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目的 以羟丙基甲基纤维素 (HPMC E5LV)为载体材料制备HPMC 西沙必利固体分散体 ,通过提高模型药物的溶解度来改善药物的体外释放。方法 分别用乙醇和人工胃液将药物和载体材料溶解 ,使药物均匀分散在载体中 ,减压干燥除去溶剂得到HPMC 西沙必利固体分散物 ;用X射线粉末衍射法分别测定了纯载体材料、纯西沙必利、载体材料和西沙必利物理混合物以及载体材料和西沙必利固体分散体 4∶1的晶体衍射峰 ,以确定是否有晶体存在 ;分别考察纯西沙必利和HPMC 西沙必利固体分散体在水、人工胃液和人工肠液中的溶解度 ;分别以纯西沙必利和载体材料和西沙必利固体分散体制备了西沙必利缓释片并考察了其在水和人工胃液中的药物释放。结果 当载体与药物的比例达到 4∶1时 ,X射线衍射实验表明药物的晶体峰已经消失 ,形成无定型固体分散体 ;与西沙必利原料药相比 ,固体分散体中药物在人工胃液、水和人工肠液中的溶解度分别提高了 2 39 4%、1 32 6 %和 1 1 7 9%;体外药物释放结果表明 ,当以水和人工胃液为介质时 ,药物从固体分散体制备的缓释片中的释放速度要快于用纯原料药制备的缓释片中的释放速度 ,体外释药规律可以用Higuchi’s动力学方程描述。结论 以HPMC为载体材料与西沙必利制成固体分散体 ,可以通过改善药物?
OBJECTIVE To prepare hydroxypropyl methylcellulose (HPMC E5LV) as a carrier material for the solid dispersion of cisplatin HPMC and to improve the drug release in vitro by increasing the solubility of the model drug. Methods The drugs and carrier materials were dissolved in ethanol and artificial gastric juice, respectively, the drugs were uniformly dispersed in the carrier and the solvent was removed by drying under reduced pressure to obtain the solid dispersion of cisplatin HPMC. The pure carrier materials were determined by X-ray powder diffractometry Cisapride, a physical mixture of the support material and cisapride, and a 4: 1 crystal diffraction peak of the carrier material and the solid material dispersion of cisapride to determine whether crystals were present. The effects of pure cisapride and HPMC cisapride solid dispersion In water, artificial gastric juice and artificial intestinal juice. Cisapride sustained-release tablets were prepared with pure cisapride, carrier materials and cisapride solid dispersion, respectively, and their drug release in water and artificial gastric juice was investigated. Results When the ratio of carrier to drug reached 4: 1, X-ray diffraction experiments showed that the crystal peak of the drug had disappeared to form an amorphous solid dispersion. Compared with cisapride drug substance, Solubility in water and artificial intestinal fluid increased by 2 39 4%, 1 32 6% and 1 1 7 9%, respectively. In vitro drug release results showed that when water and artificial gastric fluid were used as medium, the solubility of the drug from the solid dispersion The release rate in release tablets is faster than in release tablets prepared with pure APIs and the in vitro release profile can be described by Higuchi’s kinetic equation. Conclusion HPMC as carrier material and cisapride made of solid dispersion, can improve the drug?