和厚朴酚-交联羧甲基纤维素钠表面固体分散体的制备及表征

Surface solid dispersion of honokiol-croscarmellose sodium:preparation and characterization

利用和厚朴酚熔点低的特点,以亲水性惰性交联羧甲基纤维素钠为载体材料,采用熔融法制备新型和厚朴酚表面固体分散体,对其溶出行为和稳定性进行初步的考察,并通过差示扫描量热法、X射线粉末衍射法、扫描电镜法等探究药物在载体中物相特征。结果表明,当和厚朴酚与交联羧甲基纤维素钠质量比为1∶2时,和厚朴酚表面固体分散体15 min溶出度大于90%,且药物平均溶出时间大幅缩短;在表面固体分散体中和厚朴酚以微晶形态分布在载体材料交联羧甲基纤维素钠的表面;初步稳定性试验结果显示,药物溶出速率未发生显著性变化。采用熔融法制得的表面固体分散体制备工艺简单,载药量高,药物以微晶形态存在,其体外溶出速率显著提高,可为和厚朴酚固体制剂的研究与开发提供新的思路和方法。

The surface solid dispersion of honokiol was prepared by melting method with croscarmellose sodium as carrier to improve the dissolution rate of honokiol,taking the advantage of its low melting point.The dissolution rate and stability test of surface solid dispersion of honokiol were carried out.Its physical properties were then investigated by DSC,PXRD and SEM analysis.The results indicated that the dissolution rate of honokiol from sodium solid dispersion was more than 90%at 15 min while its mean dissolution time was significantly decreased.Honokiol was distributed on the surface of croscarmellose sodium in the form of microcrystal;moreover,its dissolution behavior didn′t change significantly after six months of stability tests.Therefore,surface solid dispersion of honokionl could be prepared by simple process.The formed solid dispersion achieved high drug loading and fast in vitro dissolution rate,which could provide a novel idea for developing solid preparations of honokiol.