石杉碱甲前体液晶制剂的制备及释放度研究  

Preparation and release of huperzine A precursor liquid crystal formulations

作　　者：郭偲 周萌萌 潘倩文 李力[1] 刘宏 罗亮[4] 

机构地区：[1]中国人民解放军武汉总医院药剂科,武汉430070 [2]湖北中医药大学药学院,武汉430065 [3]国家纳米药物工程技术研究中心,武汉430075 [4]华中科技大学生命与技术学院,武汉430070

出　　处：《中国新药杂志》2017年第23期2859-2863,共5页Chinese Journal of New Drugs

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。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.

关 键 词：石杉碱甲 大豆卵磷酯 二油酸甘油酯 无水乙醇 缓释 

分 类 号：R943.41[医药卫生—药剂学]