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Comparative pharmacokinetics and bioavailability of escin la and isoescin Ia after administration of escin and of pure escin Ia and isoescin Ia in rat

文献类型：期刊论文

作者Wu, Xiu-Jun3,4; Zhang, Meng-Liang2; Cui, Xiang-Yong2; Gao, Feng2; He, Qun2; Li, Xiao-Jiao2; Zhang, Ji-Wen1; Fawcett, J. Paul5; Gu, Jing-Kai2,3
刊名JOURNAL OF ETHNOPHARMACOLOGY
出版日期2012-01-06
卷号139期号:1页码:201-206
关键词Escin Ia Isoescin Ia Sodium escinate LC-MS/MS Pharmacokinetics Rat
ISSN号0378-8741
DOI10.1016/j.jep.2011.11.003
文献子类Article
英文摘要Ethnopharmacological relevance: Escin la and isoescin la have been traditionally used clinically as the chief active ingredients of escin, a major triterpene saponin isolated from horse chestnut (Aesculus hippocastanum) seeds for the treatment of chronic venous insufficiency, hemorrhoids, inflammation and edema. Aim of the study: To establish a sensitive LC-MS/MS method and investigate the pharmacokinetic properties of escin la and isoescin la in rats and the pharmacokinetics difference of sodium escinate with pure escin la and isoescin Ia. The absolute bioavailability of escin la and isoescin la and the bidirectional interconversion of them in vivo were also scarcely reported. Materials and methods: Wister rats were administrated an intravenous (i.v.) dose (1.7 mg/kg) of sodium escinate (corresponding to 0.5 mg/kg of escin la and 0.5 mg/kg of isoescin la, respectively) and an i.v. dose (0.5 mg/kg) or oral dose (4 mg/kg) of pure escin la or isoescin la, respectively. At different time points, the concentrations of escin la and isoescin la in rat plasma were determined by LC-MS/MS method. Main pharmacokinetic parameters including t(1/2), MRT, CL, V-d, AUC and F were estimated by non-compartmental analysis using the TopFit 2.0 software package (Thomae GmbH, Germany) and statistical analysis was performed using the Student's t-test with P<0.05 as the level of significance. Results: After administration of sodium escinate, the t(1/2) and MRT values for both escin la and isoescin la were larger than corresponding values for the compounds given alone. Absorption of escin la and isoescin la was very low with F values both <0.25%. Escin la and isoescin la were found to form the other isomer in vivo with the conversion of escin la to isoescin la being much extensive than from isoescin la to escin Ia. Conclusion: Comparison of the pharmacokinetics of escin Is and isoescin la given alone and together in rat suggest that administration of herbal preparations of escin for clinical use may provide longer duration of action than administration of single isomers. The interconversion of escin la and isoescin la when given alone indicates that administration of one isomer leads to exposure to the other. (C) 2011 Elsevier Ireland Ltd. All rights reserved.
WOS关键词AESCULUS-HIPPOCASTANUM L. ; HORSE-CHESTNUT ; BIOACTIVE SAPONINS ; BETA-ESCIN ; ALPHA-ESCIN ; SEEDS ; IB ; FORMULATIONS ; GLYCOSIDES ; CHINENSIS
资助项目National Natural Science Foundation[30772613] ; Chinese Academy of Sciences[KSCX2-YW-R-205] ; International Science and Technology Cooperation Project[S2010GR0920]
WOS研究方向Plant Sciences ; Pharmacology & Pharmacy ; Integrative & Complementary Medicine
语种英语
WOS记录号WOS:000299976900027
出版者ELSEVIER IRELAND LTD
源URL[http://119.78.100.183/handle/2S10ELR8/278222]  
专题药物制剂研究中心
通讯作者Gu, Jing-Kai
作者单位1.Chinese Acad Sci, Shanghai Inst Mat Med, Ctr Drug Delivery Syst, Shanghai 200031, Peoples R China;
2.Jilin Univ, Res Ctr Drug Metab, Changchun 130012, Peoples R China;
3.Jilin Univ, Hosp 1, Changchun 130012, Peoples R China;
4.Univ Tradit Chinese Med, Affiliated Hosp Liaoning, Shenyang, Peoples R China;
5.Univ Otago, Sch Pharm, Dunedin, New Zealand
推荐引用方式
GB/T 7714		 Wu, Xiu-Jun,Zhang, Meng-Liang,Cui, Xiang-Yong,et al. Comparative pharmacokinetics and bioavailability of escin la and isoescin Ia after administration of escin and of pure escin Ia and isoescin Ia in rat[J]. JOURNAL OF ETHNOPHARMACOLOGY,2012,139(1):201-206.
APA Wu, Xiu-Jun.,Zhang, Meng-Liang.,Cui, Xiang-Yong.,Gao, Feng.,He, Qun.,...&Gu, Jing-Kai.(2012).Comparative pharmacokinetics and bioavailability of escin la and isoescin Ia after administration of escin and of pure escin Ia and isoescin Ia in rat.JOURNAL OF ETHNOPHARMACOLOGY,139(1),201-206.
MLA Wu, Xiu-Jun,et al."Comparative pharmacokinetics and bioavailability of escin la and isoescin Ia after administration of escin and of pure escin Ia and isoescin Ia in rat".JOURNAL OF ETHNOPHARMACOLOGY 139.1(2012):201-206.

入库方式： OAI收割

来源：上海药物研究所

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