醋酸地塞米松脂质纳米粒的优化处方及制备工艺  

The preparation of dexamethasone acetate lipid nanoparticles

作　　者：王敏婷[1] 简炎林[2] 金韵[1] 张志荣[1] 黄园[1] 

机构地区：[1]四川大学华西药学院,四川成都610041 [2]深圳市第二人民医院,广东深圳518031

出　　处：《中国医院药学杂志》2008年第15期1258-1262,共5页Chinese Journal of Hospital Pharmacy

基　　金：深圳市科技计划项目(编号:200602154)

摘　　要：目的:制备一种具有较高载药量,避免药物突释,达到缓释的新型醋酸地塞米松脂质纳米粒。方法:利用薄膜-超声法,使用卵磷脂和大豆油作为载体材料,制备醋酸地塞米松脂质纳米粒。以纳米粒的粒径、Zeta电位、载药量和包封率作为考察指标,对有机溶剂的种类、投药量、载体材料投料比、表面活性剂种类、表面活性剂用量和超声时间进行筛选,并进行体外释放研究。结果:最终确定最优处方及制备工艺为醋酸地塞米松15mg,大豆油100mg,卵磷脂100mg,二氯甲烷20mL,4%的聚山梨酯80和4%的泊洛沙姆188各10mL,超声时间5min。结论:该处方制备的纳米粒不仅可提高醋酸地塞米松的载药量和包封率,且可避免药物的突释现象,为其纳米新剂型的制备提供了新方法。OBJECTIVE To prepare the novel dexamethasone actate lipid nanoparticles with high drug loading ability and avoiding burst release as well as having a in vitro slow release profiles. METHODS The freeze-dried preparation of dexamethasone acetate （DXM） lipid nanoparticles were prepared by film-ultrasonic wave dissolving techniques using natural Lecithin and Soybean oil as carrier materials. During the single-factor screening, the influences of the organic solvents types,the initial mass of DXM,the proportion of the carrier materials, the surfactant types, the surfactant concentrations and the probe sonicate time on the properties of nanoparticles such as the size,Zeta potential,drug loading （DL） and entrapment efficiency （EE） were investigated, and then in vitro release experiments were performed. RESULTS The optimum formula and preparation method of NP were.-DXM 15 mg,soybean oil 100 mg, lecithin 100 mg,dichlormethane 20 mL, Polysorbate 80 （4%） 10 mL, Poloxamer 188 （4%） 10 mL with sonicate time of 5 min. CONCLUSION According to the optimum formula,the size of the obtained NP was 151 nm,Zeta potential was - 33. 7 mV while EE and DL was （97. 11 ± 1.42）% and （4. 41 ± 0. 05）%, and the cumulative amount of DXM was 65% in in vitro release within 288 h.

关 键 词：醋酸地塞米松 脂质纳米粒 体外释放 

分 类 号：R944[医药卫生—药剂学]