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目的:比较马钱子碱脂质体与游离药物溶液的药物动力学。方法:大鼠尾静脉给药,以士的宁为内标,用HPLC法测定大鼠血浆中马钱子碱的浓度,用3p97程序拟合房室模型并计算药物动力学参数。结果:马钱子碱脂质体大鼠尾静脉单次给药血药浓度经时曲线符合三室模型,而游离马钱子碱溶液符合二室模型。与游离药物相比,马钱子碱脂质体的AUC(增加3.75倍)、CL、T1/2(延长了4.78倍)等药动学参数有显著改善。结论:马钱子碱脂质体具有比马钱子碱溶液更为理想的药物动力学性质。
OBJECTIVE: To compare the pharmacokinetics of strychnine liposomes with free drug solution. Methods: The tail vein of rats was administered with strychnine as internal standard. The concentration of brucine in rat plasma was determined by HPLC. The pharmacokinetic parameters were calculated by 3p97 program. Results: The single-dose plasma concentration of strychnine-liposome rat tail vein curve in time fit the three-compartment model, while the free brucine solution conforms to the two-compartment model. The AUC (3.75-fold increase), CL, T1 / 2 (4.78-fold longer) pharmacokinetic parameters of brucine liposomes were significantly improved compared with the free drug. Conclusion: The strychnine liposomes have better pharmacokinetic properties than strychnine solution.