石杉碱甲脂质体肌肉注射对小鼠脑缺血模型的长效缓释作用

中国药物评价 ›› 2021, Vol. 38 ›› Issue (5): 398-404.

石杉碱甲脂质体肌肉注射对小鼠脑缺血模型的长效缓释作用

王瑜歆1，臧广喜2，3*，于耀宏2

1. 辽宁省检验检测认证中心，辽宁沈阳 110036；
2. 沈阳药科大学，辽宁沈阳 110016；
3. 广州慧柏瑞生物医药科技有限公司，广东广州 510000

收稿日期:2021-06-15 修回日期:2021-09-22 出版日期:2021-10-28 发布日期:2021-10-28

Huperzine A Liposome Intramuscular Injection on Cerebral Ischemia Mouse Model for Long-term Control Release Effect

1. Liaoning Inspection，Examination & Certification Centre， Liaoning Shenyang， 110036， China；
2. Shenyang Pharmaceutical University， Liaoning Shenyang 110016， China；
3. Guangzhou HuiBoRui Biological Pharmaceutical Technology Co.， Ltd， Guangdong Guangzhou 510000， China

Received:2021-06-15 Revised:2021-09-22 Online:2021-10-28 Published:2021-10-28

摘要/Abstract

摘要： 目的：小鼠脑缺血再灌注制备缺血性痴呆（AD）动物模型，采用肌肉注射石杉碱甲脂质体（HUPAL），考察石杉碱甲脂质体肌肉注射后对小鼠脑缺血模型的长效缓释作用。方法：采用硫酸铵梯度法制备HUPAL，采用小鼠的脑缺血再灌注为痴呆模型（AD），HUPAL 给药后考察实验动物行为学变化，并以大脑皮层乙酰胆碱酯酶水平的高低为评价指标，验证HUPAL的长效缓释作用。结果：采用硫酸铵梯度法制备HUPAL，小鼠脑缺血再灌注动物肌肉注射HUPAL，逃逸潜伏期和逃逸实验中犯错的次数明显降低（P≤0.01）。HUPA溶液剂和HUPAL制剂在同样的给药剂量下，脂质体发挥更长的药理效应。结论：通过硫酸铵梯度法制备的石杉碱甲脂质体（HUPAL），肌肉注射小鼠脑缺血实验动物模型，可以显著延长HUPAL药理作用，达到降低给药次数的目的。

关键词: font-size:medium, ">石杉碱甲脂质体；长效缓释；(NH4)2SO4梯度法；胆碱酯酶抑制剂

Abstract: Objective： Animal model of ischemic stroke were developed to test Huperzine A Liposomes controlled release and long time effect. Methods： Huperzine A Liposomes were developed by ammonium sulfate [(NH4)2SO4] gradient， a novel mouse model of subcortical infarcts with dementia. Comparing with HUPA solution， Huperzine A Liposomes muscle tremors and time slobber extent was decreased after administration of HUPA liposomes. According to the results of Morris test， The ability of learning and memory in vascular dementia mice were both enhanced in group HUPA liposomes and group HUPA solution. Results： After intramuscular injection of Huperzine A Liposomes， HUAPLgroup inhibition of acetylcholinesterase percentage were statistically significant compared with the control group. HUPAL 1.0 mg·kg-1 group， 1，3 days remain a significant inhibitory effect. Other treatment group compared with the control group， no difference in inhibition of acetylcholinesterase percentage. Conclusion： Huperzine A liposome formulation has long-term sustained-release effect and reduces the times of drug administration.

Key words: font-size:medium, ">Huperzine A Liposomes；Long-time control release； Ammonium sulfate gradient； Cholinesterase inhibitor

中图分类号:

王瑜歆, 臧广喜, 于耀宏. 石杉碱甲脂质体肌肉注射对小鼠脑缺血模型的长效缓释作用[J]. 中国药物评价, 2021, 38(5): 398-404.

WANG Yu-xin, ZANG Guang-xi, YU Yao-hong, . Huperzine A Liposome Intramuscular Injection on Cerebral Ischemia Mouse Model for Long-term Control Release Effect[J]. CHINESE JOURNAL OF DRUG EVALUATION, 2021, 38(5): 398-404.

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