[1]郑小林,刘洪英,唐伟,等.苦参碱遥控释药胶囊近端小肠定点释放的药代动力学研究[J].陆军军医大学学报(原第三军医大学学报),2010,32(06):529-532.
 Zheng Xiaolin,Liu Hongying,Tang Wei,et al.Pharmacokinetics of matrine in proximal small intestine based on remote controlled capsule[J].J Amry Med Univ (J Third Mil Med Univ),2010,32(06):529-532.
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苦参碱遥控释药胶囊近端小肠定点释放的药代动力学研究(/HTML )
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陆军军医大学学报(原第三军医大学学报)[ISSN:1000-5404/CN:51-1095/R]

卷:
32卷
期数:
2010年第06期
页码:
529-532
栏目:
论著
出版日期:
2010-03-30

文章信息/Info

Title:
Pharmacokinetics of matrine in proximal small intestine based on remote controlled capsule
作者:
郑小林刘洪英唐伟皮喜田侯文生周承文
重庆大学:生物工程学院生物医学工程系,微系统研究中心;第三军医大学西南医院设备科
Author(s):
Zheng Xiaolin Liu Hongying Tang Wei Pi Xitian Hou Wensheng Zhou Chengwen
College of Bioengineering, Microsystem Research Center, Chongqing University, Chongqing, 400030; Department of Equipment, Southwest Hospital, Third Military Medical University, Chongqing, 400038, China
关键词:
缓释制剂苦参碱投药局部药代动力学色谱法高效液相
Keywords:
sustained-release preparations administration topical matrine pharmacokinetics chromatography high performance liquid
分类号:
R282.71;R944.9;R969.1
文献标志码:
A
摘要:
目的   研究苦参碱在健康志愿者近端小肠内定点释放后的药代动力学特征。   方法   用自主研制的遥控释药胶囊系统,将200 mg苦参碱定位释放于志愿者的近端小肠内。用高效液相色谱法,以槐果碱为内标,甲醇-水-乙二胺(70∶30∶0.02)为流动相,测定志愿者血浆中苦参碱的含量。采用3p87程序计算药代动力学参数。   结果   近端小肠定点释放苦参碱的药代动力学符合二室开放模型,Cmax为10.52 μg/ml,Tmax为2.08 h,T1/2α和T1/2β分别为0.90 h和9.02 h,AUC(0-t) 为91.90 μg·h /ml。   结论   苦参碱在健康人近端小肠段定位释放后,小肠对苦参碱有明显的吸收且吸收过程呈二室模型分布。
Abstract:
Objective   To investigate the pharmacokinetics of remote controlled capsule for matrine in the proximal small intestine of healthy volunteers and obtain the standard pharmacokinetic parameters.    Methods   A total of 200 mg matrine was delivered in the proximal small intestine of 12 healthy male volunteers by remote controlled capsule system, which made by our work group. Blood sample of 3 ml for each time was harvested respectively in 0, 0.5, 1.0, 1.5, 2.0, 4.0, 6.0, 8.0, 12.0, 16.0, 24.0, 30.0 and 36.0 h after the matrine was released when the capsule entered into the proximal small intestine. HPLCUV was used to measure matrine concentrations in the plasma by adding an internal standard (sophocarpine). Methanol-water-ethylenediamine (70∶30∶0.02) was used as the mobile phase. The main parameters were calculated by 3p87 pharmacokinetic program.    Results   The martine pharmacokinetics conforms to a twocompartment open model after a single delivery of martine at a dose of 200 mg in upper small intestine of healthy volunteers. The main parameters were as follows: Cmax was 10.52 μg/ml, Tmax was 2.08 h, T1/2α was 0.90 h, T1/2β was 9.02 h, K12 was 0.21 h, K21 was 0.53 h, K10 was 0.12 h, MRT(0-t) was 11.56 h and AUC(0-t) was 91.90 μg·h/ml.    Conclusion   There is an effective absorption when matrine is site-specific delivered in the proximal small intestine. The process in vivo fits well to two compartment open model.

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更新日期/Last Update: 2010-03-24