【摘要】 目的:制备石杉碱甲前体液晶制剂并考察其注射性能、形态特征及体外释放度。方法:以二油酸甘油酯和大豆卵磷酯为液晶材料、无水乙醇为溶剂、石杉碱甲为主药制备石杉碱甲前体液晶制剂;用流变仪测量出黏度随剪切速率的变化曲线;用偏光显微镜表征其吸水后形态变化;采用高效液相色谱法测定体外释放度。结果:不同配比的石杉碱甲前体液晶制剂均可以注射;当充分吸水后,大豆卵磷酯∶二油酸甘油酯=70∶30和60∶40时石杉碱甲前体液晶制剂在偏光显微镜下呈现出偏光纹理,其余比例则未呈现出偏光性;大豆卵磷酯∶二油酸甘油酯=70∶30的石杉碱甲前体液晶制剂在p H 7.4磷酸盐缓冲液(PBS 7.4溶液)中持续释药达168 h,累积释放率可达90%以上。结论:前体液晶可以作为石杉碱甲中长效释药体系。更多还原

【Abstract】 Objective:To prepare huperzine A precursor liquid formulations and study the injection performance,morphological characteristics and in vitro release.Methods:In the huperzine A precursor liquid crystal formulations,glyceryl dioleate(GDO) and soybean phospholipid(SPC) were used as liquid crystal forming materials,and ethanol was used as solvent.Huperzine A was loaded as the main drug at different ratios.The viscosities of the formulations were measured as a function of shear rate using a rheometer.The morphological change of the formulations after hydration was measured by polarize microscopy;In vitro release rate was determined by HPLC.Results:Different ratios of huperzine A precursor liquid crystal formulation are all injectable;When fully absorbing water,the huperzine A precursor liquid crystal formulations with SPC∶GDO=70∶30 and 60∶40 showed polarizing textures under polarized light,while other SPC∶GDO ratios did not show any birefringence;The release of SPC∶GDO=70∶30 huperzine A from the precursor liquid crystal formulation in pH 7.4 phosphate buffer solution(PBS pH 7.4 solution) lasted for over 168 h,with a cumulative release rate of above 90%.Conclusion:The precursor liquid crystal can be used as a long-acting drug delivery system for huperzine A.更多还原