...
  • 主题
高级搜索  >
历史搜索 清空历史
首页> 外文期刊>Journal of Microencapsulation: Microcapsules Liposomes Nanoparticles Microcells Microspheres >Micronisation of simvastatin by the supercritical antisolvent technique: in vitro-in vivo evaluation
【24h】

Micronisation of simvastatin by the supercritical antisolvent technique: in vitro-in vivo evaluation

机译：通过超临界抗溶剂技术将辛伐他汀微粉化：体内外评价

获取原文
获取原文并翻译 | 示例
           
页面导航
  • 摘要
  • 著录项
  • 相似文献
  • 相关主题

摘要

Micronisation of simvastatin dissolved in acetone, dimethyl sulfoxide and ethanol with supercritical carbon dioxide as antisolvent was successfully performed using a supercritical antisolvent technique. The effect of a few process parameters such as precipitation temperature, the pressure and solute concentration in the liquid solution has been studied to evaluate their influence on morphology and size of particles. The micronised simvastatin were evaluated for drug content, particle size analysis and in vitro dissolution profiles. Fourier transform infrared spectroscopy, differential scanning calorimetry and PXRD patterns was used to study the possible changes after micronisation of simvastatin. The dissolution rate was increased after micronised compared with pure simvastatin in distilled water, pH 1.2 buffer and pH 7.0 buffer. In vivo performance of the optimised formulation was evaluated in rats using pharmacodynamic marker parameters like serum total cholesterol (CH) and triglycerides (TG) for 21 days. Pharmacodynamic studies of micronised simvastatin revealed improved reduction in CH and TG values as compared with pure simvastatin indicating improved bioavailability. In vivo pharmacokinetics in rats showed an increase in bioavailability of micronised simvastatin (3.14 times) compared with plain simvastatin.
机译：使用超临界抗溶剂技术成功地将辛伐他汀溶解在丙酮，二甲基亚砜和乙醇中，并以超临界二氧化碳作为微溶剂进行了微粉化。研究了一些工艺参数的影响，例如沉淀温度，溶液中的压力和溶质浓度，以评估它们对颗粒形态和尺寸的影响。对微粉化的辛伐他汀进行药物含量，粒度分析和体外溶出度分析。傅里叶变换红外光谱，差示扫描量热法和PXRD图谱用于研究辛伐他汀微粉化后的可能变化。与纯辛伐他汀相比，微粉化后在蒸馏水中，pH 1.2缓冲液和pH 7.0缓冲液中的溶解速率增加。使用药效学指标参数（例如血清总胆固醇（CH）和甘油三酸酯（TG））在大鼠中评估优化配方的体内性能21天。微粉化的辛伐他汀的药效学研究表明，与纯辛伐他汀相比，CH和TG值的降低有所改善，表明生物利用度得到改善。与普通辛伐他汀相比，大鼠体内的药代动力学显示微粉化的辛伐他汀的生物利用度增加（3.14倍）。

著录项

相似文献

  • 外文文献
  • 中文文献
  • 专利
获取原文

客服邮箱：kefu@zhangqiaokeyan.com

京公网安备：11010802029741号 ICP备案号：京ICP备15016152号-6 六维联合信息科技 (北京) 有限公司©版权所有

  • 客服微信

  • 服务号