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首页> 外文期刊>Journal of Microencapsulation: Microcapsules Liposomes Nanoparticles Microcells Microspheres >Microencapsulation of a hydrophilic drug into a hydrophobia matrix using a salting-out procedure.I:Development and optimization of the process using factorial design
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Microencapsulation of a hydrophilic drug into a hydrophobia matrix using a salting-out procedure.I:Development and optimization of the process using factorial design

机译：使用盐析程序将亲水性药物微囊化为疏水性基质I：使用析因设计开发和优化工艺

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The congealahle disperse phase method for preparing sustained release microspheres involves an emulsification process using water as the external phase and molten hydrophobic wax as the disperse phase into which the drug is loaded.Attempts to entrap highly water-soluble drugs using this process have often resulted in low loading efficiency as the drugs partition into the external water phase during emulsification and are lost.A novel method employing salts and wetting agents was developed to improve the loading efficiency of the highly water-soluble drug,guaifenesin,using this method.The drug/wax ratio (D/W) and the presence of salts and etting agents greatly influenced microsphere properties.To optimize the process for drug loading efficiency and release rate,three different D/Ws,salts and wetting agents were chosen and a full 3~3 factorial design experiment was performed.Any significant differences among the levels of the variables and their individual and joint effects on entrapment efficiency and T_(50) (time for 50% drug release) were determined.Entrapment efficiencies in the range 35.1- 86.3% were obtained for the various factor-level combinations of the variables.Particle size was in the range 140-385 mum and T_(50) was 0.59-2.72 h for the microspheres obtained.The D/W and type of salt used significantly affected drug entrapment and T_(50),while the nature of wetting agent was not significant at p<0.05.The microspheres prepared using 1:4 D/W showed the highest entrapment efficiency and slowest drug release.
机译：制备缓释微球的凝乳分散相法涉及以水为外相，熔融疏水蜡为分散相的乳化过程，这种方法试图将高水溶性药物截留。由于药物在乳化过程中分配到外部水相中并丢失而导致较低的负载效率。开发了一种使用盐和润湿剂的新方法来改善这种高度水溶性药物愈创甘油醚的负载效率。蜡比（D / W）以及盐和润湿剂的存在对微球的性能影响很大。为了优化药物装载效率和释放速率的过程，选择了三种不同的D / W，盐和润湿剂，并选择了全3〜进行了3个析因设计实验。变量水平之间的显着差异以及它们对包裹体的个体和联合影响确定了nt效率和T_（50）（药物释放50％的时间）。对于变量的各种因子水平组合，其包封效率为35.1-86.3％。颗粒大小在140-385微米范围内得到的微球的T_（50）为0.59-2.72 h。所用盐的D / W和盐类型显着影响药物的包封和T_（50），而润湿剂的性质在p <0.05时不显着。使用1：4 D / W制备的药物具有最高的包封效率和最慢的药物释放。

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