期刊文献+

银杏叶片长期给药后对大鼠灌服氯沙坦的药代动力学影响 被引量:3

Effect of Ginkgo biloba talbes on the pharmacokinetics of intragastrically administered losartan in rats
下载PDF
导出
摘要 目的:研究银杏叶提取物(GBE)制剂银杏叶片长期给药后对大鼠灌服氯沙坦(Los)的药代动力学影响。方法:SD大鼠随机分为Los单用组,GBE+Los联合用药组。试验第1天起,联合用药组大鼠灌胃给予GBE 100mg/kg,共14d。单用组大鼠灌胃给予等量纯净水。第15天,单用药组大鼠灌胃给予Los 10mg/kg,GBE+Los联合给药组大鼠同时灌胃给予GBE 100mg/kg和Los 10mg/kg。于Los给药后0.5、1、2、3、4、6、8、10、12、24h从大鼠眼眦静脉丛取血。HPLC法测定血浆中Los及其活性代谢产物EXP3174的浓度,计算其主要药代动力学参数,并进行统计学分析。结果:合用GBE后,Los的各药代动力学参数差异无统计学意义。EXP3174的tmax显著缩短(P<0.05),Cmax、AUC0-8和AUC0-∞显著增加(P<0.01),CL显著降低(P<0.05),t1/2、MRT变化无统计学差异。结论:GBE能够影响EXP3174的体内代谢,但对Los的药代动力学过程影响没有统计学意义。 To investigate the possible effect of ginkgo biloba tablets which were prepared by Ginkgo biloba extracts (GBE) on the pharmacokinetics of losartan by intragastrically administering in rats. METHODS: SD rats were randomly divided into two groups (losartan group and GBE+losartan group). Rats in GBE losartan group were administered with GBE 100 mg/kg from day 1 to 14. On day 15, Rats in the losatan group were administered with losar- tan 10 mg/kg, and Rats in the GBElosartan group were added with GBE 100 mg/kg. Blood samples were collected from the angulus oculi veins at 0. 5,1,2, 3,4, 6,8, 10, 12, 24 h. The blood plasma concentration of losartan and EXP3174 were determined by HPLC. Main pharmacokinetic parameters were calculated and cornpared by statistical analysis. RESULTS.After coadministrating with GBE, there were no significantly different pharmacokinetic parameters of losartan were found. However, the t_max of EXP3174 was markedly decreased (P〈0.05). The C AUC0-sh, AUC0of EXP3174 were significantly increase (P〈0.01). And the CL of EXP3174 was markedly decreased (P〈0.01). There was no significantly changed of tl/2 and MRT about EXP3174. CONCLUSION: GBE can affect the metabolism of no significantly different ics of losartan. EXP3174, which were on the pharmacokinetics of losartan.
出处 《中国临床药理学与治疗学》 CAS CSCD 2011年第12期1326-1331,共6页 Chinese Journal of Clinical Pharmacology and Therapeutics
基金 上海市卫生局科研项目(2010228) 上海医院药学科研基金(2010-YY-02-20) 上海交通大学医学院药学科研基金(JYY0915)
关键词 银杏叶提取物 氯沙坦 细胞色素P450 药代动力学 Ginkgo biloba extracts Losartan CYP Pharmacokinetics
  • 相关文献

参考文献13

  • 1Sica DA, Gehr TW, Ghosh S. Clinical pharmacoki netics of losartan [J]. Clin Pharmacokinet, 2005, 44(8) :797-814.
  • 2Bailey DG, Dresser GK. Interactions between grapefruit juice and cardiovascular drugs [J]. Am J Cardiovasc Drugs,2004, 4(5) :281-297.
  • 3Mahadevan S, Park Y. Multifaceted therapeutic benefits of Ginkgo biloba L: chemistry, efficacy, safety, and uses [J].J FoodSic,2008, 73(1): R14 -19.
  • 4赵丰戎,赵丰文,孙连军.银杏叶胶囊合并综合康复训练治疗慢性精神分裂症临床观察[J].中国临床药理学与治疗学,2010,15(5):565-569. 被引量:3
  • 5Zhou S, Gao Y, Jiang W, et al. Interactions of herbs with cytochrome P450[J]. Drug Metab Rev, 2003, 35(1): 35-98.
  • 6Helium BH, Nilsen OG. In vitro inhibiton of CYP3A4 metabolism and P glycoprotein-mediated transport by trade herbal products [J]. Basic Clin Pharmaeol Toxicol,2008, 102(5) : 466-475.
  • 7Soldner A, Spahn-Langguth H, Mutschler E. HPLC assays to simultaneously determine the an- giotensimAT1 antagonist losartan as well as its main and active metabolite EXP3174 in biological material of humans and rats [J]. J Pharm Biomed Anal, 1998, 16(5):863-873.
  • 8韦阳,黄慧芳,邵庆翔,张美云,孙东升,王恪申,郝转业,陈建新,桑国卫.国产氯沙坦钾片的生物等效性研究[J].中国临床药理学杂志,2000,16(2):106-110. 被引量:9
  • 9李烈权.高效液相色谱荧光法测定人血浆氯沙坦浓度[J].中国民康医学,2008,20(15):1738-1738. 被引量:1
  • 10孙鲁宁,刘园园,赵燕荣,云昌宏,刘筱雪,丁黎.HPLC-MS法同时测定人血浆中氯沙坦及其代谢物EXP3174[J].药学与临床研究,2009,17(2):115-119. 被引量:8

二级参考文献28

  • 1乔海灵,田鑫,温强,张莉蓉,贾琳静,张启堂,郭玉忠,郜娜.替米沙坦片在健康人体的药代动力学和相对生物利用度[J].中国临床药理学杂志,2005,21(1):33-36. 被引量:7
  • 2张向阳,周东丰,张培琰,苏建民.银杏叶提取物对中枢神经系统的作用[J].国外医学(精神病学分册),1996,23(1):35-40. 被引量:88
  • 3石金钟,张秀英,张刚,杜希文,刘广志,常志杰,马东方,陈克政,王世强,李德恩.舒血宁合并治疗慢性精神分裂症双盲对照研究[J].临床精神医学杂志,1996,6(6):338-338. 被引量:2
  • 4杨平,王艳娇,李琳,孙进,何仲贵.氯沙坦钾胶囊与片在健康人体的生物等效性[J].中国临床药理学杂志,2006,22(6):436-439. 被引量:12
  • 5Tamaki T, Nishiyama A, Kimura S, et al. EXP3174: The major active metabolite of losartan [J].Cardiovasc Drug Rev, 1997, 15(2) : 122-136.
  • 6Soldner A, Spahn-Langguth H, Mutschler E. HPLC assays to simultaneously determine the angiotensin-AT1 antagonist losartan as well as its main and active metabolite EXP 3174 in biological material of humans and rats[ J ]. J Pharm Biomed Anal, 1998, 16 (5) :863-873.
  • 7Yeung PKF, Jamieson A, Smith G J, et al. Determination of plasma concentrations of losartan in patients by HPLC using solid phase extraction and UV deteetion[J]. Int J Pharm, 2000,204 ( 1-2 ) :17-22.
  • 8Farthing D, Sica D, Fakhry I, et al. Simple high-performance liquid chromatographic method for determination of losartan and E-3174 metabolite in human plasma, urine and dialysate [ J]. J Chromatogr B Biomed Sci Appl, 1997,704 (1-2) 374-378.
  • 9Polinko M, Riffel K, Song HC, et al. Simultaneous determination of losartan and EXP3174 in human plasma and urine utilizing liquid chromatography tandem mass speetrometry[J]. J Pharm Biomed Anal, 33 ( 2003 ) : 73-84.
  • 10Zhao LZ,Huang M,Chen J,et al.Induction of propranolol metabolism by Ginkgo biloba extract EGb 761 in rats[J].Curr Drug Metab,2006,7:577-587.

共引文献24

同被引文献57

  • 1Defeudis FV. Bilobalide and neuroprotection [J]. Pharmacol Res, 2002, 46 (6) : 565-568.
  • 2Smith JV, Luo Y. Studies on molecular mechanisms of Ginkgo biloba extract [J]. Appl Microbiol Biotechnol, 2004, 64 ( 4 ) : 465 -472.
  • 3Chang TK, Chen J, Yeung EY. Effect of Ginkgo biloba extract on procarcinogen-bioactivating human CYP 1 enzymes: identifi- cation of isor hamnetin, Kaempferol, and quercetin as potent in hibitors of CYP 1B 1 [J]. Toxicol Appl Pharmacol, 2006,213 ( 1 ): 18-26.
  • 4Rendic S. Summary of information on human CYP enzymes: hu- man P450 metabolism data [J]. Drug Metab Rev, 2002, 34 ( 1-2 ): 83-448.
  • 5Ding X, Kaminsky LS. human extra hepatic cytoc hromes P450: function in xenobiotic metabolism and tissue-selective chemical toxicity in the respiratory and gastrointestinal tracts [J]. Annu Rev PharmacolToxicol, 2003, 43: 149-173.
  • 6Plant NJ, Gibson GG. Evaluation of the toxicological relevance ofCYP3A4 induction [J]. Cult Opin Drug Discov Devel, 2003, 6 (1) : 50-56.
  • 7Rettie AE, Jones JP. Clinical and toxicological relevance of CYP2C9 : drug-drug interactions and pharmacogenetics [J]. Annu Rev Pharmacol Toxicol, 2005, 45 : 477-494.
  • 8Mahady GB. Ginkgo biloba for the prevention and treatment of cardiovascular disease: a review of the literature [J]. J Cardiovasc Nuts, 2002, 16 (4) : 21-32.
  • 9Ponto LL, Schultz SK. Ginkgo biloba extract: review of CNS ef- fects [J]. Ann Clin Psychiatry, 2003, 15 ( 2 ) : 109-119.
  • 10Deng Y, Bib C, Zhao LZ, et al. Induction of eytochrome P450 3A by the Ginkgo biloba extract and bilobalides in human and rat primary hepatocytes [J]. Drug Metab Lett, 2008, 2 ( 1 ) : 60-66.

引证文献3

二级引证文献9

相关作者

内容加载中请稍等...

相关机构

内容加载中请稍等...

相关主题

内容加载中请稍等...

浏览历史

内容加载中请稍等...
;
使用帮助 返回顶部