摘要
本文研究了南五味子总木脂素肠溶(SLE)纳米粒的制备工艺,并进行大鼠体内药代动力学评价。采用改良乳化溶剂扩散法制备南五味子总木脂素肠溶纳米粒,并考察载药纳米粒的形态及粒径分布。以五味子甲素(QS)和五味子酯甲(SA)为指标成分,用HPLC法测定药物的包封率和经大鼠灌胃给药的血药浓度,用3p97程序计算药代动力学参数。制得的纳米粒在透射电镜下均成圆球形,平均粒径为(36.7±4.4)nm、多分散度指数为0.231±0.031,QS和SA包封率分别为(97.5±0.7)%和(91.3±0.8)%。大鼠血药浓度曲线经3p97程序拟合,确定QS和SA在大鼠体内的药代动力学过程为一室模型。其中QS的AUC为75.65μg·mL-1·h,SA的AUC为109.32μg·mL-1·h,分别是对照组的2.3倍和5.8倍。改良乳化溶剂扩散法制备SLE纳米粒工艺可行,且包封率高,大鼠体内药代动力学结果表明SLE纳米粒能提高药物生物利用度。
To study the preparation method of Schisandra total lignanoids enteric （SLE） nanoparticles and evaluate its pharmacokinetics in rats, SLE nanoparticles were prepared by modified emulsion solvent diffusion method. The properties of SLE nanoparticles were evaluated of morphology, mean diameter and entrapment efficiency. An HPLC method was employed to determine the concentration of deoxyschisandrin （QS） and schisantherrin A （SA） in plasma, which were used as an index of Schisandra total lignanoids, and the bioavailability of the nanoparticles was compared with the reference group by oral administration using SD rats. The nanoparticles observed by transmission electronmicroscopy were round, and the mean particle sizes of SLE were （36.7±4.4） nm. Entrapment efficiency of QS and SA were （97.5±0.7） % and （91.3±0.8） %, respectively. Its pharmacokinetic process calculated with 3p97 software was fitted to a one-compartment model. The pharmacokinetic parameters showed sustained-release property. Compared with reference formulation, the AUCs of SLE nanoparticles were 2.3 and 5.8 times separately. These results suggested that the incorporation into Eudragit S 100 of Schisandra total lignanoids can improve the bioavailability.
出处
《药学学报》
CAS
CSCD
北大核心
2009年第9期1046-1050,共5页
Acta Pharmaceutica Sinica
基金
北京市自然科学基金资助项目(7072076)
关键词
肠溶纳米粒
药代动力学
南五味子总木脂素
enteric nanoparticle
pharmacokinetics
Schisandra total lignanoids
