大黄酸固体分散体在大鼠体内药动学研究  

Study on Pharmacokinetics of Rhein Solid Dispersion in Rats

作　　者：李琳玉[1] 王昆[1] 潘菲[1] 赵鸣飞[1] 侯凌宇 韩刚[1] 

机构地区：[1]河北联合大学公共卫生学院,河北唐山063000

出　　处：《中药新药与临床药理》2015年第2期214-216,共3页Traditional Chinese Drug Research and Clinical Pharmacology

摘　　要：目的研究大黄酸固体分散体在大鼠体内的药动学过程。方法以聚乙烯吡咯烷酮(K30)为载体制备大黄酸固体分散体。大鼠分别灌胃给予大黄酸及大黄酸固体分散体,2组均按大黄酸50mg·kg-1的剂量给药。高效液相色谱法测定大黄酸在大鼠体内血药浓度变化。血药浓度数据采用3P97药动学软件进行处理,确定药动学参数。结果大鼠给予大黄酸及大黄酸固体分散体后,大黄酸药-时过程均符合二房室模型,大黄酸组的药-时曲线下面积(AUC)、最大血药浓度(Cmax)、达峰时间(Tmax)分别为(1.16±0.17)μg·h-1·mL-1、(1.78±0.33)μg·mL-1和(0.14±0.02)h,大黄酸固体分散体组的AUC、Cmax、Tmax分别为(4.77±0.89)μg·h·mL-1、(7.24±1.18)μg·mL-1和(0.10±0.02)h。大黄酸组与大黄酸固体分散体组的AUC、Cmax比较差异均有统计学意义(P<0.05)。结论大黄酸固体分散体能提高大黄酸在大鼠体内的吸收。Objective To study the pharmacokinetics of rhein solid dispersion in rats after oral administration of rhein and rhein solid dispersion.Methods Rhein solid dispersion was prepared with polyvinyl pyrrolidone（K30）.The rats were administrated intragastrically rhein and rhein solid dispersion respectively,in the same rhein dosage of 50mg/kg.The plasma concentration of rhein was determined by high performance liquid chromatography（HPLC）.The software of 3P97 was used to process the pharmacokinetic parameters.Results The concentration-time profiles of rhein and its solid dispersions were shown to fit two-compartment model.Their AUC,Cmax,and Tmaxfor rhein group were（1.16 ±0.17） μg·h·m L^-1,（1.78 ±0.33） μ g·m L^-1 and（0.14 ±0.02） h,while for rhein solid dispersions group were（4.77 ±0.89） μ g·h·m L-1,（7.24 ±1.18） μ g·m L^-1,and（0.10 ±0.02） h respectively.Statistical results showed that the differences of AUC and Cmaxwere significant（P〈0.05）.Conclusion With polyvinyl pyrrolidone as the carrier,the preparation of the solid dispersion of rhein has higher rhein absorption rate in rats.

关 键 词：大黄酸 固体分散体 聚乙烯咯烷吡酮 药物动力学 高效液相色谱法 

分 类 号：R285.5[医药卫生—中药学]