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熊果酸对大鼠体内瑞舒伐他汀的药代动力学影响 被引量:3

Effect of Ursolic Acid on Pharmacokinetics of Rosuvastatin in Rats
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摘要 目的:探讨熊果酸对大鼠体内瑞舒伐他汀的药代动力学影响。方法12只雄性 SD 大鼠(200~235 g)按随机数字表法分为2组,分别为单用瑞舒伐他汀组与瑞舒伐他汀合用熊果酸组,每组6只,以瑞舒伐他汀100 mg· kg^-1、熊果酸80 mg·kg^-1的剂量灌胃给药,两药合用时先熊果酸后瑞舒伐他汀相继灌胃。采用 LC-MS 测定血药浓度,比较2组间药代动力学参数。结果合用熊果酸后,瑞舒伐他汀药代动力学参数 Cmax、AUC0-t、AUC0-∞参数值分别增加163.02%、145.99%和157.55%,而 CLz/F 值降低了57.84%(P <0.05或 P <0.01)。结论熊果酸可影响大鼠体内瑞舒伐他汀的药代动力学特性。 Objective To study the effect of ursolic acid on the pharmacokinetics of rosuvasta-tin in rats.Methods Twelve male rats(200-235 g)were randomly given rosuvastatin alone(control group)or in combination with ursolic acid(treatment group),with 6 rats in each group.Rosuvastatin(100 mg·kg^-1 ),ursolic acid(80 mg·kg^-1 )were adiministered by intragastric adminis-tration.Combination of both recipes were adiministered first ursolic acid.LC-MS was used to determine the plasma concentrations of rosuvastatin.Pharmacokinetic parameters were compared between the two groups.Results Compared with control group,Cmax ,AUC0-t and AUC0-∞ parameters were respectively increased by 163.02%,145.99% and 157.55%,but CLz/F was decreased by 57.84% in treatment group(P 〈0.05 or P〈0.01).Conclusion Ursolic acid can affect the pharmacokinetic properties of rosuvastatin in rats.
出处 《南昌大学学报(医学版)》 CAS 2014年第2期1-4,共4页 Journal of Nanchang University:Medical Sciences
基金 国家自然科学基金青年项目(81202583) 江西省教育厅青年基金(GJJ12145)
关键词 熊果酸 瑞舒伐他汀 药代动力学 ursolic acid rosuvastatin pharmacokinetics
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  • 1Liu Jie. Oleanolic acid and ursolic acid: research perspectives[J]. J Ethnopharmacol, 2005,100(1/2) :92-94.
  • 2Hua W J, Hua W X, Fang H J. The role of OATP1B1 and BCRP in pharmacokinetics and DDI of novel statins[J]. Card- iovasc Ther,2012,30(5) :e234-e241.
  • 3Gui C, Obaidat A, Chaguturu R, et al. Development of a cell- based high-throughput assay to screen for inhibitors of organic anion transporting polypeptides 1B1 and 1B3[J]. Curt Chem Geuomics, 2010,4 : 1-8.
  • 4Cziraky M J,Willey V J,Mckenney J M,et al. Statin safety:an assessment using an administrative claims database[J]. Am J Cardiol, 2006,97 (SA) : 61 C-68C.
  • 5Soran H, Durrington P. Rosuvastatin : efficacy, safety and clini- cal effectiveness[J]. Expert Opin Pharmacot her, 2008,9 (12) : 2145-2160.
  • 6温文冰,成伙清,刘治军.他汀类药物与其他药物的相互作用[J].中国医院药学杂志,2008,28(4):298-301. 被引量:13
  • 7Neuvonen P J. Drug interactions with HMCr-CoA reductase in- hibitors(statins) : the importance of CYP enzymes, transporters and pharmacogenetics[J]. Curr Opin Investig Drugs, 2010,11 (3) :323-332.
  • 8Pasanen M K, Fredrikson H, Neuvonen P J, et al. Different effects of SLCO1B1 polymorphism on the pharmacokinetics of atorvastatin and rosuvastatin[J]. Clin Pharmacol Ther, 2007, 82 (6) : 726-733.
  • 9Choi J H,Lee M G,Cho J Y,et al. Influence of OATP1B1 gen- otype on the pharmacokinetics of rosuvastatin in Koreans[J]. Clin Pharmacol Ther,2008,83(2) :251-257.
  • 10Lu H,Choudhuri S,Ogura K,et al. Characterization of organ- ic anion transporting polypeptide lb2-null mice:essential role in hepatic uptake/toxicity of phalloidin and microcystin- LR[J]. Toxicol Sci, 2008,103(1) :35-45.

二级参考文献30

  • 1Shitara Y, Hirano M, Sato H, et al. Gemfibrozil and its glucuronide inhibit the organic anion transporting polypeptide 2 (OATP2/OATP1B1)-mediated hepatic uptake and CYP2C8-mediated metabolism of cerivastatin., analysis of the mechanism of the clinically relevant drug-drug interaction between cerivastatin and gemfibrozil[J]. J Pharmacol Exp Ther, 2004, 311 (1) : 228-236.
  • 2Christians U,Jacobsen W,Floren LC. Metabolism and drug interactions of 3-hydroxy-3-methylglutaryl coenzyme A reduetase inhibitors in transplant patients:are the statins mechanistically similar[J]. Pharmacol Ther, 1998,80(1 ):1-34.
  • 3Cohen LH,van Leeuwen RE,van Thiel, et al. Equally potent inhibitors of cholesterol synthesis in human hepatocytes have distinguishable effects on different cytochrome P450 enzymes [J]. Biopharm Drug Dispos,2000,21 (9) : 353-364.
  • 4Fujino H,Saito T,Tsunenari Y, et al. Metabolic properties of the acid and lactone forms of HMG-CoA reductase inhibitors[J]. Xenobiotica,2004,34(11-12):961-971.
  • 5Andrus MR. Oral anticoagulant drug interactions with statins:case report of fluvastatin and review of the literature[J]. Pharmacotherapy, 2004,24(2): 285-290.
  • 6Ahmad SL. Warfarin interaction[J]. Arch Intern Med, 1990, 150(11) :2407.
  • 7Jacobson TA. Comparative pharmacokinetic interaction profiles of pravastatin, simvastatin, and atorvastatin when coadministered with cytochrome P450 inhibitors[J]. Am J Cardiol,2004, 94(9) : 1140-1146.
  • 8Kanathur N, Mathai MG, Byrd RP Jr, et al. Simvastatin-diltiazem drug interaction resulting in rhabdomyolysis and hepatitis [J]. Tenn-Med,2001, 94(9): 339-341.
  • 9Lewin JJ, Nappi JM, Taylor MH . Rhabdomyolysis with concurrent atorvastatin and diltiazem [J]. Ann Pharmacother, 2002, 36(10): 1546-1549.
  • 10Prueksaritanont T, Zhao JJ, Ma B,et al. Mechanistic studies on metabolic interactions between gemfibrozil and statins[J]. J Pharmacol Exp Ther,2002,301 (3) :1042-1051.

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