摘要
目的研究氧化苦参碱缓释片在Beagle犬体内的代谢及其相对生物利用度。方法采用单剂量双周期自身交叉设计,分别给犬单剂量灌胃氧化苦参碱缓释片或胶囊,用LC-MS测定给药后的血浆中氧化苦参碱和其代谢物苦参碱浓度。结果氧化苦参碱缓释片中氧化苦参碱、代谢物苦参碱的相对生物利用度分别为(73.9±2.1)%和(122.0±11.7)%。结论以氧化苦参碱或代谢物苦参碱为统计指标,氧化苦参碱缓释片和胶囊在吸收程度上生物不等效。
Abstract
OBJECTIVE To study metabolism and relative bioavailability of oxymatrine sustained-release tablets in Beagle dogs.METHODS A cross-over design was used.Plasma concentration of oxymatrine and metabolite matrine were determined by LC/MS method after Beagle dogs were administrated with a single dose of 300 mg oxymatrine sustained-release tablets or oxymatrine capsules.RESULTS The relative bioavailability of oxymatrine and metabolite matrine in Beagle dogs were(73.9±2.1)% and(122.0±11.7)%,respectively.CONCLUSION Oxymatrine sustained-release tablets were unbioequivalent to oxymatrine capsules when the absorption of oxymatrine or its metabolite matrine was taken as the index.
关键词
氧化苦参碱缓释片 /
氧化苦参碱胶囊 /
苦参碱 /
相对生物利用度
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Key words
oxymatrine sustained-release tablets /
oxymatrine capsules /
matrine /
relative bioavailability
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王素军;王广基;李晓天;阮金秀;张振清.
氧化苦参碱缓释片在犬体内的代谢及其相对生物利用度[J]. 中国药学杂志, 2008, 43(02): 129-131
WNG Su-jun;WNG Gung-ji;LI Xio-tin;RUN Jin-xiu;ZHNG Zhen-qing.
Metabolism and Relative Bioavailability of Oxymatrine Sustained-Release Tablets in Beagle Dogs [J]. Chinese Pharmaceutical Journal, 2008, 43(02): 129-131
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参考文献
[1] JIAO X, SHEN Q Y. Research progress on clinic and pharmacology of Alkaloids of Sophora Flavescens[J] . Tradit Chin Drug Res Pharmcol (中药新药与临床药理),2002,13(9):192-194.
[2] LU L G,MAO Y M,ZENG M D,et al. Capsule oxymatrine in the treatment of chronic hepatitis B: A randomized double-blind placebo-controlled multicenter study(I)[J] .Chin Hepatol(肝脏),2002,7(4):218-221.
[3] MAO Y M,ZENG M D,LU L G,et al. Capsule oxymatrine in the treatment of chronic hepatitis B: A randomized double-blind placebo-controlled multicenter study(Ⅱ)[J] . Chin Hepatol(肝脏),2002,7(4):222-224.
[4] WANG S J,WANG G J,LI X T, et al. Phamacokinetics of oxymatrine in beagle dogs by LC-MS[J] . Chin J Clin Pharmacol The(中国临床药理学与治疗学),2004,9(7):751-754.
[5] WANG S J,WANG G J,LI X T,et al. Pharmacokinetics of oxymatrine and its metabolite in beagle dogs by LC-MS[J] . China J Chin Mater Med(中国中药杂志),2005,30(2):133-136.
[6] WANG S J,WANG G J,LI X T, et al. Simultaneous determination of oxymatrine and its active metabolite matrine in dog plasma by liquid chromatography-mass spectrometry and its application to pharmacokinetic studies[J] . J Chromatogr B,2005,817(2):319-325.
[7] WANG S J,WANG G J,LI X T,et al. Determination of matrine in beagle dog plasma by liquid chromatography electrospray ionization mass spectrometry and its application to pharmacokinetic studies[J] . Clin Pharmacol Exp Ther Asia,2005,2(1):64-67.
[8] XIE M Z, ZHOU W Z,ZHANG Y. Metabolism of oxymatrine[J] . Acta Pharm Sin (药学学报),1981,16 (7):481-486.
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脚注
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