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目的:考察磷脂组成对马钱子总生物碱隐形脂质体静脉注射后马钱子碱在体内分布的影响。方法:采用硫酸铵梯度法和隐形脂质体技术制备马钱子总生物碱脂质体,除去游离药物后,利用HPLC测定马钱子碱的含量,流动相乙腈-0.01mol·L-1庚烷磺酸钠与0.02 mol·L-1磷酸二氢钾等量混合液(24∶76),检测波长264 nm。比较马钱子总生物碱溶液和不同磷脂组成马钱子总生物碱隐形脂质体静脉注射给药后马钱子碱的组织分布情况。结果:不同磷脂组成脂质体中马钱子碱占总生物碱的质量分数在26%~31%。与大豆磷脂隐形脂质体相比,马钱子总生物碱复合磷脂隐形脂质体静脉注射给药5 min后在血液和小肠中的浓度分别增加了2.35,1.34倍;而氢化大豆磷脂隐形脂质体在血液中的浓度极显著增加,给药后5 min的浓度增加了8.52倍,并且在脾、肺、心等组织中的浓度也明显增加,在小肠中浓度显著下降。结论:磷脂组成对马钱子总生物碱隐形脂质体的体内分布有显著影响。
Objective: To investigate the effect of phospholipid composition on the distribution of brucine in vivo after intravenous injection of total alkaloids of Strychnos nux - vomica. Methods: Strychnostella pneumoniae liposomes were prepared by ammonium sulfate gradient method and invisible liposome technique. After free drug was removed, the content of brucine was determined by HPLC. The mobile phase was acetonitrile-0.01mol·L-1 Sodium alkanesulfonate was mixed with 0.02 mol·L-1 potassium dihydrogen phosphate (24:76) at a detection wavelength of 264 nm. To compare the tissue distribution of brucine in the total alkaloids solution of Strychnos nux-vomica and the composition of different phospholipids composed of strychnos alkaloids stealth liposomes administered intravenously. Results: The mass fraction of brucine in different phospholipid liposomes was 26% ~ 31% of total alkaloids. Compared with soybean lecithin stealth liposomes, Strychnos alkaloids compound phospholipid stealth liposomes intravenous injection of 5 min after the blood and small intestine in the concentration increased by 2.35,1.34 times; and hydrogenated soybean lecithin stealth fat The concentration of plastid in the blood increased significantly, and the concentration of plastid in the blood increased 8.52-fold 5 min after administration. The concentration of plastid in the spleen, lung, heart and other tissues also increased significantly, and the concentration in the intestine decreased significantly. Conclusion: The phospholipid composition has a significant effect on the in vivo distribution of the total alkaloid stealth liposomes of Strychnos nux vomica.