穿心莲内酯脂质体的制备及质量控制

Preparation and Quality Conrol of Andrographolide Liposomes

目的:制备穿心莲内酯脂质体并建立其质量控制方法。方法:采用薄膜分散-超声法制备穿心莲内酯脂质体,以包封率为指标,通过正交试验考察大豆卵磷脂-胆固醇、大豆卵磷脂-穿心莲内酯、维生素E用量、超声时间对脂质体制备工艺的影响。观察所制备脂质体的形态和粒径,利用HPLC测定穿心莲内酯含量。结果:最佳制备工艺为大豆卵磷脂-胆固醇(6∶1),大豆卵磷脂-穿心莲内酯(4∶1),维生素E用量20 mg,超声时间5 min。制备的穿心莲内酯脂质体平均粒径625.8 nm,包封率81.35%,渗透率1.54%,穿心莲内酯线性范围8.16～48.96 mg.L-1(r=0.999 8)。结论:采用薄膜分散-超声法制备的穿心莲内酯脂质体粒径大小合适、包封率高、渗透率低,建立的质量控制方法可靠,为制备穿心莲内酯脂质体气雾剂奠定基础。

Objective ： To prepare androgra Method： Andrographolide liposomes was prepared pholide liposomes and establish its quality control method. by film dispersion-ultrasound method, with encapsulation efficiency as index, orthogonal test was adopted to investigate effects of ratio of soybean lecithin-cho!esterol, ratio of soybean lecithin-andrographolide, the amount of vitamin E and ultrasonic time on preparation technology of andrographolide liposomes. Particle size and morphology of these prepared liposomes was assessed. The content of andrographolide was determined by HPLC. Result： Optimum preparation technology was as following： ratio of soybean lecithin-cholesterin 6： 1, ratio of soybean lecithin-andrographolide 4： 1, the amount of vitamin E 20 mg, ultrasonic time 5 min. Morphology of prepared liposome showed sphere structure with uniform diameter. The average particle size was 625.8 nm and encapsulation efficiency was 81.35% , rate of leakage was 1.54%. The linear range of andrographolide was 8. 16-48.96 mg ·L^- 1 （ r = 0. 999 8 ）. Conclusion ： Prepared andrographolide liposomes had high entrapment efficiency and low leakage rate, this established method for quality control was reliable, which lay foundation for preparing andrographolide liposomes aerosol.