缓控释微丸制备方法的研究进展

缓控释微丸制剂是一种多单元型给药系统,具有单一给药系统无法比拟的优点,成为目前缓控释制剂研究的热点。本文对缓控释微丸制剂的制备方法包括冻干制粒法,挤出滚圆法,离心造粒制丸法等方法的研究进展进行了综述,并对微丸制剂制备方法的未来前景进行展望。     

中药浸膏微丸制备研究

目的:制备圆整度好、含药量较高的中药浸膏微丸.方法:用挤出滚圆制粒法制备微丸,并考察微丸的部分物理性质.结果:微丸中浸膏含量达40%,成品收率达80%,微丸物理性能稳定.结论:用挤出滚圆法制备的中药浸膏微丸具有产率高、物理性能优良的特点,挤出滚圆法在中药制粒领域具有巨大的应用潜力.     

挤出滚圆-流化床包衣法制备决明子微丸的研究

目的考察并优化挤出滚圆-流化床包衣法制备决明子醇提物微丸的工艺条件。方法采用L9（34）正交设计实验优化制剂工艺条件制备决明子醇提物微丸,考察微丸的粉体学性质,流化制粒包衣机将微丸包衣,并测定体外溶出度。结果以MCC为主要辅料,载药量40%,挤出频率30 Hz,滚圆频率50 Hz,滚圆时间4 min,经流化床包衣制得的决明子醇提物微丸,圆整度、流动性、体外释放度均较理想。结论应用挤出滚圆-流化床包衣法制备决明子醇提物微丸,其工艺简便,成品质量好。     

探究挤出滚圆法制备中药微丸的效果

目的：研究挤出滚圆法在制备中药微丸中的应用效果。方法查阅相关文献,结合当前该领域研究的成果,从处方来源、制备工艺等方面分析挤出滚圆法在制备中药微丸中的应用效果及前景。结果挤出滚圆法制备中药微丸工艺简单、材料易得,已经得到了较为广泛的应用。结论挤出滚圆法制备中药微丸可行性高,具有很好的实用价值。     

挤出滚圆法制备阿莫西林微丸的处方工艺研究

目的 应用挤出滚圆法制备阿美西林微丸,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阿莫西林微丸;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阿莫西林微丸在30min内体外溶出均达80%以上,且圆整度好,收率高.结论 挤出滚圆法制备阿莫...     

挤出滚圆法在中药微丸中的应用

目的促进挤出滚圆法在制备中药微丸中的推广。方法查阅相关文献,从处方来源、制备工艺、评价指标等方面,对挤出滚圆法制备中药微丸的现状和前景进行分析。结果挤出滚圆法辅料易得,工艺简单,在中药微丸的研究中已得到普遍应用。结论挤出滚圆法是制备中药微丸最可行的方法之一,在中药微丸的研制和生产中具有实用价值。     

氧化苦参碱微丸的制备及其性质考察

目的:制备氧化苦参碱微丸并考察其性质。方法:用实验型低温挤出滚圆制粒机制备氧化苦参碱微丸;采用L9(34)正交设计优化工艺条件;考察不同含药量的微丸的粉体学性质及体外溶出度。结果:用挤出滚圆法制备的氧化苦参碱微丸圆整度好,大小均匀;最佳工艺为水∶微晶纤维素=0.90∶1,滚圆速度为35Hz,滚圆时间为5min,挤出速度为40Hz;体外溶出度在30min内达到75%以上。结论:挤出滚圆法制备氧化苦参碱微丸的工艺简便易行,制得的微丸质量好。     

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。     

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。     

乙肝解毒微丸制备工艺研究

目的应用挤出-滚圆法制备中药乙肝解毒微丸,研究微丸制备的最佳处方和工艺。方法采用挤出-滚圆法对润湿剂、药料、乙醇的用量进行筛选,最终筛选出最佳用量。结果用挤出-滚圆法制备的乙肝解毒微丸圆整度好,大小均匀,成品收率高。结论通过加入合适的润湿剂,可以采用挤出滚圆法制备乙肝解毒微丸,该工艺稳定、辅料用量少,挥发性有效成分破坏程度小。     

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。     

Immediate release pellets with lipid binders obtained by solvent-free cold extrusion

Lipid-based drug delivery systems have spread in their use in pharmaceutical drug development. This work focuses on the use of lipid binders as alternative non-toxic extrusion aid for pellet formulations. The preparation of immediate release pellets with solid lipid binders through a solvent-free cold extrusion/spheronisation process was investigated in this study. Various binary, ternary and quaternary mixtures of powdered lipids and the model drug sodium benzoate were investigated and compared to well-known wet extrusion binders like microcrystalline cellulose and κ-carrageenan. The cold lipid extrusion process offers multiple advantages as it is suitable for thermal sensitive as well as for hygroscopic drugs, furthermore no drying process to evaporate the solvent is needed and the process is feasible for different extruder types. Some of the developed pellets showed favourable properties like spherical shape, narrow size distribution, a high drug load of 80% sodium benzoate and a drug release of more than 90% within 40 min. The stability of drug release, which can be problematic when using lipid excipients, was sufficient for some mixtures, as storage under elevated temperatures changed the release profiles only slightly and no formulation released less than 80% within the first 60 min. A formulation with a mixture of hard fat, glycerol distearate and glycerol trimyristate showed the best results, as pellets with a low aspect ratio, narrow size distribution and complete drug release were obtained. Using appropriate mixtures of acylglycerides it becomes possible to produce pharmaceutical pellets with immediate release characteristics by cold extrusion and subsequent spheronisation. Thus, lipids are very promising alternatives to commonly used extrusion/spheronisation binders.     

Box-Behnken设计-效应面法优化番泻苷微丸的制备工艺

目的:考察挤出-滚圆的工艺参数对番泻苷微丸性质的影响,优化番泻苷微丸的制备工艺。方法:采用挤出-滚圆法制备微丸,以挤出速度、滚圆速度、滚圆时间为自变量,得丸率、圆整度、归一化总值为因变量,采用3因素3水平的Box-Behnken设计进行试验,借助Minitab 14拟合评价指标对自变量的效应面,分析工艺参数对微丸性质的影响,优化微丸制备工艺,并对优化工艺进行验证。结果:最优工艺参数:挤出速度为17 r·min-1,滚圆速度为740 r·min-1,滚圆时间为3 min。该工艺制备的微丸得丸率(84.71±2.38)%,水平面临界角(9.38±0.60)°,总分(0.90±0.04),实测值与预测值(0.86)无显著差异。结论:采用Box-Be-hnken设计-效应面法能够快速得到番泻苷微丸制备工艺的优化模型,实现了工艺的优化。     

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。     

Box-Behnken法优化渗透泵微丸丸芯的制备工艺

目的：优化渗透泵微丸丸芯的处方、制备工艺,为渗透泵载药微丸研究提供优质丸芯。方法：在单因素的基础上,以休止角、硬度为评价指标,采用Box-Behnken法优选渗透丸芯的最佳制备工艺。结果：由单因素试验及Box-Behnken试验可知,以乳糖-微晶纤维素-PVP（5∶1∶0.1,w/w）为丸芯组成,以挤出转速30 r·min^-1,挤出温度24℃,滚圆转速1 800 r·min^-1为最佳制备工艺,制得粒径为0.8 mm,休止角为28.42°,硬度为17.52 kg·cm^-2的丸芯。结论：本实验筛选出渗透泵丸芯的处方组成及制备工艺,可为以渗透压为动力的渗透泵丸芯的制备研究提供参考。     

Study of the influence of alkalizing components on matrix pellets prepared by extrusion/spheronization

The aim of this study was to investigate the effects of alkalizing components and the nature of the wetting liquid on the properties of matrix pellets prepared by extrusion and spheronization. Atenolol was used as an active pharmaceutical ingredient, ethylcellulose as a matrix former, microcrystalline cellulose as a filler and disodium phosphate anhydrous and trisodium phosphate dodecahydrate as alkalizing materials. Water and a water-ethanol mixture served as granulation liquids. Pellet formation was evaluated via mechanical, dissolution and morphological studies. In order to enhance the dissolution of Atenolol from the pellets, alkalizing components were used and the influence of these components on the pH was tested. Investigations of the breaking hardness, the morphology and the dissolution revealed that the pellets containing trisodium phosphate dodecahydrate and prepared with a higher amount of water as binding liquid displayed the best physico-chemical parameters and uniform dissolution. In in vitro experiments, the dissolution release complied with the texture of the pellets and the effect of pH. The pellets have suitable shape and very good hardness for the coating process and are appropriate for subsequent in vivo experiments.     

热熔法制备曲普瑞林长效生物可降解微粒处方工艺的研究

目的 研究热熔法制备曲普瑞林长效生物可降解微粒的处方工艺,并对其质量进行考察。方法 首先进行单因素实验,对骨架材料PLGA的种类、PLGA与曲普瑞林重量比值、热熔挤出温度和时间、粉碎温度等参数进行筛选。在此基础上,对热熔挤出时间、热熔挤出温度、挤出后粉碎冷却温度三个因素进行正交试验,优化处方工艺,将制得的样品进行湿、热、光照影响因素实验、加速实验和长期实验考察。结果 热熔法制备的曲普瑞林微粒外观形态良好,且经加速实验考察,有关物质含量符合要求,微粒释放情况良好。结论 热熔法制备出的曲普瑞林质量稳定,该研究为制备出安全有效、质量可控的微粒提供理论与实践依据,适合进一步开发。     

挤出滚圆造粒法制备氨咖黄敏胶囊的工艺研究

目的 研究微丸制备的最佳工艺和处方。方法 用新型挤出滚圆造粒机制备氨咖黄敏胶囊，以微丸的外观性状、堆密度、休止角和成丸率为参考因素优化工艺、筛选处方。结果 用优化的工艺和筛选的处方制得的微丸外观圆整、微丸大小分布均匀、成丸率高。结论 用挤出滚圆法制备氨咖黄敏胶囊，造粒容易，效率高，工艺简便，成本降低。     

Properties of drug-containing spherical pellets produced by a hot-melt extrusion and spheronization process

The objectives of this study were to investigate the particle size distribution, morphology and dissolution properties of spherical pellets produced by hot-melt extrusion and spheronization and to compare the properties of hot-melt extruded pellets with beads manufactured by a traditional wet-mass extrusion and spheronization method. Spherical pellets were produced by hot-melt extrusion without the use of water or other solvents. A powder blend of theophylline, Eudragit Preparation 4135 F, microcrystalline cellulose and polyethylene glycol 8000 was hot melt-extruded and the resulting composite rod was cut into cylindrical pellets. The pellets were then spheronized in a traditional spheronizer at an elevated temperature. The same powder blend was processed using conventional wet-mass techniques. Unlike wet-mass extruded pellets, pellets prepared from hot-melt extrusion displayed both a narrow particle size distribution and controlled drug release in dissolution media less than pH 7.4. Scanning electron microscopy, X-ray diffraction and porosity measurements were employed to explain the differences in drug release rates of theophylline from pellets produced by the two processing techniques. Theophylline release from the hot-melt extruded pellets was described using the Higuchi diffusion model, and drug release rates from wet-granulated and melt-extruded pellets did not change after post-processing thermal treatment.     

白术黄连微丸结肠靶向胶囊的制备及体外释放研究

目的 将中药"白术黄连方"制备成以胃溶微丸和肠溶微丸为基础的结肠靶向胶囊,优化其处方组成和制备工艺,考察其体外释放特性.方法 采用单因素实验和正交实验法优化微丸的处方组成和工艺参数.用挤出-滚圆技术制备素丸,流化床底喷方式进行包衣,考察隔离衣增重、肠溶衣中聚合物比例、增塑剂用量和包衣增重对肠溶微丸释放行为的影响,并对其...