芦丁固体分散体的制备及其溶出性能研究

Preparation of rutin solid dispersion and dissolution properties

目的:采用固体分散技术,提高芦丁在水中的溶出,增强生物利用度。方法:采用7种载体(β-环糊精、聚乙烯吡咯烷酮、羟丙基纤维素、聚乙二醇6000、琥珀酸、乳糖、泊洛沙姆188),3种常用方法制备固体分散体,确定制备所选择的载体及方法;利用正交试验设计,以15 min时芦丁溶出度为指标成分,优化制备的具体工艺。并采用差示扫描量热法对分散体进行物相鉴别。利用相似因子法对固体分散体与其它混合物进行统计学评价;研究不同温度、不同浓度的固体分散体的溶解度,从化学热力学角度探讨固体分散体的形成机制。结果:以聚乙二醇6000为载体,溶剂熔融法,熔融时间1min、药物与载体比例1∶9、加热温度70℃为最佳方案;差示扫描量热法显示制备的固体分散体符合要求。相似因子法显示,固体分散体芦丁是分散在载体中。结论:聚乙二醇6000是提高芦丁溶出的理想载体,并表明固体分散体的形成为自发过程。

AIM： To improve the dissolution of rutin solid dispersions（RSD）,and enhance bioavailability.METHODS： RSD were prepared respectively by three methods with seven carriers（β-cyclodextrin,PVP,HPMC;Polyglycol 6000,succinic acid,lactose,and poloxamer 188）.With the method of orthogonal experiment design,choosing the 15 minute solubility of rutin as the index and the specific progress optimization for preparation,powder differential scanning calorimetry（DSC） were used to examine the physical and chemical characteristics of the solid dispersions.The similarity factor was used for statistical evaluation of RSD,and the other mixture.The solubility of RSD with different temperate and concent was studied in order to be discussed by the thermodynamic theory.RESULTS： The result showed that every method and carrier could enhance the solubility of RSD,expecial the PEG6000 as carrier and solvent evaporation-fusion method.The optimized preparation conditions were that the fusion time was 1 min,the ratio of rutin to carrier was 1 ∶ 9,temperature was 70 ℃.DSC showed that RSP was required.Method of similarity factor showed that rutin was dispersed in carrier.CONCLUSION： PEG6000 is a very useful carrier for improvement in the solubility of rutin and solution was a spontaneous process.