| 微乳型丙泊酚纳米注射液的制备与评价 |
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| 引用本文： | 蔡伟惠,陈小平,金方.微乳型丙泊酚纳米注射液的制备与评价[J].中国新药杂志,2011(13). |
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| 作者姓名： | 蔡伟惠 陈小平 金方 |
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| 作者单位： | 上海医药工业研究院创新药物与制药工艺国家重点实验室;北京世桥生物制药有限公司; |
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| 基金项目： | 国家“重大新药创制”科技重大专项(2009ZX09301-007); 上海市优秀学科带头人计划(08XD14225); 上海市纳米科技专项(0952nm04500) |
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| 摘 要： | 目的:制备微乳型丙泊酚纳米注射液,并对其进行体内外评价,为新型微乳型纳米注射液研究提供参考。方法:使用可注射用乳化剂和油制备丙泊酚纳米注射液,旋转黏度计测定其黏度,动态光散射法测定其粒径和Zeta电位,透射电镜测定其显微外观,透析法测定其游离药物浓度,并研究其体外溶血性和Beagle犬体内药动学性质。结果:黏度为1.5×10-3 Pa.s,粒径为(22.7±10.2)nm,Zeta电位为-5.82 mV;透射电镜照片显示微乳粒子外观近球状,游离药物浓度为(17.9±0.8)μg.mL-1(n=3),不引起溶血的发生;微乳与脂肪乳主要药动学参数t1/2α分别为(1.506±0.994)和(2.512±2.122)min,t1/2β分别为(42.221±43.878)和(49.095±42.521)min,V1分别为(1.947±1.17)和(3.546±3.836)L.kg-1,CL分别为(0.218±0.07)和(0.219±0.068)L.min-1.kg-1,AUC0～t分别为(17.916±6.772)和(16.968±5.395)mg.min.L-1,AUC0～∞分别为(20.488±7.729)和(...
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| 关 键 词： | 丙泊酚 微乳 注射液 制备 评价 |
Preparation and evaluation of propofol injectable microemulsion |
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| CAI Wei-hui,CHEN Xiao-ping,JIN Fang.Preparation and evaluation of propofol injectable microemulsion[J].Chinese Journal of New Drugs,2011(13). |
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| Authors: | CAI Wei-hui CHEN Xiao-ping JIN Fang |
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| Institution: | CAI Wei-hui1,CHEN Xiao-ping2,JIN Fang1(1 Shanghai Institute of Pharmaceutical Industry,State Key Laboratory of New Drug and Pharmaceutical Process,Shanghai 200040,China,2 Beijing Shiqiao Biopharmaceutical Co.,Ltd.,Beijing 101301,China) |
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| Abstract: | Objective:Propofol injectable microemulsion was prepared and evaluated to provide some references for research and development of injectable microemulsion.Methods:Propofol injectable microemulsion was developed with injectable emulsifiers and oil.The viscosity,particle size,zeta potential and morphology were characterized,respectively,by rotation viscometer,dynamic light scattering and transmission electron microscope.The free propofol was determined by equilibrium dialysis method.The hemolytic activities a... |
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| Keywords: | propofol microemulsion injection preparation evaluation |
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