二氢杨梅素固体分散体的制备及其体内药动学研究  

Preparation and in vivo pharmacokinetics of dihydromyricetin solid dispersions

作　　者：范炎峰[1] 荆玲[1] 范金点 邹梦梦 刘宽浩[1] FAN Yan-feng;JING Ling;FAN Jin-dian;ZOU Meng-meng;LIU Kuan-hao(Huanghe Science and Technology College,Zhengzhou 450063,China;Guangdong Pharmaceutical University,Guangzhou 510006,China;The Sixth People’s Hospital of Zhengzhou,Zhengzhou 450015,China)

机构地区：[1]黄河科技学院,河南郑州450063 [2]广东药科大学,广东广州510006 [3]郑州市第六人民医院,河南郑州450015

出　　处：《中成药》2020年第3期553-558,共6页Chinese Traditional Patent Medicine

基　　金：河南省2017年科技发展计划(172102310420)。

摘　　要：目的制备二氢杨梅素固体分散体,并研究其体内药动学。方法以PVP K30为载体,溶剂挥发法制备固体分散体,考察其溶解度和体外溶出。18只大鼠随机分为3组,分别灌胃给予原料药、物理混合物、固体分散体0.5%CMC-Na混悬液(150 mg/kg),于0.167、0.25、0.5、0.75、1、2、4、6、8、12 h取血,HPLC法测定血药浓度,计算主要药动学参数。结果二氢杨梅素制成固体分散体后以无定型状态存在,其表观溶解度提高了9.8倍,累积溶出度增加。与原料药、物理混合物比较,固体分散体tmax缩短(P<0.05),Cmax、AUC0~t、AUC0~∞升高(P<0.05,P<0.01),生物利用度提高了2.66倍。结论固体分散体技术可明显促进二氢杨梅素体内吸收,提高其生物利用度。AIM To prepare dihydromyricetin solid dispersions and to study their in vivo pharmacokinetics.METHODS Solvent evaporation method was adopted in the preparation of solid dispersions with PVP K30 as a carrier, after which the solubility and in vitro dissolution were investigated. Eighteen rats were randomly assigned into three groups and given intragastric administration of raw medicine, physical mixture and 0.5% CMC-Na suspensions of solid dispersions(150 mg/kg), respectively, blood collection was made at 0.167, 0.25, 0.5, 0.75, 1, 2, 4, 6, 8, 12 h, HPLC was applied to determining plasma concentration, and main pharmacokinetic parameters were calculated.RESULTS Dihydromyricetin existed in an amorphous state after being prepared into solid dispersions, whose apparent solubility was enhanced by 9.8 times with increased accumulative dissolution rate. Compared with raw medicine and physical mixture, the solid dispersions demonstrated shortened tmax(P<0.05) and elevated Cmax, AUC0-t, AUC0-∞(P<0.05, P<0.01), and the bioavailability was enhanced by 2.66 times.CONCLUSION Solid dispersion technology can obviously promote the in vivo absorption of dihydromyricetin and enhance its bioavailability.

关 键 词：二氢杨梅素 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]