替硝唑固体分散体的制备及其体外释放特性研究

Preparation and In Vitro Dissolution Rate of Tinidazole Solid Dispersion

目的:利用固体分散技术制备替硝唑固体分散体,增加替硝唑溶解度和溶出速度。方法:以聚乙二醇(PEG)为载体材料,采用溶剂-熔融法制成固体分散体,测定表观溶解度,进行体外溶出试验,并采用差示扫描量热(DSC)法鉴别药物在固体分散体中的存在状态。结果:替硝唑的溶出度和表观溶解度随PEG的比例不同而不同,且溶出度随载体用量增加而增加。固体分散体的DSC曲线中替硝唑药物的特征熔融峰消失。结论:所制得的固体分散体能明显提高替硝唑的溶出度和表观溶解度。

OBJECTIVE： To prepare tinidazole solid dispersion using the technology of solid dispersion, and to increase the dissolubility and the dissolution rate of tinidazole. METHODS： Tinidazole solid dispersion were prepared by solvent evaporation fusion method using PEG 6000 or PEG 4000 as carriers. The apparent solubility and in vitro dissolution characteristics were studied. Differential scanning calorimetry （DSC） method was used to determine the status of tinidazole in solid dispersions. RESULTS： The in vitro dissolution and apparent solubility of TNZ varied with the difference in proportion and of PEG, and the dissolution increased with the increase of the amount of carrier. Characteristic melting peak of TNZ in DSC curve of solid dispersion disappeared. CONCLUSION： The apparent solubility and in vitro dissolution of TNZ solid dispersion were increased significantly.