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Nucleation and growth of crystalline nitrendipine in amorphous nanoparticle suspensions containing polymers

机译:含聚合物的无定形纳米颗粒悬浮液中结晶硝苯地平的形核和生长

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摘要

Purpose: To investigate the nucleation and growth of crystalline nitrendipine in amorphous nanoparticle suspensions containing polymers. Methods: The transformation process of nitrendipine nanoparticles from amorphous to its crystalline form was investigated using Raman spectroscopy and X-ray powder diffraction (XRPD) techniques. Moreover, the nucleation and crystal growth rate were quantitatively determined by image analysis with video recorded under polarized light microscope. Results: It was confirmed that the amorphous nanoparticles were easily transformed into crystalline phase. The rates of crystalline nucleation and growth were decreased with an increase in concentration of PEG 200 from 0% to 75%, and PVA concentration from 0.1% to 1%. However, a further increase in PVA concentration to 2% did not show a significant decrease in nucleation and crystal growth rate. When the drug concentration in organic phase was 30mg/ml, the nucleation rate is higher than that of 10mg/ml, however, it had no difference with 100mg/ml. There is no difference between 10mg/ml and 30mg/ml in nucleation rate, however, it slowed down when drug concentration increased to 100mg/ml. Conclusions: Nucleation and growth of crystalline nitrendipine in amorphous nanoparticle suspensions was investigated effectively using image analysis of polarized light micrographs, Raman spectroscopy and XRPD, and provides an indepth insight into solid state transformation of Pharmaceuticals during processing.
机译:目的:研究含聚合物的无定形纳米颗粒悬浮液中结晶硝苯地平的形核和生长。方法:利用拉曼光谱和X射线粉末衍射(XRPD)技术研究了尼群地平纳米颗粒从无定形到结晶形式的转变过程。此外,通过在偏光显微镜下记录的视频通过图像分析来定量确定成核和晶体生长速率。结果:证实了无定形纳米颗粒易于转化为结晶相。随着PEG 200的浓度从0%增加到75%,PVA的浓度从0.1%增加到1%,结晶成核和生长速率降低。但是,PVA浓度进一步增加到2%并没有显示出成核和晶体生长速率的显着降低。当有机相中的药物浓度为30mg / ml时,成核速率高于10mg / ml,而与100mg / ml相比无差异。 10mg / ml和30mg / ml之间的成核速率没有差异,但是,当药物浓度增加到100mg / ml时,其成核速度减慢。结论:使用偏光显微图像分析,拉曼光谱和XRPD图像分析有效地研究了非晶态纳米颗粒悬浮液中结晶硝苯地平的形核和生长,并提供了对制药过程中固态转化的深入了解。

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  • 来源
  • 会议地点 Xian(CN)
  • 作者单位

    Department of Pharmaceutics, School of Pharmaceutical Science, Shenyang Pharmaceutical University, No.103, WenhuaRoad, Shenyang 110016, China Department of Pharmaceutics and Analytical Chemistry, Faculty of Pharmaceutical Sciences, University of Copenhagen, Universitetsparken 2, 2100 Copenhagen, Denmark;

    Department of Pharmaceutics and Analytical Chemistry, Faculty of Pharmaceutical Sciences, University of Copenhagen, Universitetsparken 2, 2100 Copenhagen, Denmark;

    Department of Pharmaceutics, School of Pharmaceutical Science, Shenyang Pharmaceutical University, No.103, WenhuaRoad, Shenyang 110016, China;

    Department of Pharmaceutics and Analytical Chemistry, Faculty of Pharmaceutical Sciences, University of Copenhagen, Universitetsparken 2, 2100 Copenhagen, Denmark;

    Department of Pharmaceutics and Analytical Chemistry, Faculty of Pharmaceutical Sciences, University of Copenhagen, Universitetsparken 2, 2100 Copenhagen, Denmark;

  • 会议组织
  • 原文格式 PDF
  • 正文语种 eng
  • 中图分类 药剂学;
  • 关键词

    amorphous; crystalline; nucleation; image analysis; nitrendipine;

    机译:非晶态;结晶;成核;图像分析;硝苯地平;

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