盐酸罗沙替丁醋酸酯脉冲控释微丸的研制

目的:制备盐酸罗沙替丁脉冲控释微丸(ROXPCP)。方法:取空白丸芯分别以含药层、溶胀层(含交联羧甲基纤维素钠)和控释层(含乙基纤维素水分散体)顺序包衣制备ROXPCP,通过考察不同类型空白丸芯、溶胀层材料及溶胀层与控释层的不同包衣增重对药物释放的影响来优选工艺,并进行处方验证试验。结果:各考察因素均对药物的释放影响显著。优选工艺结果为:空白丸芯采用蔗糖型,溶胀层材料采用交联羧甲基纤维素钠,溶胀层和控释层包衣增重分别为15%、24%。以此制备的微丸时滞时间为4h左右,时滞后4h内累积释药百分率达到80%。结论:所制备的ROXPCP具有体外脉冲控释作用。

Preparation of Roxatidine Aidcetic Hydrochloride Pulsatile Controlled-release Pellets

OBJECTIVE： To prepare the roxatidine aidcetic hydrochloride pulsatile controlled-release pellets （ROXPCP）. METHODS： Blank core were coated with Roxatidine aidcetic hydrochloride （ROX） as drug-containing layer, swelling agent containing croscarmellose sodium and controlled-release layer containing ethylcellulose aqueous dispersion respectively to prepare ROXPCP. The effects of the materials of blank core and swelling layer, the weight of swelling layer and controlled-release layer on the release of ROX were investigated to optimize process technology and validate formula. RESULTS： The release behavior was influenced strikingly by the types and weight of coating layer. The optimal formula was as follows： ROXPCP were prepared using croscarmellose sodium as inner layer with 15% （weight） coating level and ethylcellulose aqueous dispersion （surelease） as outer controlled-release layer with 24% （weight） coating level. The lag time of prepared pellets was about 4 h and accumulative release rate reached 80% within 4 h. CONCLUSIONS： The drug release of ROXPCP was shown in pulsatile way in vitro.