摘要
目的制备五味金色缓释片,比较自制五味金色缓释片与市售缓释丸剂比格犬体内药动学。方法采用单因素方法筛选处方,制备五味金色缓释片。单剂量口服、双周期交叉实验,以市售缓释丸剂为参比制剂,采用液相色谱-串联质谱(LC-MS/MS)法同时测定两种成分血药浓度,采用DAS2.0版药动学智能分析软件拟合药动学参数。结果所制备的五味金色缓释片重复性良好,性能稳定。以芍药苷为内标,测定血浆中鞣花酸、去氢木香内酯浓度,在1.006~301.8 ng·mL^-1范围内呈线性关系,平均回收率均>85.81%,日内与日间精密度RSD均<9.74%。五味金色缓释片去氢木香内酯和鞣花酸在血浆中tmax显著高于缓释丸剂,Cmax、血药浓度-时间曲线下面积(AUC)、MRT差异无统计学意义。五味金色缓释片剂与缓释丸剂去氢木香内酯和鞣花酸吸收相同,达峰时间更长,有效成分释放缓慢,毒性延缓。结论 LC-MS/MS法可用于五味金色缓释片药动学研究,自制五味金色缓释片具有缓释效果。
Objective To prepare Wuwei Jinse sustained release tablets and to study the pharmacokinetics of Wuwei Jinse sustained release tablets and commercial pills. Methods Preparation of Wuwei Jinse sustained release tablets by single factor method.Single-dose oral,double cycle cross test,using commercially available pills as a reference preparation,simultaneous determination of plasma concentrations of both components by LC-MS/MS method,and pharmacokinetic parameters were fitted with das 2.0. Results The preparation of Wuwei Jinse sustained release tablets showed good reproducibility and stable performance.The concentration of ellagic acid and dehydrocostus lactone in plasma was measured with paeoniflorin as the internal standard.The linear relationship was observed in the range of 1.006-301.8 ng·mL^-1.The average recovery rate was greater than 85.81%.The intra-day and inter-day precision were determined. RSD are all less than 9.74%.The tmax of Wuwei Jinse sustained-release Tablets dehydrocostus lactone and ellagic acid in plasma was significantly higher than that of the sustained-release pellets,and there was no significant difference in Cmax,AUC,and MRT.Wuwei Jinse sustained release tablets and sustained release pills are the same as dehydroabiolide and ellagic acid,longer peak time,slow release of active ingredients,and delay of toxicity. Conclusion The method can be used to study the pharmacokinetics of Wuwei Jinse sustained release tablets.The self-made sustained-release tablets have sustained-release effect.
作者
朱烨
张洁
关志宇
林春莲
颜洁
刘婧
黄潇
ZHU Ye;ZHANG Jie;GUAN Zhiyu;LIN Chunlian;YAN Jie;LIU Jing;HUANG Xiao(School of Pharmacy,Jiangxi University of Traditional Chinese Medicine,Nanchang 330000,China)
出处
《医药导报》
CAS
北大核心
2020年第3期292-297,共6页
Herald of Medicine
基金
江西省教育厅科技计划项目(GJJ170718)
中药学一流学科科研项目(JXSYLXK-ZHYAO049)。
关键词
五味金色缓释片
处方筛选
药动学
体内
Wuwei Jinse sustained release tablets
Prescription screening
Pharmacokinetics,in vivo
