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丹参酮IIA与羟基磷灰石固体分散体的表征及稳定性

Characterization and Stability of Tanshinone IIA Solid Dispersions with Hydroxyapatite.

作者信息

Wang Xiaopan, Li Li, Huo Wei, Hou Lulu, Zhao Zhiying, Li Weiguang

机构信息

State Key Laboratory of Natural Medicines, China Pharmaceutical University, No. 24 tongjiaxiang, Nanjing 210009, China.

Department of Pharmacy, the Second Affiliated Hospital, Nanjing Medical University, No. 121 jiangjiayuan, Nanjing 210028, China.

出版信息

Materials (Basel). 2013 Mar 6;6(3):805-816. doi: 10.3390/ma6030805.

DOI:10.3390/ma6030805
PMID:28809341
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC5512800/
Abstract

Solid dispersions of tanshinone IIA (TanIIA) using hydroxyapatite (HAp) as the dispersing carrier (TanIIA-HAp SDs) were prepared by the solvent evaporation method. The formed solid dispersions were characterized by scanning electron microscopy (SEM), differential scanning calorimetry analysis (DSC), X-ray powder diffraction (XRPD) and Fourier transforms infrared (FTIR) spectroscopy. The dissolution rate and the stability of TanIIA-HAp SDs were also evaluated. DSC and XRPD showed that TanIIA was changed from a crystalline to an amorphous form. FTIR suggested the presence of interactions between TanIIA and HAp in solid dispersions. The result of an dissolution study showed that the dissolution rate of TanIIA-HAp SDs was nearly 7.11-folds faster than free TanIIA. Data from stability studies for over one year of TanIIA-HAp SDs performed under room temperature revealed no significant differences in drug content and dissolution behavior. All these results indicated that HAp may be a promising carrier for improving the oral absorption of TanIIA.

摘要

采用溶剂蒸发法制备了以羟基磷灰石(HAp)为分散载体的丹参酮IIA(TanIIA)固体分散体(TanIIA-HAp SDs)。通过扫描电子显微镜(SEM)、差示扫描量热分析(DSC)、X射线粉末衍射(XRPD)和傅里叶变换红外(FTIR)光谱对形成的固体分散体进行了表征。还评估了TanIIA-HAp SDs的溶出速率和稳定性。DSC和XRPD表明TanIIA从结晶形式转变为无定形形式。FTIR表明固体分散体中TanIIA与HAp之间存在相互作用。溶出度研究结果表明,TanIIA-HAp SDs的溶出速率比游离TanIIA快近7.11倍。在室温下对TanIIA-HAp SDs进行的一年多稳定性研究数据显示,药物含量和溶出行为没有显著差异。所有这些结果表明,HAp可能是一种有前途的载体,可用于改善TanIIA的口服吸收。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/736d/5512800/c092e1d22ada/materials-06-00805-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/736d/5512800/9dd17a548abd/materials-06-00805-g001.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/736d/5512800/b7546261227c/materials-06-00805-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/736d/5512800/0e78f04a36e6/materials-06-00805-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/736d/5512800/c092e1d22ada/materials-06-00805-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/736d/5512800/9dd17a548abd/materials-06-00805-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/736d/5512800/684d55f8dba9/materials-06-00805-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/736d/5512800/b01914bb4450/materials-06-00805-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/736d/5512800/b7546261227c/materials-06-00805-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/736d/5512800/0e78f04a36e6/materials-06-00805-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/736d/5512800/c092e1d22ada/materials-06-00805-g006.jpg

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