基于“溶质相转移”技术的黄芩提取物鼻用亚微乳制备工艺研究  

Nasal submicron emulsion of Scutellariae Radix extract preparation technology research based on phase transfer of solute technology

作　　者：史亚军[1] 施俊辉[2] 陈世彬[2] 杨明[3] 

机构地区：[1]陕西中医药大学药学院,陕西咸阳712046 [2]成都中医药大学药学院,四川成都611137 [3]江西中医药大学现代中药制剂教育部重点实验室,江西南昌330004

出　　处：《中国中药杂志》2015年第14期2825-2831,共7页China Journal of Chinese Materia Medica

基　　金：国家"重大新药创制"科技重大专项(2009ZX09103-353);陕西省教育厅科研专项(11JK0680)

摘　　要：该研究基于鼻腔给药制剂高载药量的要求,采用独特的溶质相转移技术,将黄芩提取物磷脂复合物制备与亚微乳成型工艺集成,制备得到了高载药量的亚微乳。在药物溶散方法研究中,对传统的搅拌法、研磨法、匀浆法和创新的溶质相转移技术进行了考察,以药物分散的均匀性和载药量作为评价指标,确定了溶质相转移技术作为药物的溶散方法,该技术使亚微乳的黄芩提取物载药量达到了1.33%(磷脂复合物为4%),较传统亚微乳载药量显著提高;对溶质相转移的方法和相转移时机进行了研究,确定在黄芩提取物磷脂复合物的无水乙醇液总体积回收至剩余30%时加入油相,继续回收无水乙醇而实现溶质相转移,溶质相转移效果理想;药物溶散至油相后,采用单因素实验法,确定了初乳的制备工艺;以初乳和亚微乳的粒径、PDI以及稳定性参数为评价指标,采用正交设计对处方组成和高压均质参数进行了优化,最终形成了稳定可行的制备工艺。Based on the demand of nasal drug delivery high drug loadings, using the unique phase transfer of solute, integrating the phospholipid complex preparation and submicron emulsion molding process of Scutellariae Radix extract, the study obtained the preparation of the high drug loadings submicron emulsion of Scutellariae Radix extract. In the study of drug solution dispersion method, the uniformity of drug dispersed as the evaluation index, the traditional mixing method, grinding, homogenate and solute phase transfer technology were investigated, and the solute phase transfer technology was adopted in the last. With the adoption of new technology, the drug loading capacity reached 1.33% （phospholipid complex was 4% ）. The drug loading capacity was improved significantly. The transfer of solute method and timing were studied as follows ,join the oil phase when the volume of phospholipid complex anhydrous ethanol solution remaining 30%, the solute phase transfer was completed with the continued recycling of anhydrous ethanol. After drug dissolved away to oil phase, the preparation technology of colostrum was determined with the evaluation index of emulsion droplet form. The particle size of submicron emulsion, PDI and stability parameters were used as evaluation index, orthogonal methodology were adopted to optimize the submicren emulsion ingredient and main influential factors of high pressure homogenization technology. The optimized preparation technology of Scutellariae Radix extract nasal submicron emulsion is practical and stable.

关 键 词：溶质相转移 鼻用制剂 黄芩提取物 亚微乳 

分 类 号：R283.6[医药卫生—中药学]