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.docVIP

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 　　[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。 　　[关键词]溶质相转移; 鼻用制剂; 黄芩提取物; 亚微乳 　　Nasal submicron emulsion of Scutellariae Radix extract preparation technology 　　research based on phase transfer of solute technology 　　SHI Ya-jun1*， SHI Jun-hui2， CHEN Shi-bin2 ， YANG Ming3 　　（1. College of Pharmacy， Shaanxi University of Traditional Chinese Medicine， Xianyang 712046， China; 　　2.College of Pharmacy， Chengdu University of Traditional Chinese Medicine， Chengdu 611137， China; 　　3. Key Laboratory of Modern Preparation of Traditional Chinese Medicine， Ministry of Education， Jiangxi University of Traditional 　　Chinese Medicine， Nanchang 330004， China） 　　[Abstract]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 sol