中国中药杂志

2014, v.39(13) 2489-2494

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麦冬多糖MDG-1油混悬长效注射剂的制备及药动学评价
Preparation and pharmacokinetic evaluation of long-acting injectable oily suspensions for Ophiopogonis Radix polysaccharide MDG-1

时潇丽;姚春霞;林晓;沈岚;冯怡;
SHI Xiao-li;YAO Chun-xia;LIN Xiao;SHEN Lan;FENG Yi;College of Chinese Materia Medica,Shanghai University of Chinese Materia Medica;Engineering Research Cener of Modern Preparation Technology of Traditional Chinese Medicine of Ministry of Education,Shanghai University of Traditional Chinese Medicine;

摘要(Abstract):

目的:对制备的不同处方的注射用麦冬多糖MDG-1油混悬剂进行大鼠体内药动学评价,探究利用油性混悬释药系统以实现MDG-1注射长效给药的可行性。方法:采用反溶剂沉淀法制备MDG-1微粒,对其粒径、粒径分布进行表征;在低黏度的大豆油中加入高黏度的蓖麻油或加入硬脂酸铝,制备不同黏度的油性介质,对其进行流变学性质考察,筛选较优处方进行体内评价。结果:微粒体积平均粒径D(4,3)为21.81μm,径距为2.63;对筛选的大豆油-蓖麻油混合油(2∶3)及2%,4%硬脂酸铝凝胶化大豆油处方进行体内评价,其中4%硬脂酸铝凝胶化大豆油处方能够极显著降低Cmax,显著延长表观t1/2,MDG-1释放时间可达数天。结论:利用高黏度的油性介质来实现MDG-1注射长效给药具有可行性。
Objective: To evaluate in vivo pharmacokinetics of Ophiopogonis Radix polysaccharide MDG-1 oily suspension injection prepared with different prescriptions in rats,and explore the feasibility of the long-acting drug delivery of MDG-1 Injection by using the oily suspension drug release system. Method: MDG-1 microparticles were prepared by the anti-solvent precipitation method.Their size and size distribution were characterized. Castor oil with a high viscosity or aluminum stearate were added into soybean oil with a low viscosity,in order to prepare oily media with different viscosities,detect their rheological properties and screen out superior prescriptions for in vivo evaluation. Result: The average size of microparticles was 21. 81 μm,and the span between them was 2. 63.The in vivo evaluation was conducted for prescriptions of mixed oil(soybean oil /castor oil,2∶ 3) and soybean oils gelled by 2% and4% aluminium stearate. Among them,the prescription of soybean gelled by 4% aluminium stearate could significantly reduce Cmaxand prolong the apparent t1 /2,with the MDG-1 release time of several days. Conclusion: It is feasible to achieve the long-acting MDG-1drug delivery by using oily media with a high viscosity.

关键词(KeyWords): 麦冬;多糖;油混悬剂;长效注射剂;药物动力学
Ophiopogonis Radix;polysaccharide;oily suspension;long-acting injection;pharmacokinetics

Abstract:

Keywords:

基金项目(Foundation): 国家教育部“新世纪优秀人才支持计划”项目(NCET-13-0906)

作者(Authors): 时潇丽;姚春霞;林晓;沈岚;冯怡;
SHI Xiao-li;YAO Chun-xia;LIN Xiao;SHEN Lan;FENG Yi;College of Chinese Materia Medica,Shanghai University of Chinese Materia Medica;Engineering Research Cener of Modern Preparation Technology of Traditional Chinese Medicine of Ministry of Education,Shanghai University of Traditional Chinese Medicine;

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