马来酸罗格列酮固体分散体及其溶出速率

Study on the solid dispersion of rosiglitazone maleate and its dissolution rate

目的提高难溶性药物马来酸罗格列酮的体外溶出速率 ,满足脉冲制剂的设计要求。方法选用PVPK3 0为载体 ,用溶剂法制备了马来酸罗格列酮固体分散体 ,比较考察了原料药及其物理混合物和固体分散体的溶出差别 ,并通过红外光谱及X 射线粉末衍射对固体分散体进行了鉴定。结果体外溶出结果表明固体分散体能显著增加药物在水中及人工肠液中的溶出速率 ;红外光谱分析结果表明药物与载体之间没有发生化学反应 ;X 射线粉末衍射图谱表明药物以无定形状态分散于载体PVPK3 0中。结论固体分散体体外溶出速率的提高可以满足脉冲制剂的设计要求。

Objective To improve the dissolution rate of rosiglitazone maleate and satisfy the demand for the design of the pulsatile dosage form. Methods The solid dispersion of rosiglitazone maleate was prepared using PVP K30 as a carrier by the solvent method; and the difference of the dissolution rate between the material drug, physical mixtures and solid dispersions was investigated; the solid dispersion was identified by IR spectra and X ray powder diffractograms. Results The dissolution rate of the drug in the solid dispersion was significantly increased in the distilled water and the simulated intestinal fluid; and the IR spectra showed that there were no chemical reactions between rosiglitazone maleate and PVP K30; the X ray powder diffractograms showed that the rosiglitazone maleate was dispersed amorphously in the solid dispersion. Conclusions The increase of the dissolution rate of the drug in the solid dispersion could satisfy the demand for the design of the pulsatile dosage form.