2种斯皮诺素固体分散体的制备及其体内药动学行为  

Preparation and in vivo pharmacokinetic behavior evaluation for two spinosin solid dispersions

作　　者：张铁山[1] 尚曙玉[1] 王聪颖[1] 张智强[2] ZHANG Tie-shan;SHANG Shu-yu;WANG Cong-ying;ZHANG Zhi-qiang(Huanghe Science & Technology College,Zhengzhou 450005,China;Tianjin Institute of Pharmaceutical Research Pharmaceutical Co.,Ltd., Tianjin 300301,China)

机构地区：[1]黄河科技学院,河南郑州450005 [2]天津药物研究院药业有限责任公司,天津300301

出　　处：《中成药》2019年第9期2025-2029,共5页Chinese Traditional Patent Medicine

基　　金：河南省重大科技专项(162102310003)

摘　　要：目的制备斯皮诺素固体分散体、磷脂复合物固体分散体,并考察其体内药动学行为。方法溶剂挥发法制备2种固体分散体后,X射线粉末衍射(XRPD)分析存在状态,测定溶解度和体外溶出速率。大鼠灌胃给药后,HPLC法测定斯皮诺素血药浓度,计算主要药动学参数。结果斯皮诺素在2种固体分散体中以无定型状态存在,溶解度、体外溶出速率明显提高。与原料药比较,固体分散体、磷脂复合物固体分散体相对生物利用度分别增加到219.61%、265.39%。结论固体分散体、磷脂复合物固体分散体均可促进斯皮诺素口服吸收,以后者更明显。AIM To prepare spinosin solid dispersions and phospholipid complex solid dispersions, and to investigate their in vivo pharmacokinetic behaviors.METHODS For the two solid dispersions prepared by solvent evaporation method, the existential state was analyzed by X-ray power diffraction(XRPD), along with the determination of solubility and in vitro dissolution rate. Rats were given intragastric administration, then HPLC was adopted in the plasma concentration determination of spinosin, and the main pharmacokinetic parameters were calculated.RESULTS In the two solid dispersions, spinosin existed in an amorphous state with obviously elevated solubility and in vitro dissolution rate. The solid dispersions and phospholipid complex solid dispersions were increased to 219.61% and 265.39% as compared with that of raw medicine, respectively.CONCLUSION Both solid dispersions and phospholipid complex solid dispersions can promote the oral absorption of spinosin, especially for the latter.

关 键 词：斯皮诺素 固体分散体 磷脂复合物 制备 体内药动学行为 溶剂挥发法 XRPD HPLC 

分 类 号：R944[医药卫生—药剂学]