阿莫西林脉冲释药微丸的研制

目的:制备阿莫西林脉冲释药微丸。方法:取空白丸芯分别以含药层、溶胀层(羧甲基淀粉钠)和控释层(乙基纤维素水分散体)顺序依次进行包衣制备阿莫西林脉冲释药微丸。采用紫外法和篮法考察溶胀层(12%、16%、20%)和控释层包衣增重(24%、28%、32%)及不同介质(水、盐酸、pH6.8磷酸盐缓冲液)对药物释放的影响。结果:溶胀层和控释层包衣增重对脉冲控释微丸的释药时滞和释放速率具有显著影响,药物释放情况不受介质pH值的影响;溶胀层和控释层包衣增重分别为16%、28%时制备的微丸时滞时间约为4h,时滞后4h累积释药率达到80%。结论:所制备的阿莫西林脉冲释药微丸具有体外脉冲释放作用。

Preparation of Amoxicillin Pulsatile Release Pellets

OBJECTIVE:To prepare Amoxicillin pulsatile release pellets.METHODS:Blank core were coated with amoxicillin as drug-containing layer,swelling agent containing sodium carboxymethyl starch and controlled-release layer containing ethylcellulose aqueous dispersion respectively to prepare Amoxicillin pulsatile release pellets.UV method and basket method were used to investigate the weight increment of coating in swelling layer(12%,16%,20%),controlled-release layer(24%,28%,32%) and effects of different solvents(water,hydrochloric acid,pH 6.8 phosphoric acid buffer solution) on drug release.RESULTS:The weight increment of coating in swelling layer and controlled-release layer had significant effect on lag time and velocity of drug release,and the drug release wasn’t influenced by pH value of medium.The coating weight of swelling layer and controlled-release layer increased by 16% and 28%,the lag time of prepared pellets was about 4 h and accumulative release rate reached 80% within 4 h.CONCLUSIONS:The drug release of Amoxicillin pulsatile release pellets is shown in pulsatile way in vitro.