蓓萨罗丁固体分散体制备及药物代谢动力学检测  

Preparation of Pessaroddin Solid Dispersion System and Drug Metabolism Dynamics Detection

作　　者：曲方圆 QU Fang-yuan(Yuncheng Nursing Vocational College,Yuncheng 044000,China)

机构地区：[1]运城护理职业学院,山西运城044000

出　　处：《化工管理》2021年第35期77-78,共2页Chemical Engineering Management

摘　　要：为观察蓓萨罗丁固体分散体制备并评估蓓萨罗丁固体分散体药物代谢动力学特征。经LC-MS方法检测,观察SD大鼠体内药物代谢动力学,并进一步观察SD大鼠体内该分散体组织分布特征。蓓萨罗丁固体分散体血浆AUC浓度显著提升,从7035.15μg·L^(-1)·h增长至10157.12μg·L^(-1)·h,给药峰值时间得到显著缩短,从7.32 h缩短为0.9 h,Cmax呈现增加趋势,具体增长幅度为626.35~3012.89μg·L^(-1),MRT呈现下降趋势,下降幅度为11.32~6.31 h。蓓萨罗丁固体分散体使原药药物代谢动力学特征得到一定的改变,无论是生物利用度,还是组织含量均得到显著提升,能够为后续蓓萨罗丁晶型药物临床研究积累数据,并为验证蓓萨罗丁药物的质量和效用提供依据。To observe the preparation and evaluate the drug metabolism dynamics of Pessosoddin solid dispersion system.The pharmacometabolic kinetics of SD rats were observed and the tissue distribution characteristics of this dispersion in SD rats.Results:The plasma AUC concentration of Besarodin solid dispersion increased signif icantly,from the peak time of 7035.15 to 10157.12μg L^(-1) h,from 7.32 h to 0.9h,Cmax,and from 626.35~3012.89μg L^(-1),MRT with a decreasing trend of 11.32~6.31 h.Pessaroddin solid dispersion changes the kinetic characteristics of primary drug metabolism,signif icantly improving both bioavailability and tissue content,which can accumulate data for the subsequent clinical research of Pessaroddin crystal drugs to provide a basis for verifying the quality and eff icacy of pessaroddin.

关 键 词：蓓萨罗丁 固体分散体 药物代谢动力学检测 LC-MS 

分 类 号：R969.1[医药卫生—药理学] R943[医药卫生—药学]