[1]罗德凤,叶建涛,张毅珊,等.人参皂苷Rd固体脂质纳米粒的体外释放和大鼠的在体吸收[J].中国药理学通报,2009,(07):0.
 LUO De feng,YE Jian tao,ZHANG Yi shan,et al.Studies on drug release in vitro and absorption in rat in vivo of ginsenoside Rd solid lipid nanoparticles[J].Chinese Pharmacological Bulletin,2009,(07):0.
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人参皂苷Rd固体脂质纳米粒的体外释放和大鼠的在体吸收()
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《中国药理学通报》[ISSN:/CN:]

卷:
期数:
2009年07期
页码:
0
栏目:
论著
出版日期:
2009-07-25

文章信息/Info

Title:
Studies on drug release in vitro and absorption in rat in vivo of ginsenoside Rd solid lipid nanoparticles
作者:
罗德凤叶建涛张毅珊刘德育
中山大学药学院,广东 广州510089
Author(s):
LUO Defeng YE Jiantao ZHANG Yishan LIU Deyu
School of Pharmaceutical Sciences, Sun Yatsen University, Guangzhou510089, China
关键词:
人参皂苷Rd固体脂质纳米粒体外释药肠吸收药物动力学血药浓度
Keywords:
ginsenoside Rd solid lipid nanoparticles drug release in vitro intestinal absorption pharmacokineticsplasma concentration
分类号:
R332;R 28271
文献标志码:
A
摘要:
目的研究人参皂苷Rd固体脂质纳米粒(RdSLN)的体外释药特性、在大鼠肠道的吸收和体内药物动力学行为。方法采用透析法测定RdSLN体外释药速率;通过大鼠在体分段肠回流实验,研究RdSLN的肠道吸收行为;建立血浆样品中人参皂苷Rd的HPLC分析方法,在大鼠灌胃给药后测定不同时间的血药浓度,观察RdSLN在体内的吸收和药动学特征。结果RdSLN具有缓释特征。在十二指肠和空肠段,RdSLN与人参皂苷Rd对照溶液的吸收率差异没有显著性;在回肠和结肠段,RdSLN与对照溶液的吸收率差异有显著性。RdSLN在回肠段的吸收率高于其它肠段。与对照组相比,RdSLN组的血药浓度水平维持时间更长,其Cmax、MRT、AUMC和AUC均明显增加。结论RdSLN具有一定的缓释作用,其在回肠的吸收优于其他肠段,并且能明显提高人参皂苷Rd的生物利用度。
Abstract:
AimTo investigate the release feature of ginsenoside Rd solid lipid nanoparticles (RdSLN) in vitro,and to clarify the difference in absorption of RdSLN from varied rat intestinal segments and pharmacokinetic properties in vivo. MethodsDialysis method was used to determine ginsenoside Rd release rate from nanoparticles in vitro. Perfusion method was used to study the intestinal absorption of RdSLN in rat. HPLC assay was established to determine the concentration of ginsenoside Rd in plasma. After intragastric administration, the concentrations of drug in rat blood at different time points were recorded to investigate the absorption and pharmacokinetics of RdSLN. ResultsThe release of ginsenoside Rd from RdSLN was slowed down and presented the property of sustained release. There was no significant difference between the absorption rate of RdSLN and control solution in duodenum and jejunum. However, it was obviously different in ileum and colon. Comparing with other intestinal segments, significantly higher percentage of RdSLN was absorbed in colon. In RdSLN group, the concentration of ginsenoside Rd in blood was maintained, and the Cmax,MRT,AUMC,and AUC were all increased. ConclusionsRdSLN possesses sustainedrelease effect. The colon is the preferable absorption site for RdSLN in intestinal tract. RdSLN can enhance the oral bioavailability of ginsenoside Rd.

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备注/Memo

备注/Memo:
收稿日期:2009-02-01,修回日期:2009-04-22基金项目:国家“十五”重大科技专项“创新药物和中药现代化”资助项目(No 2002AA2Z3228)作者简介:罗德凤(1981-),女,硕士,研究方向:中药新剂型及药理学,Tel:02039943057, Email:luodefeng18@163.com;刘德育(1953-),男,教授,硕士生导师,研究方向:中药新剂型及药理学,通讯作者,Tel/Fax:02039943057,Email: liudeyu@mail.sysu.edu.cn
更新日期/Last Update: 2009-07-25