沈阳药科大学学报,2005,22(1):1-4. 被引量:4

二级参考文献24

  • 1曾苏,沈向忠.体内手性药物的测定[J].国外医药(合成药.生化药.制剂分册),1994,15(1):41-43. 被引量:1
  • 2王春祥,刘文英.HPLC非手性柱手性柱联用技术和直接进样法在体内手性药物分析中的应用[J].国外医学(药学分册),1997,24(1):6-10. 被引量:3
  • 3Itoh T, Maruyama J, Tsuda Y, et al. Stereoselective pharmacokinetics of ibuprofen in rats: effects of enantiomer-enantiomer interaction in plasma protein binding[J]. Chirality, 1997, 9:354 - 361.
  • 4Hage DS, Noctor TAG, Wainer IW. Characterization of the protein binding of chiral drugs by high-performance affinity chromatography: interaction of R- and S-ibuprofen with human serum albumin[J]. J Chromatogr A, 1995,693.23 - 32.
  • 5Baumgartner H, Schwarz HA, Blum W, et al. Ibuprofen and diclofenac sodium in the treatment of osteoarthritis:a comparative trial of two once-daily sustained-released NSAID formulations [J]. Current Medical Research and Opinion, 1996,13(8) :435 - 444.
  • 6Davies NM. Clinical pharrnacokinetics of ibuprofen. The first 30 years [J]. Clin Pharmacokinet, 1998, 34(2):101 - 154.
  • 7Zhou Q, Yao T, Zeng S. Effects of stereochemical aspects on drug interaction in pharmaeokinetics [ J ]. Acta Pharmacol Sin, 2002, 23 : 385 - 392.
  • 8Knihinicki RD, Williams KM, Day RO. Chiral inversion of 2-arylpropionic acid non-stereoidal anti-inflammatory drugs 1. In vitro studies of ibuprofen and flurbiprofen[J]. Biochem Pharmacol, 1989, 38 : 4389 - 4395.
  • 9Doki K, Hayakawa T, Lin W, et al. Effects of absorption rate on the pre-systemie chiral inversion of ibuprofen in rabbits[J]. J Pharm Pharmeol, 2003, 55:1091 -1097.
  • 10Lin W, Hayakawa T, Yanaguimoto H, et al. Pharmacokinetic interaction of ibuprofen enantiomers in rabbits[J].J Pharm Pharmacol, 2004:317 - 321.

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