超临界CO_2抗溶剂法制备谷维素/PVP-K30固体分散体  

Preparation of Oryzanol/PVP-K30 Solid Dipersions by Supercritical CO_2 Anti-Solvent Technology

作　　者：朱甜[1] 缪虹刚 林文[1] 王志祥[1] 黄德春[1] 颜庭轩[1] 

机构地区：[1]中国药科大学制药工程教研室,江苏南京210009

出　　处：《今日药学》2015年第2期86-89,95,共5页Pharmacy Today

基　　金：江苏省自然科学基金资助项目(BK2012763)

摘　　要：目的制备谷维素/PVP-K30固体分散体,提高谷维素的体外溶出度。方法采用超临界CO2抗溶剂法,以回收率为主要评价指标,在单因素试验的基础上设计正交试验优选制备谷维素/PVP-K30固体分散体的工艺,对最优工艺下得到的复合物进行红外光谱(IR)及扫描电镜(SEM)的表征,并测定其体外溶出度。结果制备谷维素/PVP-K30的最优工艺为:谷维素质量浓度14 mg/m L,结晶压力14 MPa,结晶温度55℃,溶液体积流量0.9 m L/min。此条件下产品平均回收率为88.22%,IR和SEM表明固体分散体中谷维素可能与PVP-K30发生氢键作用并以无定型形式存在,体外溶出度实验表明谷维素/PVP-K30固体分散体能显著提高谷维素的体外溶出度。结论超临界CO2抗溶剂法制备维素/PVP-K30固体分散体工艺可行,谷维素溶出度显著提高。OBJECTIVE To improve the in vitro dissolution rate of oryzanol,oryzanol / PVP-K30 solid dispersions were prepared.METHODS With recovery rate and drug-loading rate as the main evaluation indexs,on the basis of single factor experiments,orthogonal experimental design was used to optimize the preparation process of oryzanol / PVP-K30 solid dispersions by supercritical CO2anti-solvent technology. The experiments such as DSC,IR,SEM and in vitro dissolution were used to analyze the optimal process combination. RESULTS The orthogonal experimental optimization process conditions were set as follows： mass concentration of oryzanol 14 mg / m L,crystallization pressure 14 MPa,crystallization temperature 55 ℃,solvent flow rate 0. 9 m L / min. Under the optimal conditions,the average recovery rate of the solid dispersion was 88. 22%,IR and DSC analysis showed that oryzanol in the solid dispersion was amorphous form,and hydrogen bond may have been formed between oryzanol and PVP-K30. The experiments of in vitro dissolution showed that the dissoluion rate of oryzanol / PVP-K30 solid dispersions was significantly increased. CONCLUSION Supercritical CO2anti-solvent technology is feasible to prepare oryzanol / PVP-K30 solid dispersions.

关 键 词：超临界CO2抗溶剂法 谷维素 固体分散体 溶出度 

分 类 号：R943[医药卫生—药剂学]