挤出滚圆法制备克拉霉素微丸的处方工艺研究

目的应用挤出滚圆法制备克拉霉素微丸,研究微丸制备的最佳工艺和处方。方法采用挤出滚圆造粒机制备克拉霉素微丸;采用单因素考察和正交设计筛选最优化处方及工艺条件;评价了微丸的粉体学性质、收率和体外溶出度。结果用挤出滚圆法制备的克拉霉素微丸在30min内体外溶出均达80%以上,且圆整度好,收率高。结论挤出滚圆法制备克拉霉素微丸工艺简便易行,制得的微丸质量好,收率高,体外释药迅速。     

中心复合设计法优化丹七有效部位缓释微丸

目的:应用挤出滚圆法制备丹七提取物缓释微丸,研究微丸制备的最佳工艺和处方.方法:用挤出滚圆机制备丹七提取物缓释微丸;采用单因素考察和中心复合设计筛选最优处方和工艺条件;考察了微丸粉体学性质、收率和体外溶出度.结果:用挤出滚圆法制备的微丸圆整度好,大小均匀,收率高,药物体外溶出具有明显的缓释作用,体外释放曲线符合Peppas和Higuchi方程.结论:该工艺简便易行.     

挤出滚圆法制备中药复方当归补血微丸及其性质考察*

目的：应用挤出滚圆法制备中药复方当归补血微丸，研究微丸制备的最佳工艺和处方。方法：用新型的挤出滚圆造粒机制备当归补血微丸；采用单因素考察和正交设计筛选最优处方和工艺条件；考察了微丸的粉体学性质、收率和体外溶出效果。结果：用挤出滚圆技术制备的当归补血微丸圆整度好，大小均匀，收率高，体外溶出迅速。结论：挤出滚圆法可以制备中药微丸。该工艺简便易行，制得的微丸质量好。     

探究挤出滚圆法制备中药微丸的效果

目的:对应用挤出滚圆法制备中药复方杞芪微丸的效果进行探讨和分析。方法:采用新型挤出滚圆造粒机行复方杞芪微丸制备并对不同处方微丸的体外溶出度、收率以及粉体化学性质进行考察和分析。结果:3种处方微丸质量和收率均非常理想,处方A微丸质量和收率优于处方B和处方C,随着载药量的不断上升,微丸的流动性和圆整度会出现下降,收率会相应降低。3种处方微丸1小时内溶出度均超过80%,胶囊在40min内溶出度即可达到80%,杞芪微丸具有更佳的溶解度,制剂效果更优。结论:应用挤出滚圆法制备中药复方杞芪微丸具有较高的收率和较好的质量,而且具有非常理想的体外溶出效果,值得研究和应用。     

挤出滚圆法制备克拉霉素微丸及工艺优化

目的 制备克拉霉素含药微丸,并对制备处方及工艺进行筛选。方法 采用挤出滚圆技术制备微丸,对处方和工艺进行分析及筛选。结果 根据优选的处方和工艺制备的克拉霉素含药微丸,成型性好、收率高、体外溶出完全。结论 利用挤出滚圆法制备克拉霉素微丸,简单易行,制备的微丸质量好,值得进一步开发研究。     

挤出-滚圆和流化床包衣法制备盐酸二甲双胍肠溶微丸

目的研制盐酸二甲双胍肠溶微丸。方法采用挤出-滚圆工艺和流化床包衣法制备,用正交试验设计优化处方,考察产品的体外释放度。结果制得的盐酸二甲双胍肠溶微丸圆整度高、收率高、体外释放度好。结论所用制备工艺简单易行,重现性好。     

盐酸文拉法辛缓释胶囊制备

目的研究盐酸文拉法辛缓释胶囊的制备工艺和处方。方法首先用挤出滚圆造粒机制备盐酸文拉法辛微丸,微丸包衣,装胶囊,通过评价微丸的特征、收率和胶囊体外释放度,筛选最佳处方和工艺。结果用挤出滚圆法制备的盐酸文拉法辛微丸圆整度好,收率高。经包衣、填装胶囊制备的盐酸文拉法辛缓释胶囊的释放度与进口盐酸文拉法辛胶囊一致。结论挤出滚圆法制备盐酸文拉法辛微丸工艺简便易行,制得的微丸质量好,收率高;用乙基纤维素包衣获得满意的释放度。     

布地奈德肠溶微丸的制备

目的研制布地奈德肠溶微丸。方法采用挤出滚圆工艺及流化床包衣法制备了伐他汀钠肠溶肠溶微丸,并采用正交试验设计对处方进行了优化,考察了微丸的粉体学性质及不同包衣增重微丸的体外释放实验。结果制得的布地奈德微丸圆整度高、收率高、体外释放度好。结论本方法制备工艺简单易行,重现性好,值得进一步的工业化生产。     

挤出滚圆法制备阿托伐他汀钙速释微丸

目的采用挤出滚圆法制备阿托伐他汀钙速释微丸,研究处方及制备工艺。方法在单因素实验的基础上,以微丸的粉体学性质、收率和体外溶出度为评价指标,对影响微丸成型的关键工艺参数进行正交设计优化。结果用挤出滚圆法制备的阿托伐他汀钙速释微丸圆整度好、粒度分布窄、收率高,且在30 min体外溶出均在95%以上。结论成功地制备了阿托伐他汀钙微丸,该制备工艺重现性好、质量高,具有理想的速释效果。     

挤出滚圆法制备天山雪莲提取物骨架微丸

目的应用挤出滚圆法制备天山雪莲提取物骨架微丸,并研究微丸制备的最佳处方和工艺。方法采用单因素考察和正交设计,用挤出滚圆法筛选天山雪莲提取物骨架微丸最优处方和工艺条件;考察微丸的粉体学性质及累积释放度。结果制得微丸圆整度、均匀度、流动性及堆密度均较好,成品收率高,且30 min内体外释放度均>80%。结论本法制备的雪莲提取物骨架微丸,工艺简便易行,质量可控,收率高。     

挤出滚圆法制备间尼索地平-磺丁醚-β-环糊精微丸及其质量评价

目的制备具有较高水溶性的间尼索地平微丸。方法以磺丁醚-β-环糊精（SBE-β-CD）为成丸辅料,羟丙基纤维素乙醇溶液为黏合剂,采用挤出滚圆法制备间尼索地平微丸,对影响成球的关键参数挤出速度、滚圆转速进行筛选优化,对微丸体外释放进行评价,并对微丸进行粉体学性质的考察。结果制得的间尼索地平微丸水中溶出度高,圆整度好,收率可达70%,各项粉体学性质较为理想。结论以SBE-β-CD为成丸辅料,采用挤出滚圆法制备高水溶性的间尼索地平微丸在工艺上是可行的,对难溶性药物微丸的制备具有一定借鉴作用。     

黄柏微丸的制备和体外溶出度考察

目的：制备黄柏微丸并进行处方优化,考察微丸的体外溶出度。方法：用挤出滚圆造粒机制备黄柏微丸,优化制剂处方组成;采用高效液相色谱法以盐酸小檗碱有为指标,对其体外溶出度进行考察。结果：制得微丸圆整度好,大小均匀,收率在82%以上。盐酸小檗碱的溶出度60min内达88%以上。结论：本法研制的黄柏微丸,处方合理,工艺可行。     

中药素丸的制备工艺研究

本文以自制黄芩有效部位提取物药物固体分散体为原药,采用挤出滚圆法制备微丸。用此法制备微丸操作简便、效率高,制得的微丸圆整度好,大小均一,堆密度大,适宜进一步包衣。本文对微丸的处方及制备工艺进行了考察^[1]。     

普伐他汀钠肠溶小丸的制备

目的：研制普伐他汀钠肠溶小丸。方法：采用挤出滚圆工艺及流化床包衣法制备了普伐他汀钠肠溶小丸,并采用正交试验设计对处方进行了优化,考察了小丸的粉体学性质及不同包衣增重小丸的体外释放试验。结果：制得的普伐他汀钠小丸圆整度高,收率高,体外释放度也比较理想。结论：本方法制备工艺简单易行,重复性好,值得进一步的工业化生产。     

Synergistic effect of polyethylene glycol and superdisintegrant on dissolution rate enhancement of simvastatin in pellet formulation

Slow dissolution is a major drawback for poorly water-soluble drugs when they are extruded-spheronized with microcrystalline cellulose (MCC). Therefore, the aim of the current study was to explore excipients to enhance the dissolution of simvastatin without compromising the extrudability and sphericity of pellets. Pellets containing simvastatin, MCC and polyethylene glycols (PEGs) or superdisintegrants were prepared by extrusion-spheronization and their micromeritics and mechanical properties, drug release and solid state of simvastatin were studied. All formulations produced pellets with reasonable size and sphericity. Generally, the inclusion of PEG and superdisintegrants decreased crushing strength and elastic modulus of pellets and increased the dissolution rate of simvastatin. A substantial increase in dissolution rate was observed when a combination of PEG and superdisintegrant was used due to the formation of more porous matrix, faster disintegration and remarkable reduction in drug crystallinity. It was interesting to note that the use of PEG and superdisintegrant had a synergistic effect on the dissolution enhancement of simvastatin in pellet formulation. The results of this study confirmed that a simple method of extrusion-spheronization can be employed to enhance the dissolution of simvastatin in multi particulates dosage form which can also be employed for other poorly water-soluble drugs.     

挤出-滚圆和流化床包衣法制备硫普罗宁肠溶微丸的研究

目的应用挤出 滚圆法及流化床包衣制备硫普罗宁肠溶微丸，并对其性质进行考察。方法采用国产挤出 滚圆造粒机制备硫普罗宁微丸，采用L9(34)正交设计实验优化工艺条件；用微型流化床包衣设备，将微丸包肠溶衣，考察微丸的粉体学性质及不同包衣增重微丸的体外释放实验。结果制得的硫普罗宁微丸圆整度好，大小均匀。15%包衣增重的微丸体外释放比较理想。结论应用国产挤出 滚圆造粒机制备硫普罗宁微丸，工艺简便，制得的微丸质量好，采用适当的包衣工艺，可制得硫普罗宁肠溶微丸。     

Formulation of ranitidine pellets by extrusion-spheronization with little or no microcrystalline cellulose

The present study was concerned with the feasibility of formulating ranitidine into pellets with a range of alternative excipients in place of microcrystalline cellulose (MCC). Eight ranitidine formulations employing two or more of the excipients lactose, barium sulfate, glyceryl monostearate, and MCC were processed by extrusion-spheronization, and characterized according to a series of physico-mechanical and dissolution criteria. Formulations containing lactose produced unsatisfactory pellets of wide size distribution and irregular shape, whereas formulations incorporating barium sulfate and glyceryl monostearate with or without MCC resulted in relatively spherical pellets of narrow size distribution and good mechanical properties. Ranitidine release was found to be rapid and virtually complete within 15 min, regardless of the pellet formulation. A direct relationship was observed between the concentration of MCC in the formulation and the properties of the pellets. In general, the higher the concentration of MCC, the rounder, stronger, and less friable the pellets. However, even pellets without MCC were also successfully prepared with a superior size distribution and shape over those with MCC. Overall, these results confirm that ranitidine can be formulated into pellet dosage forms with little or no MCC by the extrusion-spheronization process.