The objective of this study was to prepare tamsulosin hydrochloride-sustained release(TSH-SR)pellets which showed good release stability with frame-controlled method.TSH was added to Eudragit~?NE30D and Eudragit~?L30D...The objective of this study was to prepare tamsulosin hydrochloride-sustained release(TSH-SR)pellets which showed good release stability with frame-controlled method.TSH was added to Eudragit~?NE30D and Eudragit~?L30D-55 polymers to form drug-loaded inner core.Afterwards,enteric Eudragit~?L30D-55 polymer was modified on the surface of it to the final product.Dissolution studies showed that TSH-SR pellets were more stable during the coating process,different curing temperatures and storage conditions compared with TSH pellets produced by film-controlled technique.Appearances and glass transition temperatures(Tgs)of free films and surface morphologies observed by scanning electron microscopy(SEM)of blank sustained release pellets prepared by different ratios of Eudragit~?NE30D and Eudragit~?L30D-55 further indicated that temperature and relative humidity(RH)were the key factors when Eudragit~?NE30D blended with Eudragit~?L30D-55 were applied to sustained/controlled release preparations.In addition,SEM identified the surface morphologies of TSH-SR pellets before and after dissolution,which showed intact surface structure and great correlation with release curve respectively.展开更多
Eudragit~ NE 30D作为一种常用的缓释包衣、缓释骨架及掩味包衣材料,在药物制剂中应用广泛。而该类水分散体成膜机理较为复杂,对药物释放控制存在不稳定性现象,即物理老化,也是目前该品种应用中存在的最为突出的问题。本文基于丙烯酸...Eudragit~ NE 30D作为一种常用的缓释包衣、缓释骨架及掩味包衣材料,在药物制剂中应用广泛。而该类水分散体成膜机理较为复杂,对药物释放控制存在不稳定性现象,即物理老化,也是目前该品种应用中存在的最为突出的问题。本文基于丙烯酸树脂成膜机理研究,结合国内外相关文献报道,对Eudragit~ NE 30D物理老化问题的解决及预防措施进行归纳总结,从而促进其在药物制剂,特别是在缓控释制剂中的应用。展开更多
目的:制备非诺贝特缓释微丸。方法:采用BZJ-360M离心包衣造粒机制备微晶纤维素空白丸核和非诺贝特含药素丸,并在此基础上进行丙烯酸树脂水分散体(Eudragit NE 30D)包衣。用释放度测定法考察影响药物释放的各种因素,对包衣微丸体外释药...目的:制备非诺贝特缓释微丸。方法:采用BZJ-360M离心包衣造粒机制备微晶纤维素空白丸核和非诺贝特含药素丸,并在此基础上进行丙烯酸树脂水分散体(Eudragit NE 30D)包衣。用释放度测定法考察影响药物释放的各种因素,对包衣微丸体外释药机制进行研究。结果:包衣材料为Eudragit NE 30D,增重3%时包衣微丸呈现良好的缓释效果,体外释药过程基本符合Higuchi方程:Q=0.436+30.316t1/2(r=0.9997)。结论:成功的制备了非诺贝特缓释微丸。展开更多
目的制备日服2次的盐酸曲马多缓释微丸。方法选用Eudragit NE 30D作为包衣缓释材料,采用Glatt流化床底喷溶液上药法制备载药微丸,并进行缓释包衣。结果所制得的缓释微丸在1、4、8h的释放率分别为标示量的30%～33%,60%～66%和80%～83%,...目的制备日服2次的盐酸曲马多缓释微丸。方法选用Eudragit NE 30D作为包衣缓释材料,采用Glatt流化床底喷溶液上药法制备载药微丸,并进行缓释包衣。结果所制得的缓释微丸在1、4、8h的释放率分别为标示量的30%～33%,60%～66%和80%～83%,药物的释放行为符合中国药典2005版对该缓释制剂释放度的相关规定。结论本研究工艺简便,重现性良好,有望进行工业化生产。展开更多
文摘The objective of this study was to prepare tamsulosin hydrochloride-sustained release(TSH-SR)pellets which showed good release stability with frame-controlled method.TSH was added to Eudragit~?NE30D and Eudragit~?L30D-55 polymers to form drug-loaded inner core.Afterwards,enteric Eudragit~?L30D-55 polymer was modified on the surface of it to the final product.Dissolution studies showed that TSH-SR pellets were more stable during the coating process,different curing temperatures and storage conditions compared with TSH pellets produced by film-controlled technique.Appearances and glass transition temperatures(Tgs)of free films and surface morphologies observed by scanning electron microscopy(SEM)of blank sustained release pellets prepared by different ratios of Eudragit~?NE30D and Eudragit~?L30D-55 further indicated that temperature and relative humidity(RH)were the key factors when Eudragit~?NE30D blended with Eudragit~?L30D-55 were applied to sustained/controlled release preparations.In addition,SEM identified the surface morphologies of TSH-SR pellets before and after dissolution,which showed intact surface structure and great correlation with release curve respectively.
文摘Eudragit~ NE 30D作为一种常用的缓释包衣、缓释骨架及掩味包衣材料,在药物制剂中应用广泛。而该类水分散体成膜机理较为复杂,对药物释放控制存在不稳定性现象,即物理老化,也是目前该品种应用中存在的最为突出的问题。本文基于丙烯酸树脂成膜机理研究,结合国内外相关文献报道,对Eudragit~ NE 30D物理老化问题的解决及预防措施进行归纳总结,从而促进其在药物制剂,特别是在缓控释制剂中的应用。
文摘目的:制备非诺贝特缓释微丸。方法:采用BZJ-360M离心包衣造粒机制备微晶纤维素空白丸核和非诺贝特含药素丸,并在此基础上进行丙烯酸树脂水分散体(Eudragit NE 30D)包衣。用释放度测定法考察影响药物释放的各种因素,对包衣微丸体外释药机制进行研究。结果:包衣材料为Eudragit NE 30D,增重3%时包衣微丸呈现良好的缓释效果,体外释药过程基本符合Higuchi方程:Q=0.436+30.316t1/2(r=0.9997)。结论:成功的制备了非诺贝特缓释微丸。
文摘目的制备日服2次的盐酸曲马多缓释微丸。方法选用Eudragit NE 30D作为包衣缓释材料,采用Glatt流化床底喷溶液上药法制备载药微丸,并进行缓释包衣。结果所制得的缓释微丸在1、4、8h的释放率分别为标示量的30%～33%,60%～66%和80%～83%,药物的释放行为符合中国药典2005版对该缓释制剂释放度的相关规定。结论本研究工艺简便,重现性良好,有望进行工业化生产。
文摘目的制备肠溶性包衣膜,考察混合膜材以及添加剂对膜材性质的影响。方法采用平面铸膜法制备Eudragit NE30D/L 30D-55及Eudragit FS 30D/L 30D-55游离膜,并以膜的透湿性、机械性能为指标,考察膜材比例及添加剂[增塑剂柠檬酸三乙酯(TEC)、抗黏剂单硬脂酸甘油酯(GMS)、乳化剂吐温80(Tween-80)]对游离膜的影响。结果 Eudragit NE 30D及Eudragit FS 30D的加入能够增加Eudragit L 30D-55膜材的延展性、弹性和耐撞击负载的能力,同时也会减小膜材的强度、增加其透湿性。Eudragit L 30D-55与Eudragit NE 30D的混合膜材透湿性较大,对于湿度敏感性药物,应尽量避免选择透湿性大的包衣膜材。TEC和Tween-80的加入可改善膜材的柔韧性和弹性,降低膜材的强度,同时,TEC的加入可以增加膜材的透湿性,而GMS对膜材各项机械性质和透湿性影响不大。结论通过简单的调节混合膜材的种类、比例、添加剂的用量可以制得符合要求的肠溶游离膜。
