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高乌甲素磷脂复合物及其固体分散体在大鼠体内的药动学 预览

Pharmacokinetics of Lappaconitine-phospholipid Complex and Its Solid Dispersion in SD Rats in Vivo
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摘要 目的比较高乌甲素磷脂复合物及其固体分散体在SD大鼠体内的生物利用度。方法采用溶剂挥发法制备高乌甲素磷脂复合物及其固体分散体,X线衍射(XRD)法分析高乌甲素在磷脂复合物及其固体分散体的存在状态。SD大鼠分别灌胃给予高乌甲素原料药、磷脂复合物及磷脂复合物固体分散体(按高乌甲素计:5 mg·kg-1),取血,以延胡索乙素为内标,高效液相色谱(HPLC)法测定血高乌甲素浓度,并计算主要药动学参数。结果高乌甲素磷脂复合物及其固体分散体的AUC 0~t与原料药相比都有显著性提高,其中磷脂复合物的AUC 0~t提高了1.41倍;固体分散体的AUC 0~t提高了2.04倍,且C max显著提高。结论高乌甲素磷脂复合物及其固体分散体均可提高高乌甲素的口服生物利用度,且但高乌甲素磷脂复合物固体分散体效果更优。 Objective To compare the relative bioavailability of lappaconitine phospholipids complex and itssolid dispersion.Methods Solvent evaporation method was employed to preparelappaconitine phospholipids complex and its solid dispersion,and their existential state was analyzed by X-ray diffraction(XRD).After each of groups of SD rats were administered intragastrically with lappaconitine,phospholipid complex,and its solid dispersion,respectively(equivalent to 5 mg·kg-1 of lappaconitine).The blood samples were collected at different time intervals.The concentration of lappaconitine in blood was analyzed by HPLC method using tetrahydropalmatine as internal standard,and then the main pharmacokinetic parameters were calculated.Results The AUC 0~t of the phospholipids complex and its solid dispersions were significantly increased as compared with that of lappaconitine.The AUC 0~t of phospholipid complex and its solid dispersion were increased by 1.41 and 2.04 times as compared to lappaconitine suspension,respectively.Conclusion The phospholipids complex and its solid dispersion could enhance the oral bioavailability of lappaconitine in SD rates notably.However,the bioavailability of lappaconitine phospholipids complexsolid dispersion is greater than that of phospholipids complex.
出处 《医药导报》 CAS 北大核心 2018年第4期449-452,共4页 Herald of Medicine
关键词 高乌甲素 磷脂复合物 固体分散体 生物利用度 Lappaconitine Phospholipids complex Solid dispersion Bioavailability
作者简介 刘蒸生(1982-),男,湖南邵东人,主治医师,研究方向:肿瘤内科治疗。电话:0731-85295929,E-mail:liuzs20007@126.com。;通信作者:马进安(1973-),男,湖南常德人,教授,硕士生导师,研究方向:肿瘤内科治疗。电话:0731-85295929,E-mail:maja2007@126.com。
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