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用于提高难溶性药物溶出速率的淀粉大孔泡沫的制备

Preparation of starch macrocellular foam for increasing the dissolution rate of poorly water-soluble drugs.

作者信息

Zhao Ying, Wu Chao, Zhao Zongzhe, Hao Yanna, Xu Jie, Yu Tong, Qiu Yang, Jiang Jie

机构信息

a Pharmacy School, Liaoning Medical University, Linghe District , Jinzhou , Liaoning Province , P.R. China.

出版信息

Pharm Dev Technol. 2016 Sep;21(6):749-54. doi: 10.3109/10837450.2015.1055763. Epub 2015 Jul 13.

Abstract

Starch macrocellular foam (SMF), a novel natural bio-matrix material, was prepared by the hard template method in order to improve the dissolution rate and oral bioavailability of poorly water-soluble drugs. Nitrendipine (NDP) was chosen as a model drug and was loaded into SMF by the solvent evaporation method. SMF and the loaded SMF samples (NDP-SMF) were characterized by scanning electron microscopy, differential scanning calorimetry, X-ray powder diffraction and Fourier transform infrared spectroscopy. In vitro drug release studies showed that SMF significantly increased the dissolution rate of NDP. In vivo studies showed that the NDP-SMF tablets clearly increased the oral bioavailability of NDP in comparison with the reference commercial tablets. All the results obtained demonstrated that SMF was a promising carrier for the oral delivery of poor water-soluble drugs.

摘要

淀粉大孔泡沫材料(SMF)是一种新型天然生物基质材料,采用硬模板法制备,旨在提高难溶性药物的溶出速率和口服生物利用度。选择尼群地平(NDP)作为模型药物,通过溶剂蒸发法将其载入SMF。采用扫描电子显微镜、差示扫描量热法、X射线粉末衍射和傅里叶变换红外光谱对SMF和载药SMF样品(NDP-SMF)进行了表征。体外药物释放研究表明,SMF显著提高了NDP的溶出速率。体内研究表明,与参比市售片剂相比,NDP-SMF片剂明显提高了NDP的口服生物利用度。所有结果表明,SMF是一种用于口服递送难溶性药物的有前景的载体。

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