辛伐他汀固体脂质纳米粒的制备及在大鼠体内的药动学研究  

Preparation and Pharmacokinetics in Rats of Simvastatin Solid Lipid Nanoparticles

作　　者：刘艳明[1] 王雪芳[2] 王东[3] 

机构地区：[1]解放军251医院心内科,河北张家口075000 [2]河北北方学院医学院生理教研室 [3]天津中医药大学药学院

出　　处：《中国药师》2016年第1期50-53,共4页China Pharmacist

摘　　要：目的:制备辛伐他汀固体脂质纳米粒,并研究其经灌胃给药后在大鼠体内的药动学特征。方法:采用热熔乳化超声-低温固化法制备辛伐他汀固体脂质纳米粒,考察辛伐他汀固体脂质纳米粒的粒径分布、Zeta电位、包封率、微观形态及体外药物释放特性。研究辛伐他汀固体脂质纳米粒经灌胃给药后在大鼠体内的药动学特征。结果:辛伐他汀固体脂质纳米粒平均粒径为(242.5±62.1)nm,多聚分散系数为0.225±0.031,Zeta电位为(-32.1±4.2)m V,包封率为(95.7±2.6)%,在24 h内平稳缓慢释药。辛伐他汀固体脂质纳米粒在大鼠体内的C_(max)和AUC_(0-t)分别为辛伐他汀混悬液的2.89倍和1.83倍。结论:辛伐他汀固体脂质纳米粒在大鼠体内能快速吸收,显著提高了药物在大鼠体内的生物利用度。Objective： To prepare simvastatin solid lipid nanoparticles and evaluate its characteristics of pharmacokinetics in rats after oral administration. Methods： Simvastatin solid lipid nanopartieles were prepared by a inch-emulsion uhrasonieation and low temperature-solidification method. The physicochemical properties of simvastatin solid lipid nanoparticles were studied, such as particle diameter, zeta potential, particle shape, encapsulation efficiency and in vitro release. The characteristics of pharmacokinetics in rats after oral administration of simvastatin solid lipid nanoparticals were studied. Results： For simvastatin solid lipid nanoparticles, the particle size was （242.5 ± 62.1 ） nm with the polydispersity index of （0. 225 ±0.031 ）, zeta potential was （ - 32.1 ± 4.2） mV, and the encapsulation efficiency was （95.7± 2.6） %. The in vitro release was proved that the drug release from the formula was steady during 24 h. Cmax and AUC0-t of simvastatin solid lipid nanoparticles respectively was 2.89 and 1.83 times higher than that of simvastatin sus- pension. Conclusion ： Simvastatin solid lipid nanopartieles can promote the absorption of simvastatin and increase bioavailability in rats remarkably.

关 键 词：辛伐他汀固体脂质纳米粒 热熔乳化超声-低温固化法 药动学 生物利用度 

分 类 号：R944.9[医药卫生—药剂学] R969.1[医药卫生—药学]