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目的:比较阿魏酸载脂质体壳聚糖微球、阿魏酸壳聚糖微球、阿魏酸原料药的药代动力学特征,探讨载脂质体壳聚糖微球这种新型药物载体的优势。方法:SD大鼠灌胃给予3种制剂后,定时取血,以香豆素为内标,甲醇-0.3%醋酸溶液(42∶58)为流动相,HPLC法320 nm检测血浆中的阿魏酸含量,绘制药时曲线,DAS程序计算药动学参数。结果:载脂质体壳聚糖微球的tmax,MRT,t1/2分别为2.500,7.487,7.818 h,较原料药的0.150,1.365,1.992 h,壳聚糖微球的1.000,4.171,4.857 h都有所延长;其AUC分别为原料药和壳聚糖微球的7.08,2.21倍。结论:载脂质体壳聚糖微球能延缓药物的释放并增进药物的吸收,有利于溶解度低、半衰期短的药物的口服给药。
OBJECTIVE: To compare the pharmacokinetics of ferulic acid-loaded chitosan microspheres, ferulic acid chitosan microspheres and ferulic acid as raw materials, and to explore the pharmacokinetics of liposome-loaded chitosan microspheres Advantages of drug carriers. Methods: SD rats were given intragastric administration of three kinds of preparations, blood was taken at a fixed time, coumarin as an internal standard, methanol-acetic acid solution (42:58) as the mobile phase, HPLC 320 nm detection of plasma in the ferulic Acid content, draw the drug curve, DAS program to calculate pharmacokinetic parameters. Results: The tmax, MRT and t1 / 2 of liposome-loaded chitosan microspheres were 2.500, 7.487 and 7.818 h, respectively, which were 0.150, 1.355 and 1.992 h respectively compared with that of the drug substance, 1.000, 4.171 and 4.857 h have been extended; the AUC were 7.08,2.21 times the drug substance and chitosan microspheres, respectively. CONCLUSION: Liposome-loaded chitosan microspheres can delay drug release and enhance drug absorption, which is good for oral administration of drugs with low solubility and short half-life.