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目的建立石杉碱甲脂质体(huperzine A liposome,HUPA-L)的制备方法。方法采用pH梯度、硫酸铵[(NH4)2SO4]梯度、乙二胺四乙酸铵(NH4EDTA)梯度方法制备HUPA-L,以阳离子交换树脂分离脂质体和游离药物,HPLC法测定HUPA-L的包封率,并考察温度、孵化时间及药脂比对HUPA-L包封率的影响。体外释放实验研究HUPA-L的释放行为。结果硫酸铵梯度法制备的HU-PA-L包封率最高,包封率随着硫酸铵浓度和温度的升高而增加,随着药脂比的降低而增大,当药物与磷脂质量比小于1∶100时,HUPA-L包封率可达100.0%;HUPA-L体外释放呈现明显的缓释效果。结论硫酸铵梯度法是制备HUPA-L优选方法,硫酸铵的浓度、温度和药脂比是影响包封率的重要因素。
Objective To establish a method for the preparation of huperzine A liposome (HUPA-L). Methods HUPA-L was prepared by pH gradient, ammonium sulfate [(NH4) 2SO4] gradient and ammonium ethylenediaminetetraacetate (NH4EDTA) gradient method. The liposomes and free drugs were separated by cation exchange resin. The contents of HUPA-L Encapsulation efficiency, and investigated the temperature, incubation time and drug-lipid ratio HUPA-L encapsulation efficiency. In vitro release experiments HUPA-L release behavior. Results The encapsulation efficiency of HU-PA-L prepared by ammonium sulfate gradient method was the highest. The entrapment efficiency increased with the increase of ammonium sulfate concentration and temperature, and increased with the decrease of lipid-lipid ratio. When the mass ratio of drug to phospholipid The encapsulation efficiency of HUPA-L reached 100.0% when the ratio was less than 1: 100. The sustained release of HUPA-L in vitro showed a sustained release effect. Conclusion The ammonium sulfate gradient method is the best method to prepare HUPA-L. The concentration of ammonium sulfate, the temperature and the ratio of lipid to lipid are the important factors affecting the entrapment efficiency.