齐酞酸钠固体分散物的制备和体外溶出度研究  

Study on preparation and dissolution of solid dispersion of oleanolic acid 3β-phthalic monoester disodium salt

作　　者：蒋朝晖[1] 贾宪生[1] 麻秀萍[1] 

机构地区：[1]贵阳中医学院药学系,贵州贵阳550002

出　　处：《中国现代应用药学》2005年第1期53-55,共3页Chinese Journal of Modern Applied Pharmacy

基　　金：贵州省科学技术委员会攻关项目;黔科合(1998)9号

摘　　要：目的　采用固体分散技术提高齐酞酸钠口服制剂的溶出速度和稳定性。方法　以肠溶性材料聚丙烯酸树脂Ⅲ为载体,制备药物与载体不同比例的固体分散物及物理混合物,采用X 射线衍射方法、差热分析和红外光谱分析鉴别分散状态,并测定体外溶出速度。结果　齐酞酸钠以无定形态分散在载体中,主要在碱性溶液中溶出,形成肠溶性固体分散物,溶出速率高于物理混合物。结论　齐酞酸钠与载体适当比例的肠溶性固体分散物可明显提高体外溶出速率,并可防止药物的水解。OBJECTIVE The solid dispersion technique was used to enhance the dissolution rate and stability of peroral adiministration preparation of oleanolic acid 3β-phthalic monoester disodium salt(OAPS). METHOD Solid dispersions and physical mixtures with different proportion of weight of OAPS and polyacrylic resinⅢ(PRⅢ) were prepared by using PRⅢ as a carrier. The dispersive state of the drug were discriminated by X-ray powder diffraction analysis, DTA and IR. The dissolution rate of OAPS from solid dispersions and physical mixtures were also determined.RESULTS The results showed that the drug in the solid dispersion existed in amorphous form. The dissolution of OAPS from the solid dispersions were only a few in acid solutions(pH1.2) and were large amount in basicity solutions(pH7.8~8.0). The enteric solid dispersion were formed.CONCLUSION The dissolution rate of OAPS can be improved evidently by enteric solid dispersion with proper proportion of drug and carrier, and that enteric solid dispersion can prevent hydrolysis of drug.

关 键 词：齐酞酸钠 聚丙烯酸树脂Ⅲ X-射线衍射 差热分析 红外光谱法 溶出速度 

分 类 号：R512.6[医药卫生—内科学] TQ463[医药卫生—临床医学]