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作 者:张留超[1] 刘勇华[1] ZHANG Liu-chao;LIU Yong-hua(Huanghe Science&Technology College,Zhengzhou 450005,China)
机构地区:[1]黄河科技学院,河南郑州450005
出 处:《中成药》2021年第7期1685-1690,共6页Chinese Traditional Patent Medicine
基 金:2016年科技攻关项目(162102310234)。
摘 要:目的制备鞣花酸磷脂复合物,并研究其口服生物利用度。方法溶剂挥发法制备磷脂复合物。以磷脂用量、制备温度、制备时间为影响因素,复合率为评价指标,Box⁃Behnken响应面法优化制备工艺。对磷脂复合物进行X射线粉末衍射(XRPD)分析,测定其在水、正辛醇中的溶解度。大鼠随机分为3组,分别灌胃给予原料药、物理混合物、磷脂复合物的0.5%CMC⁃Na混悬液(100 mg/kg),于0.15、0.25、0.75、1、1.5、2、3、4、6、8、12 h采血,HPLC法测定鞣花酸血药浓度,计算主要药动学参数。结果最佳条件为磷脂用量141.6 mg,制备温度46.9℃,制备时间4.7 h,复合率为99.3%。鞣花酸在磷脂复合物中以无定形状态存在,在水、正辛醇中的溶解度分别提高至3.22、7.18倍。与原料药、物理混合物比较,磷脂复合物tmax缩短(P<0.05),C_(max)、AUC_(0~t)、AUC_(0~∞)升高(P<0.01),相对口服生物利用度提高至2.46倍。结论磷脂复合物可改善鞣花酸的口服生物利用度。AIM To prepare ellagic acid phospholipids complex and to study its oral bioavailability.METHODS The phospholipids complex was prepared by solvent evaporation method.With phospholipids consumption,preparation temperature and preparation time as influencing factors,recombination rate as an evaluation index,the preparation process was optimized by Box⁃Behnken response surface method.X⁃ray powder diffraction(XRPD)was applied to analyzing the phospholipids complex,whose solubilities in water and n⁃octanol were determined.Rats were randomly assigned into three groups and given intragastric administration of 0.5%CMC⁃Na suspensions(100 mg/kg)of raw medicine,physical mixture and phospholipids complex,respectively,after which blood collection was made at 0.15,0.25,0.75,1,1.5,2,3,4,6,8,12 h,HPLC was adopted in the plasma concentration determination of ellagic acid,and main pharmacokinetic parameters were calculated.RESULTS The optimal conditions were determined to be 141.6 mg for phospholipids consumption,46.9℃for preparation temperature,and 4.7 h for preparation time,the recombination rate was 99.3%.Ellagic acid existed in an amorphous state in the phospholipids complex,whose solubilities in water and n⁃octanol were enhanced to 3.22 times and 7.18 times,respectively.Compared with the raw medicine and physical mixture,the phospholipids complex demonstrated shortened tmax(P<0.05)and increased C_(max),AUC_(0-t) and AUC_(0-∞) (P<0.01),and the relative oral bioavailability was enhanced to 2.46 times.CONCLUSION Phospholipids complex can improve the oral bioavailability of ellagic acid.
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