广藿香油胃漂浮缓释微粒处方优化及制剂评价  

Formulation optimization and Preparation evaluation for Gastro-floating sustained release particles of Pachouli oil

作　　者：刘晨[1] 吴亚楠 李博莉 王文苹[2,3] LIU Chen;WU Ya-nan;LI Bo-li;WANG Wen-ping(General Hospital of Ningxia Medical University,Yinchuang,Ningxia 750004,China;Ningxia Medical University,Yinchuan Ningxia 750004,China;College of Chinese Materia Medica,Yunnan University of Chinese Medicine,Kunming 650500,China)

机构地区：[1]宁夏医科大学总医院,宁夏银川750004 [2]宁夏医科大学,宁夏银川750004 [3]云南中医药大学中药学院,云南昆明650500

出　　处：《时珍国医国药》2024年第3期620-624,共5页Lishizhen Medicine and Materia Medica Research

基　　金：国家自然科学基金(81760713,81960719);云南省中青年学术和技术带头人后备人才项目(202205AC160038);全国中药特色技术传承人培训项目(国中医药人教函[2023]96号)。

摘　　要：目的优化广藿香油胃漂浮缓释微粒(Gastro-floating sustained release particles of patchouli oil,PO-GFSRP)的缓释材料处方,并初步评价制剂质量。方法采用挤出-滚圆法制备了胃漂浮缓释微粒。以PO体外累积释放率为考察指标,对主要缓释材料种类、含量及不同缓释材料间比例进行单因素考察,结合星点设计-效应面法优化缓释材料处方,考察缓释材料乙基纤维素(EC)和羧丙甲基纤维素(HPMC)总量及其质量比对PO累积释放率的影响;通过PO-GFSRP物理性质、体外8 h漂浮率、体外释放度以及加速稳定性实验进行制剂质量的初步评价。结果优化的缓释材料处方为EC 22.5%、HPMC 27.5%;PO-GFSRP的收率72.70%、休止角37.63°、松密度0.60 g/mL、脆碎度0.84%、体外8 h漂浮率87.67%;12 h PO累积释放率达到96%以上;在温度25℃、相对湿度60%条件下6个月药物损失量在10%以内。结论基于EC/HPMC缓释材料的PO-GFSRP具有良好的缓释效果,PO累积释放率及微粒漂浮性能良好。Objective To optimize the formulation for gastro-floating sustained release particles of Pachouli oil(PO-GFSRP),and to primarily evaluate their quality.Methods The PO-GFSRP were fabricated by the extrusion-spheronization method.The type,ratio and total amount of sustained-release polymers in formulation were screened by single factor experiments using in vitro drug release as the index.Furthermore,the central composite design-response surface methodology was adopted to optimize the ratio and total amount of ethyl celulose(EC)and hydroxypropyl methyl cellulose(HPMC)according to their influences on accumulative drug release.The obtained microparticles were evaluated on their physiochemical properties,in vitro floating rate at 8h and drug release,accelerate stabilitys.Results The optimized formulation contained 22.5%EC and 27.5%HPMC as sustained-release materials.The yield,repose angle,bulk density,friability and floating rate of particles were 72.70%,37.63°,0.60 g·mL~(-1),0.84%and 87.67%respectively.The particles released over 96%PO after 12 hours,and drug loss was within 10%after storage for 6 months at 25℃and 60%relative humidity.Conclusion PO-GFSRP showed a preferable sustained-release pattern with acceptable release and floating rates.

关 键 词：广藿香油 胃漂浮微粒 处方优化 制剂评价 

分 类 号：R283[医药卫生—中药学]