论文部分内容阅读
目的对家兔一次性颈静脉给药,检测自制药物与普通阿霉素在药动力学方面有无差异及了解新药的药动学特点。方法家兔12只,随机分为两组,每组6只,均予颈静脉置管、注射、抽血,一组按3.0mg/kg给予阿霉素;一组按63.2mg/kg给予半乳糖化白蛋白磁性阿霉素纳米粒,每次抽血1ml,分离血清低温保存,以氯仿-甲醇液萃取阿霉素,在高效液相色谱仪下检测色谱峰高。根据阿霉素标准曲线求血清中阿霉素浓度。以“3P87”进行药动学分析。结果阿霉素与半乳糖化白蛋白磁性阿霉素纳米粒在家兔体内的药动学规律符合三室开放模型;与阿霉素相比,实验组药物的消除相半衰期延长了1.9～3.2倍,清除率是阿霉素的0.5369倍;血药浓度-时间曲线下面积(AUC)是阿霉素的1.3697倍。结论阿霉素经过与白蛋白、磁性微粒结合,并以半乳糖修饰,改变了原药的体内分布特性,延长了药物半衰期,增加了靶器官肝脏的药物浓度。
Objective To study the pharmacokinetics of home-made drugs and common doxorubicin in rabbits by intravenous jugular vein. Methods Twelve rabbits were randomly divided into two groups with 6 rats in each group. All rabbits were injected with jugular vein and injected with blood. One group was given doxorubicin at 3.0mg / kg. One group was given half a dose of 63.2mg / kg Lactose albumin magnetic doxorubicin nanoparticles, each drawing 1ml, isolated serum cryogenic preservation, chloroform-methanol extraction of doxorubicin, high performance liquid chromatography detection of chromatographic peak height. According to doxorubicin standard curve serum concentration of doxorubicin. Pharmacokinetic analysis with “3P87”. Results The pharmacokinetics of doxorubicin and galactosylbumin magnetic doxorubicin nanoparticles in rabbits was in accordance with the three-compartment open model. Compared with doxorubicin, the elimination half-life of the drug in the experimental group was prolonged by 1.9 to 3.2 times , Clearance rate is 0.5369 times doxorubicin; plasma concentration - time area under the curve (AUC) is 1.3697 times that of doxorubicin. Conclusion Adriamycin combined with albumin and magnetic particles modified with galactose changed the distribution characteristics of the drug in vivo, prolonged the half-life of drug and increased the drug concentration in liver of target organ.