摘要
目的 研究水飞蓟素PLGA肠溶纳米粒在大鼠体内的药动学行为。方法 利用高效液相色谱（HPLC）法测定大鼠灌胃市售制剂水飞蓟素片益肝灵片与水飞蓟素PLGA肠溶纳米粒后的血药浓度,并采用3P97药代动力学软件处理数据。结果在25.3~5 051.0ng/mL范围内,水飞蓟宾血药浓度呈线性关系,r=0.999 9,日内、日间精密度RSD均小于8.5%;灌胃给药水飞蓟素PLGA肠溶纳米粒后,药-时曲线符合二室模型,药代动力学参数Cmax为（2 255.84±315.44）ng/mL,t1/2β为（13.85±2.29）h,相对益肝灵片的生物利用度为126%。结论 本方法准确、简单、专属性好,适合大鼠血浆中水飞蓟素PLGA肠溶纳米粒药代动力学学研究。水飞蓟素PLGA肠溶纳米粒提高了口服生物利用度。
Objective To investigate the pharmacokinetics of enteric coated silymarin-PLGA nanopartlcles m rats. lvletnocls Rats were given silymarin tablets and enteric coated silymarin-PLGA nanoparticles by intragastric administration. The HPLC meth- od was established to detect drug concentration in plasma of rats,and the obtained data were processed with 3P97 software. Results In 25.3-5 051.0 ng/mL range, silybin plasma concentration showed a linear relation, r=0. 999 9, the intra and interprecisions （RSD）were all lower than 8.5% The concentration-time curve was fitted to a 2-compartment model,the pharmacokinetie parameters of the enteric coated silymarin-PLGA nanoparticle were as follows： Cmax was （2 255.84 ± 315.44） ng/mL, t1/2β was （ 13.85 ±2.29）h,and the relative bioavailability espeetively was 126% Conclusion The method is＇accurate,simple and reproducible. It is fit to study the pharmacokinetics of the enteric coated silymarin-PLGA nanoparticle in plasma of rats. The enteric coated silymarin-PL- GA nanoparticle could improve the oral bioavailability significantly.
出处
《重庆医学》
CAS
北大核心
2016年第28期3910-3912,3915,共4页
Chongqing medicine
基金
重庆市科技攻关计划基金资助项目(cstc2012gg-yyis10008)
