阿瑞匹坦静脉注射乳剂的研制  

Preparation of Aprepitant Emulsion for Intravenous Injection

作　　者：周卫[1] 陈飞[1] 陈宁[1] 毛柯[1] 

机构地区：[1]南京工业大学药学院、南京工业大学江苏省药物研究所,江苏南京211816

出　　处：《中国医药工业杂志》2012年第12期1003-1006,共4页Chinese Journal of Pharmaceuticals

摘　　要：通过单因素试验和正交设计优选了阿瑞匹坦静脉注射乳剂的最佳处方,并考察了形态、粒径、电位和稳定性等基本性质。结果表明,乳化剂的种类和用量及油酸的用量对制品稳定性有较大影响。优化得到的阿瑞匹坦乳剂的处方为:阿瑞匹坦0.25%、大豆油15%、蛋黄磷脂E80 2.5%、油酸0.125%。所得制品外观呈乳白色,灭菌前、后的平均粒径、PDI、离心稳定常数(Ke)、ζ电位、pH和1含量(标示量%)分别为(218.71±1.26)和(220.3±0.53)nm、0.203±0.016和0.210±0.009、0.21±0.01和0.34±0.01、(-37.8±0.2)和(-37.6±0.8)mV、7.21±0.23和7.31±0.30、(101.03±0.89)%和(101.12±1.20)%。The formulation of aprepitant emulsion for intravenous injection was optimized by single factor test and orthogonal design. The properties, such as appearance, particle size, ζ potential and stability of the product were investigated. The results showed that the type and amount of emulsifier as well as the amount of oleic acid had the greater effect on stability. The optimal formulation of aprepitant emulsion was as follows： aprepitant was 0.25 %, soybean oil was 15 %, egg yolk lecithin E80 was 2.5 % and oleic acid was 0.125 %. The appearance of the product was ivory. The average particle size, PDI, centrifugal stability constant （Ke）, ζ potential, pH value and drug content of the product before and after sterilization were （218.71±1.26） and （220.3±0.53）nm, 0.203±0.016 and 0.210±0.009, 0.21±0.01 and 0.34±0.01, （-37.8±0.2） and （-37.6±0.8）mV, 7.21±0.23 and 7.31±0.30, （101.03±0.89） % and （101.12±1.20） %, respectively.

关 键 词：阿瑞匹坦 注射用乳剂 制备 离心稳定常数 粒径 电位 

分 类 号：R944.1[医药卫生—药剂学]