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目的研究马钱子碱聚乳酸纳米粒(Bru-PLA-NPs)iv注射给药后在家兔体内的药动学行为。方法建立HPLC法测定家兔血浆中马钱子碱浓度。色谱柱为Kromasil C18(250mm×4.6mm,5μm);流动相为乙腈-水(23:77),水中含庚烷磺酸钠1.01g/L,磷酸二氢钾1.36g/L,加磷酸调节pH至2.8;体积流量为1mL/min;检测波长为265nm;柱温为25℃。采用3p87软件计算马钱子碱药动学参数。结果单剂量ivBru-PLA-NPs(4mg/kg)后马钱子碱在兔体内的药动力学数据符合三室模型,单剂量静注马钱子碱溶液(4mg/kg)后符合二室模型;与马钱子碱溶液相比,Bru-PLA-NPs给药后,马钱子碱的消除半衰期(t1/2β)提高6.6倍;生物利用度提高8.7倍。结论与马钱子碱溶液相比,Bru-PLA-NPsiv给药后马钱子碱在家兔体内的药动学行为发生了显著变化。
Objective To study the pharmacokinetics of Brucine-PLA-NPs in rabbits after iv injection. Methods HPLC method was established to determine the concentration of strychnine in rabbit plasma. The column was Kromasil C18 (250mm×4.6mm, 5μm); the mobile phase was acetonitrile-water (23:77), the water contained sodium heptane sulfonate 1.01g/L, potassium dihydrogen phosphate 1.36g/L, phosphoric acid regulation pH to 2.8; volumetric flow rate 1 mL/min; detection wavelength 265 nm; column temperature 25°C. The pharmacokinetic parameters of strychnine were calculated using 3p87 software. Results The pharmacokinetics data of strychnine in rabbits after single dose of ivBru-PLA-NPs (4mg/kg) met the three-compartment model. The single-dose strychnine solution (4mg/kg) was in accordance with the two-compartment model. Compared with strychnine solution, the elimination half-life of strychnine (t1/2β) increased 6.6-fold and the bioavailability increased 8.7-fold after administration of Bru-PLA-NPs. Conclusion Compared with strychnine solution, the pharmacokinetics of strychnine in rabbits changed significantly after administration of Bru-PLA-NPsiv.