pH依赖型肠可宁结肠靶向微丸的制备及体外释放研究
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摘要
目的制备pH依赖型肠可宁结肠靶向微丸并考察其体外释放特征。方法采用离心造粒法制备含药微丸,采用流化床包衣制备结肠靶向包衣微丸;以盐酸小檗碱为指标,评价微丸的体外释放特性。结果以微晶纤维素(MCC)为稀释剂,3%羟丙甲纤维素E5(HPMC E5)为黏合剂,以肠可宁药物粉末-MCC(5∶4)的处方投药量制备丸芯,以HPMC 2910包隔离衣增重3%,Eudrugit S100包肠溶衣增重25%,制备包衣微丸。其在人工胃液中2 h和在人工小肠液中3 h后累积释放度低于10. 00%,在人工结肠液中2 h累积释放度大于90. 00%。结论该方法制备的pH依赖型肠可宁结肠靶向微丸可初步实现结肠靶向释药特征。
Objective To prepare pH-dependent Changkening colon targeted pellets and evaluate its release performance in vitro.Methods The drug containing pellets were prepared by centrifugal granulation method and the colon targeted pellets were prepared by fluidized bed coating method. In vitro release performance of the pellets was evaluated with berberine hydrochloride as the index.Results The pellet cores were prepared by the prescription dosage of Changkening powder-microcrystalline cellulose( MCC)( 5 ∶ 4) with MCC as the diluent,and 3% hydroxypropyl methylcellulose E5( HPMCE5) as the adhesive. The colon targeted pellets were prepared with HPMC 2910 isolation coating and Eudrugit S100 enteric coating with the weight increase of 3% and 25%, respectively. In artificial gastric juice after 2 h and in artificial small intestinal juice after 3 h,the cumulative release rates of the coated pellets were less than10. 00%,and more than 90. 00% in artificial colon fluid after 2 h. Conclusion The pH-dependent Changkening colon targeted pellets prepared by this method can preliminary achieve the colon targeted drug release.
Objective To prepare pH-dependent Changkening colon targeted pellets and evaluate its release performance in vitro.Methods The drug containing pellets were prepared by centrifugal granulation method and the colon targeted pellets were prepared by fluidized bed coating method. In vitro release performance of the pellets was evaluated with berberine hydrochloride as the index.Results The pellet cores were prepared by the prescription dosage of Changkening powder-microcrystalline cellulose( MCC)( 5 ∶ 4) with MCC as the diluent,and 3% hydroxypropyl methylcellulose E5( HPMCE5) as the adhesive. The colon targeted pellets were prepared with HPMC 2910 isolation coating and Eudrugit S100 enteric coating with the weight increase of 3% and 25%, respectively. In artificial gastric juice after 2 h and in artificial small intestinal juice after 3 h,the cumulative release rates of the coated pellets were less than10. 00%,and more than 90. 00% in artificial colon fluid after 2 h. Conclusion The pH-dependent Changkening colon targeted pellets prepared by this method can preliminary achieve the colon targeted drug release.
引文
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[2] HUA S,MARKS E,SCHNEIDER JJ,et al. Advances in oral nano-delivery systems for colon targeted drug delivery in inflammatory bowel disease:selective targeting to diseased versus healthy tissue[J]. Nanomedicine,2015,11(5):1117-1132.
[3]张丹参,梅燕飞,宋晓敏,等.大黄结肠靶向微丸的制备及处方优化[J].中草药,2016,47(8):1321-1326.
[4]李闻涛,万科,杨莹,等.何首乌抗性淀粉促进靶向结肠微丸体外药物释放研究[J].中国药业,2017,26(17):6-9.
[5]国家药典委员会.中华人民共和国药典(四部)[M].北京:中国医药科技出版社,2015:121-124.
[6] SINGH G,KUMAR D,SINGH M,et al. Emerging Techniques and Challenges in Colon Drug Delivery Systems[J]. J Appl Pharm Sci,2012,2(3):139.
[7] BISWARANJAN SM,ANKIT J,ASHISH J,et al. Eudragit S-100coated citrus pectin nanoparticles for Colon Targeting of 5-Fluorouracil[J]. Materials,2015,8:832-849.
[8]翟海民,冯玲,于长安,等.口服结肠定位给药系统中载体材料和剂型的选择[J].药物生物技术,2014,21(3):260-263.
[9]王勇,岳国超,王红军,等.挤出滚圆法在中药微丸中的应用[J].中国药业,2013,22(11):1-3.
[10]戚秋鹏,王中彦,莫凤奎.离心造粒法制备中药浸膏微丸的影响因素[J].中国医药工业杂志,2004,35(1):25-27.