白杨素固体脂质纳米粒的制备及其药动学行为  

Preparation of chrysin solid lipid nanoparticles and their pharmacokinetic behaviors

作　　者：杨金枝 孙文霞[2] 王姣姣[2] 崔锋[2] 郝海军[2] 

机构地区：[1]郑州澍青医学高等专科学校,河南郑州450064 [2]中国医药工业研究总院上海医药工业研究院,上海201203

出　　处：《中成药》2018年第1期76-80,共5页Chinese Traditional Patent Medicine

摘　　要：目的制备白杨素固体脂质纳米粒,并评价其药动学行为。方法乳化超声-低温固化法制备纳米粒,测定其粒径、Zeta电位、体外释放度。12只SD大鼠随机分为2组,分别灌胃给予原料药、纳米粒混悬液。HPLC法测定血浆中白杨素含有量,绘制血药浓度-时间曲线,计算药动学参数。结果所得纳米粒平均粒径为(207.15±30.59)nm,PDI为0.224±0.067,Zeta电位为(-34.8±5.9)m V,36 h内累积释放度达84.36%。其Cmax、AUC0~t分别为(9.04±1.52)μg/m L、(33.67±3.47)μg·h/m L,明显高于原料药(P<0.01)。结论固体脂质纳米粒可促进白杨素的口服吸收和生物利用度,并具有显著缓释特征。AIM To prepare chrysin solid lipid nanoparticles and to evaluate their pharmacokinetic behaviors METHODS The particle size, Zeta potential and in vitro release rate of nanoparticles prepared by emulsification ultrasonication-low temperature solidification method were determined. Twelve SD rats were randomly divided into two groups and were intragastrically given suspensions of crude drug and nanoparticles, respectively. HPLC was used for the content determination of chrysin in plasma, after which blood drug concentration-time curves were drawn, and pharmacokinetic parameters were calculated. RESULTS The obtained nanoparticles demonstrated the particle size of （207. 15 ±30. 59） nm, PDI of （0. 224±0. 067） and Zeta potential of （ -34. 8 ±5.9） mV, respectively, whose accumulative release rate reached 84. 36% within 36 h. Their Cmax [ （9.04± 1.52） μg/mL] and AUC0-t [ （33.67 ± 3.47） μg·h/mL] were much higher than those of the crude drug （P 〈 0. 01 ）. CONCLUSION Solid lipid nanoparticles can promote the oral absorption and bioavailability of ehrysin, with significant sustained-release characteristics.

关 键 词：白杨素 固体脂质纳米粒 制备 药动学 乳化超声-低温固化 HPLC 

分 类 号：R944[医药卫生—药剂学]