龙血竭提取物有效成分剑叶龙血素A小鼠药动学研究

Pharmacokinetic study on Effective Ingredient Cochinchinenin A from Dragon' s Blood Extract in Mice

目的:选取中药广西龙血竭提取物(EDB)中有效成分之一的剑叶龙血素A(2,6-二甲氧基-4’-羟基二氢查耳酮)作为考察对象,研究其药动学规律,对龙血竭临床用药具有一定的指导意义。方法:建立实验小鼠血浆中剑叶龙血素A含量的高效液相色谱测定方法,测定给药后不同时间点血浆中剑叶龙血素A的浓度。通过药动学软件3P87进行数据处理,得出剑叶龙血素A的相关药动学参数。结果:剑叶龙血素A血药浓度高效液相色谱测定方法的线性范围为50-500ng/ml,高中低三种浓度回收率分别是114.80±2.86、103.60±4.38、101.80±2.12,最小检测浓度为10ng/ml,日内差为1.28%、日间差为2.26%、精密度(RSD)小于3%;剑叶龙血素A的药动学参数是:T(peak)为77.73min、C(max)为224.99ng/ml、T1/2Ke为72.91min、T1/2Ka为40.94min、V/F(C)为1.019(mg/kg)/(ng/ml)、AUC为49553.47(ng/ml)*min。结论:建立了小鼠血浆中剑叶龙血素A高效液相色谱测定方法;EDB口服后剑叶龙血素A药动学为一室模型,有较大的吸收利用率,其消除半衰期为吸收半衰期的1.78倍,是吸收比消除快的药物。

Object：To select an effective ingredient cochinchinenin A from EDB（Extract of Dragon＇s Blood） as pharmacokinetic study＇s object.Through the experiment,the pharmacokinetic law of Dragon＇s blood was initially understood.Method：The HPLC determination of Cochinchinenin A in mice blood plasma was first established.Then the concentration of Cochinchinenin A in plasma was determined at different time points after administration.Compartmental pharmacokinetic parameters were calculated using computer program ＂3P87＂.Results：Linear range of the method was in 50-500 ng/ml.The recovery rates of three kinds of concentrations were 114.80±2.86,103.60±4.38,101.80±2.12,respectively.The minimum detectable concentration was 10 ng/ml.The difference in the day was 1.28% and the difference out of the day was 2.26% and the precision was less than 3%;T（peak） was 77.73 min.C（max） was 224.99 ng/ml.T1/2Ke was 72.91 min.T1/2Kawas 40.94 min.V/F（C） was 1.019（mg/kg）/（ng/ml）.AUC was 49553.47（ng/ml） min.Conclusions：The HPLC method had been established.The pharmacokinetic study of Cochinchinenin A was shown as one-compartment model.Cochinchinenin A＇s elimination half-life increased 178% compared with its absorption half-life.Cochinchinenin A could have great absorption and utilization after administration of EDB.