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卡维地洛-中空介孔二氧化硅固体分散体的制备与表征

任丽霞, 王柏

任丽霞, 王柏. 卡维地洛-中空介孔二氧化硅固体分散体的制备与表征[J]. 中国药科大学学报, 2014, 45(1): 59-64. DOI: 10.11665/j.issn.1000-5048.20140110
引用本文: 任丽霞, 王柏. 卡维地洛-中空介孔二氧化硅固体分散体的制备与表征[J]. 中国药科大学学报, 2014, 45(1): 59-64. DOI: 10.11665/j.issn.1000-5048.20140110
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REN Lixia, WANG Bo. Preparation and characterization of carvedilol solid dispersions using hollow mesoporous silica nanoparticles[J]. Journal of China Pharmaceutical University, 2014, 45(1): 59-64. DOI: 10.11665/j.issn.1000-5048.20140110
Citation: REN Lixia, WANG Bo. Preparation and characterization of carvedilol solid dispersions using hollow mesoporous silica nanoparticles[J]. Journal of China Pharmaceutical University, 2014, 45(1): 59-64. DOI: 10.11665/j.issn.1000-5048.20140110
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卡维地洛-中空介孔二氧化硅固体分散体的制备与表征

  • 中国药科大学药剂学教研室

Preparation and characterization of carvedilol solid dispersions using hollow mesoporous silica nanoparticles

摘要

    摘要
  • 摘要: 制备中空介孔二氧化硅纳米粒子，并考察其载药性能以及对药物溶出度的影响。以难溶性药物卡维地洛为模型药物，以中空介孔二氧化硅为载体，无水乙醇为溶剂，采用溶剂浸渍挥干法制备卡维地洛固体分散体，通过透射电镜、扫描电镜、N2吸附-脱附、红外光谱、差示扫描量热法和X线粉末衍射法等表征其物相特征，并对其溶出行为和稳定性进行考察。结果显示，药物以无定型形式高度分散于中空介孔二氧化硅的内部和孔道中；当药物与载体的质量比为1∶5时，药物60 min累积溶出可达95%；经过3个月稳定性加速试验后，固体分散体中药物的溶出和含量未发生明显变化。以中空介孔二氧化硅作为难溶性药物固体分散体载体能显著改善药物的溶出，具有实际应用价值。
    Abstract: The aims of this study were to prepare hollow mesoporous silica nanoparticles(HMSNs)and to evaluate its effect on drug loading and dissolution. Carvedilol, a sparely water-insoluble drug has been selected as the model drug. Carvedilol solid dispersions were prepared by solvent evaporation method using HMSNs as the drug carrier and absolute alcohol as solvent. The solid dispersions were characterized by transmission electron microscope(TEM), scanning electron microscope(SEM), N2 adsorption-desorption, FT-IR spectroscopy, differential scanning calorimeter(DSC)and X-ray diffraction(XRD). In vitro drug release behavior and the short-term stability were also investigated. The results showed that drugs were highly dispersed into the hollow cores and mesopores of HMSNs in amorphous form. In addition, the results of in vitro dissolution testing showed that the accumulated dissolutions of carvedilol solid dispersions could reach 95% within 60 min, when the mass ratio of the drug and the carrier was 1 ∶5. 3-Month accelerated stability testing obesrved no significant changes to drug dissolution and content presented in the solid dispersions. The significant improvement of drug dissolution demonstrated that HMSNs could provide good reservoirs or carriers for sparely water-insoluble drugs, and have high potential in future applications for oral delivery of therapeutic drugs.
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    • 参考文献(17)
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  • 刊出日期:  2014-02-24

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