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辛伐他汀微乳的制备及犬体内药物动力学

Preparation of Simvastatin Microemulsion and Pharmacokinetics in Dogs

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【作者】 孟健郑梁元

【Author】 MENG Jian~1, ZHENG Liang-yuan~(2*) (1. Pharmaceutical College of Shenyang Pharmaceutical University, Shenyang 110016; 2. Shanghai Xingkang Pharmaceuticals Research and Development Company, Shanghai 201203)

【机构】 沈阳药科大学药学院上海兴康医药研究开发有限公司 辽宁沈阳 110016上海 201203

【摘要】 以辛伐他汀在各种表面活性剂和油中的溶解度及不同体系的最大载油量为指标,筛选微乳处方。用伪三元相图确定微乳区,并以辛伐他汀片为参比制剂,考察辛伐他汀微乳在犬体内的相对生物利用度。结果表明,以Cremophor EL乃表面活性剂,Labrafac CC-Lauroglycol 90(6:4,w/w)混合油为油相制得的辛伐他汀微乳粒径为(45.1±6.4)nm,ζ电位乃(-17.7±4.3)mV,相对生物利用度为193%。

【Abstract】 The formulation of simvastatin microemulsion was optimized using the solubility of simvastatin in different surfactants and oils and the maximum loading of the oil in different systems as parameters. The microemulsion area was defined by pseudo-ternary phase diagram. The relatively bioavailability of the prepared microemulsion in dogs was examined with simvastatin tablets as control preparation, The panicles size andζpotential of the simvastatin microemulsion composed of Cremophor EL and Labrafac CC-Lauroglycol 90 (6:4, w/w)were (45.1±6.4)nm and (-17.7±4.3)mV. The relative bioavailability was 193%.

  • 【文献出处】 中国医药工业杂志 ,Chinese Journal of Pharmaceuticals , 编辑部邮箱 ,2007年11期
  • 【分类号】R96;R94
  • 【被引频次】9
  • 【下载频次】283
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