大黄酸磷脂复合物及其固体分散体的制备和体内药动学研究  

Preparation and in vivo pharmacokinetics of rhein phospholipid complex and its solid dispersions

作　　者：曹伶俐 杨宁辉 张智强[3] CAO Ling⁃li;YANG Ning⁃hui;ZHANG Zhi⁃qiang(Zhengzhou Health Vocational College,Zhengzhou 450005,China;Henan Medical College,Xinzheng 451191,China;Tianjin Institute of Phar⁃maceutical Research Pharmaceutical Co.,Ltd.,Tianjin 300301,China)

机构地区：[1]郑州卫生健康职业学院,河南郑州450005 [2]河南医学高等专科学校,河南新郑451191 [3]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12期2833-2837,共5页Chinese Traditional Patent Medicine

基　　金：河南省科技厅重点研发与推广项目(18210231168)

摘　　要：目的制备大黄酸磷脂复合物和磷脂复合物固体分散体,并考察其体内药动学。方法溶剂挥发法制备磷脂复合物及其固体分散体,X射线衍射分析晶型,测定溶出率及累积溶出度。大鼠灌胃给药后,HPLC法测定大黄酸血药浓度,计算主要药动学参数。结果大黄酸在磷脂复合物及其固体分散体中均以无定型状态存在,溶出率和累积溶出度有所增加,在后者中更明显。与原料药比较,磷脂复合物及其固体分散体Cmax、AUC0~t、AUC0~∞显著升高(P<005,P<001),以后者更明显(P<005),两者相对生物利用度分别提高到27143%、46883%。结论磷脂复合物及其固体分散体均可促进大黄酸口服吸收,后者效果更佳。AIM To prepare rhein phospholipid complex and its solid dispersions,and to investigate their in vivo pharmacokinetics.METHODS For the phospholipid complex and its solid dispersions prepared by solvent evaporation method,X ray powder diffraction(XRPD)was used to study crytal form,dissolution rate and accumu lative dissolution rate were determined.Rats were given intragastrical administrtaion,after which HPLC was adopted in the plasma concentration determination of rhein,and main pharmacokinetic parameters were calculated.RESULTS Rhein existed in an amorphous state in the phospholipid complex and its solid dispersions,whose dissolution rate and accumulative dissolution rate were enhanced,especially for those in the latter.Compared with raw medicine,the phospholipid complex and its solid dispersions demonstrated significantly increased C,AUC max 0~t andAUC0~∞(P<005,P<001),especiallyforthelatter(P<005),whoserelativebioavailabilitieswerein creased to 27143%and 46883%,respectively.CONCLUSION Both phospholipid complex and its solid dispersions can promote the oral absorption of rhein,and the latter displays a better effect.

关 键 词：大黄酸 磷脂复合物 固体分散体 制备 体内药动学 溶剂挥发法 HPLC 

分 类 号：R944[医药卫生—药剂学]