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维拉帕米对P-糖蛋白底物罗丹明123经空肠黏膜透过性的影响 被引量:3

Effect of verapamil on the permeability of the P-glycoprotein substrate rhodamine 123 across the jejunal membranes
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摘要 目的:研究维拉帕米对肠黏膜P-糖蛋白(P-gp)的调控作用。方法:使用体外扩散池测定不同浓度维拉帕米对P-gp底物罗丹明123(R123)和荧光素钠(CF)经肠黏膜透过性的影响。R123和CF在接受室中的浓度用荧光分光光度法测定。结果:维拉帕米具有增加R123经吸收方向的透过性,并且减少分泌方向的渗透性。但实验浓度的维拉帕米对CF的肠道转运没有影响。结论:维拉帕米可通过对P-gp功能的抑制而用于改善受P-gp介导药物的吸收,有望提高此类药物的口服生物利用度。 Objective To investigate the role of verapamil in the regulation of P-glycoprotein (P-gp) across the jejunal membranes. Methods The effect of veraparmil at different concentrations on the permeability of rhodamine (R123) or fluorescein sodium (CF) across the jejunal membranes was evaluated using an in vitro diffusion chamber system. The concentration of R123 or CF in the receptor chamber was determined by fluorospectrophotometry. Results Verapamil increased the serosal-to-mucosal (S-M) transport of R123 but decreased its opposite transport; however, it had no impact on the transport of CF across the intestinal membranes. Conclusion Verapamil may improve the P-gp mediated-drug transport by inhibiting P-gp function, therefore, enhancing the oral bioavailability of the medications mediated by P-gp.
出处 《实用医学杂志》 CAS 北大核心 2009年第6期861-863,共3页 The Journal of Practical Medicine
基金 国家自然科学基金资助项目(编号:C03050205) 广东省科技计划项目(编号:2005B30101007)
关键词 P糖蛋白 维拉帕米 荧光素 罗丹明123 P-glycoprotein Verapamil Fluorescein sodium Rhodamine 123
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  • 1曾抗 李国锋 许重远 等.脂质体鬼臼毒素治疗尖锐湿疣的双盲随机对照试验[J].第一军医大学学报(J First Mil Med Univ/Di YiJun Yi Da Xue Xue Bao),1998,18(3):246-246.
  • 2[1]Lown KS, Mayo RR, Leichtman AB, et al. Role of intestinal Pglycoprotein (mdrl) in interpatient variation in the oral bioavailability of cyclosporine[J]. Clin Pharmacol Ther, 1997;62:248-260.
  • 3[2]Maggio-Price L, Shows D, Waggie K, et al. Helicobacter bilis infection accelerates and H. hepaticus infection delays the development of colitis in multiple drug resistance-deficient (mdrla-/-)mice[J]. Am J Pathol, 2002; 160:739-751.
  • 4[3]Hunter J, Jepson MA, Tsuruo T, et al. Functional expression of Pglycoprotein in apical membranes of human intestinal Caco-2cells. Kinetics of vinblastine secretion and interaction with modulators[J]. J Biol Chem, 1993;268:14991-14997.
  • 5[4]Sparreboom A, van Asperen J, Mayer U, et al. Limited oral bioavailability and active epithelial excretion of paclitaxel (Taxol)caused by P-glycoprotein in the intestine[J]. Proc Natl Acad Sci USA, 1997;94:2031-2035.
  • 6[5]Malingre MM, Richel DJ, Beijnen JH, et al. Coadministration of cyclosporine strongly enhances the oral bioavailability of docetaxel[J]. J Clin Oncol, 2001;19:1160-1166.
  • 7[6]Masuda S, Uemoto S, Hashida T, et al. Effect of intestinal P-glycoprotein on daily tacrolimus trough level in a living-donor small bowel recipient[J]. Clin Pharmacol Ther, 2000;68:98-103.
  • 8[7]Masuda S, Goto M, Kiuchi T, et al. Enhanced expression of enterocyte P-glycoprotein depresses cyclosporine bioavailability in a recipient of living donor liver transplantation[J]. Liver Transpl, 2003;9:1108-1113.
  • 9[8]Wetterich U, Spahn-Langguth H, Mutschler E, et al. Evidence for intestinal secretion as an additional clearance pathway of talinolol enantiomers: concentration-and dose-dependent absorption in vitro and in vivo[J]. Pharrn Res, 1996;13:514-522.
  • 10[9]Ueda CT, Lemaire M, Gsell G, et al. Apparent dose-dependent oral absorption ofcyciosporin A in rats[J]. Biopharmn Drug Dispos,1984;5:141-151.

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  • 1门晓媛,王一飞.几种药剂辅料的应用进展[J].中国医药工业杂志,2004,35(12):764-767. 被引量:11
  • 2代方国,罗仁,王宇光,夏成云,谭洪玲,肖成荣,赵永红,高月.甘遂配伍甘草对大鼠肝脏CYP3A2影响[J].第四军医大学学报,2005,26(10):951-953. 被引量:44
  • 3刘念,耿小平,熊茂明.P-糖蛋白抑制剂的研究进展[J].国外医学(药学分册),2006,33(2):107-110. 被引量:7
  • 4刘晓磊,唐靖,宋娟,何娟,徐萍,彭文兴.川芎嗪对大鼠灌服环孢素A药代动力学的影响[J].药学学报,2006,41(9):882-887. 被引量:16
  • 5He L,Liu GQ.Effects of various principles from Chinese herhal medicine on rhodamine123 accumulation in brain capillary endothelial cells.Acta Pharmacol Sin.2002 Jul;23(7):591-6.
  • 6Pavek P,Staud F,Fendrich Z,et al.Examination of the functional activity of P-glycoprotein in the rat placental barrier using rhodamine 123.J Pharmacol Exp Ther.2003,305(3):1239-1250.
  • 7Petriz J,O Connor JE,Carmona Mls,et al.rhodamine 123 an appropriate fluorescent probe to assess P-glycoprotein mediated multidrug resistance in vinblastine-resistant CHO cells.Anal Cell Pathol.1997,14(3):129-40.
  • 8Ryoko Yumoto,Teruo Murakami,Yuko Nakamoto.Transport of Rhodamine 123,a P-Glycoprotein Substrate,across Bat Intestine and Caco-2 Cell Monolayers in the Presence of Cytachrome P-450 3A-Related Compounds.The Journal of pharmacology and experimental therapeutics.1999,289(3):149-155.
  • 9Molden E.P-glycoprotein-a pump of significance for drug response.Tidsskr Nor Laegforen,2004,124(22):2921-2923.
  • 10Sakaeda T,Nakamura T,Okumura K.Pharmacogenetics of drug transporters and its impact on the pharmacotherapy.Curr Top Med Chem,2004,4(13):1385-1398.

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