【摘要】 本文建立了异牡荆苷在大鼠血浆及不同组织中的高效液相色谱检测方法,采用RP-C₁₈色谱柱（250mm×4.6mm,5.0μm）,以甲醇-1%冰醋酸溶液（40:60,v/v）为流动相,柱温为30℃,检测波长为338nm。通过专属性、精密度、线性、准确度、稳定性、提取回收率、最低定量限等方法学考察,证实本方法可对血浆及不同组织中的异牡荆苷进行准确检测。在此方法的基础上研究了异牡荆苷在大鼠体内的药代动力学及组织分布特征。大鼠在静脉注射异牡荆苷后,在预定的时间点取样检测。结果显示异牡荆苷在高、中、低剂量（18.75,3.75,0.75mg/kg）药代动力学特征符合二室模型,在所研究的剂量范围内AUC与给药剂量呈现良好的线性相关性,符合线性动力学特征。药物t_1/2α为1.54-1.84min,t_1/2β为36.94-46.27min。异牡荆苷在组织中的浓度分布从高到低分别为肾>肝>肺≈卵巢>心≈脾>脑。更多还原

【Abstract】 An HPLC method for the determination of isovitexin in rat plasma and different tissues was developed.The separation was achieved on a C₁₈column with a mobile phase consisting of methanol-1% acetum（40:60,v/v）at a detection wavelength of 338 nm and a column temperature of 30℃.Rutin was chosen as the internal standard.The linear range of the standard curves was 0.20-128.75μg/mL in the plasma and 0.024-3.09μg/mL in the tissues.The LOQ was 0.19μg/mL in the plasma and 0.024μg/mL in the tissues.The relative recoveries of isovitexin ranged from 93% to 105% in the plasma and 87% to 112% in the tissues.The intra-and inter-day precisions were all below 8%.The pharmacokinetics and tissue distribution of isovitexin in rats were studied with the method.Blood samples were collected at fixed time intervals after the i.v.injection of isovitexin at a dosage of 18.75,3.75 and 0.75 mg/kg;the tissue samples（brain,liver,kidney,heart,lung,spleen and ovary）were obtained at 10,30,and 60 min after the i.v.injection of isovitexin at a dosage of 18.75 mg/kg.The pharmacokinetics of the isovitexin in three different dosages in the rats fit the two-compartment open model.The isovitexin displayed linear dynamics in the dosage range of 0.75-18.75 mg/kg.The mean value of t_1/2αwas 1.54-1.84 min,and t_1/2βwas 36.94-46.27 min at the three dosages.The tissue distribution study showed that the sequence of tissue drug concentration from high to low was kidney>liver>lung≈ovary>heart≈spleen>brain.更多还原