沈阳药科大学学报

2012, v.29;No.203(12) 909-912

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介孔复合硅微球的制备及载药性质
Synthesis of CaO-SiO_2-P_2O_5 microspheres and its feasibility as a drug carrier

边辰蔚,郑鑫,李乐道,常笛,姜同英,王思玲
BIAN Chen-wei1,ZHENG Xin2,LI Le-dao1,CHANG Di1,JIANG Tong-ying1,WANG Si-ling1(1.School of Pharmacy

摘要(Abstract):

目的制备介孔复合硅(CaO-SiO2-P2O5)微球,考察其作为水难溶性药物载体提高水难溶性药物的分散性及溶出度的优势。方法采用sol-gel方法制备介孔CaO-SiO2-P2O5微球,以扫描电镜及氮气吸附-脱附等方法分析表征载体的外观形貌、比表面积及孔径分布;选取尼莫地平为模型药物,以溶剂浸渍挥干法载药制得药物固体分散体;采用热分析、氮气吸附-脱附曲线分析以及溶出度实验研究药物固体分散体的基本性质。结果制得的复合硅载体的形貌近球状,粒径大小主要分布在3~6μm,载体的比表面积为637.34 m2.g-1,孔容为1.371 8 cm3.g-1,孔径分布主要集中在10~12 nm。当药物和载体的质量比为1:4时,药物能够被包埋分散于载体内部,且以无定型的形式存在,45 min尼莫地平累计溶出达80%。结论介孔CaO-SiO2-P2O5微球有望成为水难溶性药物的优良载体。
Objective To enhance the dispersibility and dissolution of poorly water-soluble drugs by using mesoporous bioactive glasses carrier.Methods A simple and effective synthesis process was developed for spherical mesoporous bioactive glasses with spherical shape,high specific surface areas and narrow pore size distributions.Nimodipine was chosen as model drug and the solid dispersion was characterized though nitrogen adsorption,differential scanning calorimetry and the dissolution experiment.Results SEM images showed the spherical shape of CSP with particle size of 3-6 μm.Nitrogen adsorption suggested a high specific surface areas reaching up to 637.34 m2 · g-1and a narrow pore size distribution between 10-12 nm.The existence form of nimodipine was changed during the drug loading process.The dissolution results indicated that the best ratio of drug to carrier was 1∶ 4 for nimodipine and the accumulated dissolution of nimodipine solid dispersions could reach about 80% within 45 min.Conclusions It is believed that CSP has a promising application value as a good carrier for poor water-soluble drug.

关键词(KeyWords): 介孔复合硅;CaO-SiO2-P2O5;微球;尼莫地平;溶出度
mesoporous compound silicon;CaO-SiO2-P2O5;microspheres;nimodipine;dissolution degrees

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作者(Author): 边辰蔚,郑鑫,李乐道,常笛,姜同英,王思玲
BIAN Chen-wei1,ZHENG Xin2,LI Le-dao1,CHANG Di1,JIANG Tong-ying1,WANG Si-ling1(1.School of Pharmacy

DOI: 10.14066/j.cnki.cn21-1349/r.2012.12.001

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