丙基硫氧嘧啶固体脂质纳米粒的制备与质量评价  

Preparation and Quality Evaluation of Propylthiouracil Solid Lipid Nanoparticles

作　　者：徐雄波[1] 崔叶妹 宋红娟[2] 卜振军 张青松[1] 唐靖[1] 马宁[1] 

机构地区：[1]长沙医学院药学院,长沙410219 [2]徐州市妇幼保健院,江苏徐州221003 [3]湖南九典制药有限公司,长沙410331

出　　处：《中国药房》2016年第7期946-949,共4页China Pharmacy

基　　金：湖南省医药卫生科研计划课题项目(No.B2014-069)

摘　　要：目的:优化丙基硫氧嘧啶(PTU)固体脂质纳米粒(PTU-SLN)的处方和制备工艺,并对PTU-SLN质量进行评价。方法:采用乳化超声分散法制备PTU-SLN,以粒径和包封率为评价指标,以脂质材料、大豆磷脂、泊洛沙姆188用量以及超声时间为考察因素,通过正交试验对处方及工艺进行优化;同时以粒径、Zeta电位、包封率、稳定性及体外累积释放度为指标评价其质量。结果:最优制备处方和工艺为脂质材料0.6 g、大豆磷脂1.0 g、泊洛沙姆188 0.8 g、超声时间10 min。所制得的PTU-SLN外观形态圆整,粒径分布均匀,平均粒径为93.5 nm,平均Zeta电位为-30.8 m V,平均包封率为74.9%;4℃条件下放置15 d粒径和外观无明显变化;体外4 h累积释放度达56.1%,24 h累积释放度达98.4%。结论:成功制得PTU-SLN,且处方工艺合理,可达到使药物缓慢释放的效果。OBJECTIVE： To optimize the formulation and preparation technology of Propylthiouracil （PTU） solid lipid nanoparticles （PTU-SLN）and to evaluate the quality of PLN-SLN. METHODS： PTU-SLN was prepared by emulsion ultrasound dispersing method. The formulation of PTU-SLN was optimized by orthogonal design with the entrapment efficacy and particle size as index, using the amount of lipid material, soybean lecithin and poloxamer 188 and ultrasonic time as factors. The quality of prepared nanoparticles was evaluated with particle size, Zeta potential, entrapment efficiency, stability and in vitro drug release rate as index. RESULTS： The optimal formulation and technology was as follows as lipid material 0.6 g, soybean lecithin 1.0 g, poloxamer 188 0.8 g, ultrasonic time 10 min. The obtained PTU-SLN was round and smooth in appearance and distributed evenly in particle size with average particle size of 93.5 nm, Zeta potential of - 30.8 mV and average entrapment efficiency of 74.9%. Prepared nanoparticles had no significant change after placing for 15 d at 4℃. Accumulative release rate of PTU-SLN was 56.1% at 4 hour in vitro and reached 98.4% at 24 hour. CONCLUSIONS： PTU-SLN is prepared successfully and reasonable in technology, and can reach sustained-release effects.

关 键 词：丙基硫氧嘧啶 固体脂质纳米粒 包封率 体外释放 正交试验 

分 类 号：R943[医药卫生—药剂学]