辛伐他汀微丸胶囊的制备

利用离心造粒机,通过粉末层积法,以微晶纤维素为稀释剂,羟丙甲纤维素(HPMC) E5水溶液为黏合剂制备辛伐他汀微丸,再将微丸灌装胶囊.考察了微晶纤维素用量、黏合剂浓度对辛伐他汀载药微丸的粉体学性质和收率的影响,以及原药粒径对溶出度的影响.所得优化处方与市售胶囊(理舒达)在4种介质中的溶出行为相似.     

快速搅拌制备肠必清微丸的工艺研究

目的：制备肠必清微丸。方法：采用正交试验设计,考察肠必清处方提取物配比微晶纤维素作赋形列比例、润湿剂乙醇浓度、粘合剂PVP浓度及快速搅拌制粒时间对微丸质量的影响。结果：优选出快速搅拌制备肠必清微丸工艺,提取物配比赋形剂比例为2：1,乙醇浓度为90％,PVP浓度为3％,搅拌时间为15min。结论：其工艺制备微丸符合设计要求,适合工业化生产。     

氯磷酸二钠缓释微丸工艺与处方的优化

目的 :优化氯磷酸二钠缓释微丸的工艺以及处方中辅料的配方。方法 :以20 mg氯膦酸二钠为一个微丸的剂量,优化滚制速度、时间和干燥温度、微晶纤维素和润滑剂的加入量及乙基纤维素和硬脂酸的比例。结果 :最佳微丸制备工艺为:高档速度下滚制6 min,干燥温度为60℃。微丸的最佳配方为:20 mg氯膦酸二钠,不加微晶纤维素,乙基纤维素和硬脂酸比例为1∶2,24μl的10%Eudragit L30D-55。结论 :该工艺和配方可以作为制备氯磷酸二钠缓释微丸的较佳方案。     

基于均匀设计三七总皂苷微丸的制备工艺研究

目的：建立三七总皂苷微丸的制备工艺。方法：采用均匀设计法,以收率和圆整度为指标,考察微晶纤维素的用量、黏合剂水的体积、滚圆时间对三七总皂苷微丸的影响。结果：最佳制备工艺为微晶纤维素用量51%,加1/3倍的水作黏合剂,滚圆时间4min。结论：优选的制备工艺简单易行,制备的微丸圆整度好,大小均匀。     

含油中药浸膏片赋形剂的筛选

目的筛选含油中药浸膏片赋形剂。方法以外观、硬度、崩解度、脆碎度等为指标评价赋形剂对片剂成型性的影响。结果稀释剂选用糖粉，吸收剂选用辅料X，粘合剂选用微晶纤维素，崩解剂选用低取代羟丙基纤维素片剂成型性好。结论以上赋形剂适合于该片剂。     

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。     

蓝莲微丸成型工艺研究

目的建立蓝莲微丸的成型工艺。方法采用单因素实验和正交实验法选择蓝莲微丸的成型工艺。结果取处方量50g(板蓝根抗病毒物质基础组分结构物和穿心莲内酯共占40%,α-乳糖占10%,微晶纤维素占50%),加30%乙醇适量,将物料混匀捏合制备成软材,挤出转速30Hz,滚圆转速50Hz,滚圆时间5min。结论该方法准确、稳定,可作为蓝莲微丸的成型工艺。     

中药微丸成型技术的研究进展

［摘要］查阅、综述及分析近年来中药微丸在辅料筛选、处方优化、制备工艺等方面的研究文献。结果显示,中药浸膏粉体的性质是影响微丸成型的主要因素,通过添加赋形剂和表面改性技术,优化工艺可制备良好的中药微丸。添加成丸促进剂及浸膏粉体改性技术在中药微丸的制备过程中至关重要。     

去甲斑蝥素骨架型缓释微丸的工艺优化

目的:优化去甲斑蝥素骨架型缓释微丸的制备工艺,并考察制剂体外释药特性.方法:采用挤出-滚圆技术制备去甲斑蝥素骨架型缓释微丸,以多因素综合评价指标,正交设计与多元回归分析相结合优化处方工艺.结果:以微晶纤维素(MCC)9.877%、乙基纤维素(EC)-硬脂酸(1:1.5)、黏合剂1%羟丙甲纤维素(HPMC)13 mL,80℃烘干制得的去甲斑蝥素骨架型缓释微丸具有较好的缓释效果.结论:采用挤出-滚圆技术,通过缓释材料制备的去甲宽蝥素骨架型缓释微丸,其体外释药缓慢、持续、平稳.     

挤出-滚圆法制备微丸的设备和辅料研究进展

随着机械设备的发展,微丸制备方法逐渐呈现出多样化趋势,而挤出-滚圆法是最为常用的一种制备微丸的方法。目前,微晶纤维素是挤出-滚圆法制备微丸的标准辅料,与此同时,正在不断研究和推出针对微晶纤维素微丸现存问题的其他替代性辅料,以期达到减少或完全替代微晶纤维素的目的。具有优良性质的通用型高载药量辅料是今后研究的方向。本文总结并阐述挤出-滚圆法所用的生产设备和辅料概况。     

复方山茱萸胶囊的成型工艺研究

目的:确定复方山茱萸胶囊的最佳成型工艺.方法:通过对不同辅料对流动性,吸湿性,成型性的考察筛选制备颗粒的辅料,优选最佳制粒成型工艺,并测定临界相对湿度.结果:最佳成型工艺为浸膏粉∶微晶纤维素∶磷酸氢钙=1:0.12:0.03,生产环境的相对湿度宜控制在62%以下.结论:本试验确定的成型工艺能为其实际大生产提供依据.     

苯磺酸左旋氨氯地平片的制备及体外溶出研究

目的：研制苯磺酸左旋氨氯地平片,并以原研药为对照,考察其体外溶出性能。方法 ：以溶出度为考察指标,优选苯磺酸左旋氨氯地平片干粉直接压片的处方工艺,在四种溶出介质下考察仿制药的溶出,以确定处方工艺的合理性。结果：处方组成除活性成分苯磺酸左旋氨氯地平外,优选微晶纤维素、甘露醇和磷酸氢钙为填充剂,交联聚维酮为崩解剂,硬脂酸镁为润滑剂,并采用粉末直接压片工艺。结论：优选的处方工艺可行,在四种溶出介质下,仿制药与原研药溶出基本一致。     

Comparative evaluation of powder and tableting properties of low and high degree of polymerization cellulose I and cellulose II excipients

Low and high degree of polymerization (DP) cellulose II powders have been prepared from Avicel PH-102 and Solka Floc 40NF (low and high DP cellulose I powders, respectively), respectively, by treatment with sodium hydroxide (5N) for 24h and their powder and tableting properties investigated. Cellulose II powders, compared to the respective cellulose I counterpart, exhibited lower crystallinity, true density, and specific surface area. They were denser and showed higher moisture uptake. The Heckel analyses revealed both low and high DP cellulose II powders to be less ductile than the low DP cellulose I powder and more ductile compared to the high DP cellulose I powder. The crushing strengths of low and high DP cellulose II powders were comparable to that of the high DP cellulose I powder but lower than the low DP cellulose I powder. When compressed to comparable crushing strengths, the low and high DP cellulose II compacts disintegrated faster in comparison to the corresponding cellulose I compacts. Low DP cellulose I and II powders, compared to the high DP cellulose I counterparts were more sensitive to magnesium stearate. Magnesium stearate decreased the disintegration times of low DP cellulose I compacts but had no effect on the low and high DP cellulose II and high DP cellulose I compacts. In conclusion, low and high DP cellulose II powders, despite their different powder properties, show similar tableting properties, leading to the formation of rapidly disintegrating compacts. The low and high DP cellulose I excipients, in contrast, differ in their powder properties as well as tableting characteristics.     

氯雷他定片的制备及质量控制

目的:制备氯雷他定片并建立其质量控制方法。方法:将氯雷他定与十二烷基硫酸钠、淀粉、微晶纤维素等辅料混合制备片剂。采用紫外分光光度法测定氯雷他定含量。结果:氯雷他定检测浓度线性范围为4~28μg/ml(r=0.9 999),平均回收率为99.9%,相对标准偏差为0.3%。结论:该制剂制备工艺简单,质量控制方法可行。     

离心造粒法制备盐酸坦索罗辛缓释微丸胶囊的工艺影响因素及体外释放度考察

目的:制备盐酸坦索罗辛缓释微丸。方法:采用离心造粒粉末层积法制备盐酸坦索罗辛微丸。通过考察主机转速、喷浆泵转速、供粉速度、喷枪雾化条件、抛光时间、包衣增重对微囊收率的影响,确定各因素较佳水平;制备微晶纤维素空白丸芯和盐酸坦索罗辛含药微丸,并在此基础上进行丙烯酸树脂水分散体包衣,对包衣微丸的释药特征进行探讨。结果:微丸成丸的最佳工艺参数为主机转速200r·min-1,喷浆泵转速20r·min-1,供粉速度50r·min-1,喷气压力0.5MPa,喷气流量10～15L·min-1,抛光时间5min,包衣增重11%。3批样品经放大试验,测得微晶纤维素空白丸芯、含药微丸、包衣微丸的收率分别是97.5%、95.4%、96.8%。缓释微丸胶囊体外释药行为较好地符合零级方程。结论:采用离心造粒法在优化的工艺条件下可制得符合要求的盐酸坦索罗辛缓释微丸。     

Evaluation of a novel cellulose powder as a filler-binder for direct compression of tablets

A novel form of cellulose powder was evaluated as a filler-binder in tablets. The particle, powder, flow and binding properties of this experimental cellulose material were compared with those of two commercial microcrystalline celluloses, Avicel^® PH 101 and Emcocel^®. The effect of various storage conditions on the physical stability of tablets compressed from celluloses was also evaluated. The particle size and shape of experimental cellulose powder differed markedly from those of microcrystalline celluloses. Experimental cellulose contained mainly large and roughly spherical agglomerates of particles, among which were few smaller regularly shaped particles. Because of spherical particle shape, the experimental cellulose powder flowed better than microcrystalline celluloses, which consisted of much more irregularly shaped particles. Experimental cellulose formed stronger tablets than microcrystalline celluloses. It also acted more effectively than microcrystalline celluloses as a binding material in tablets containing poorly compressible ascorbic acid and acetaminophenone. This may be due to the extensive surface area of the particles of experimental cellulose powder. The specific surface area of this material was over 50 times as great as that of microcrystalline celluloses. This indicates an extremely porous structure of cellulose agglomerates. Tablets containing experimental cellulose powder were able to resist a permanent loss in tablet strength at different storage conditions better than tablets containing microcrystalline celluloses. According to the results of this study an experimental agglomerated form of cellulose powder is a very advantageous material as a filler-binder for direct compression of tablets.     

卡马西平口腔速崩片的制备及质量评价

目的:制备卡马西平(CBZ)口腔速崩片并评价其质量。方法:选用CBZ为主药,微晶纤维素(MCC)、交联羧甲基纤维素钠(CCNa)为崩解剂,以直接粉末压片法制备片剂;以MCC、CCNa、乳糖用量为考察因素,崩解时间为考察指标设计正交试验筛选处方;采用紫外分光光度法测定制剂中主药的含量,同时以崩解时间、溶出度及稳定性等指标进行质量评价,并与普通片剂比较溶出度,与原料药比较稳定性。结果:优选处方为MCC75mg、CCNa9mg、乳糖30mg。所制制剂含量均匀度符合规定,崩解时间为(21±3)s,溶出迅速,2min内累积溶出率达81.46%;普通片剂90min累积溶出率为71.46%。与原料药比较,该制剂在高温下吸收峰略有变化。结论:该制剂制备方法简单,质量稳定可控,应于低温干燥环境下贮存。     

离心造粒法制备盐酸二甲双胍微丸

［摘要］目的利用离心造粒粉末层积法制备盐酸二甲双胍微丸。方法采用多功能微丸包衣造粒机制备微晶纤维素空白丸芯和盐酸二甲双胍微丸，通过产率、粒径和粒径分布、堆密度、表面形态和圆整度、脆碎度和释放度对盐酸二甲双胍微丸进行质量评价。结果以盐酸二甲双胍：乳糖：微晶纤维素为100：5：3的比例，进行制备微丸，获得了很好的效果。结论制得的盐酸二甲双胍微丸圆整度好，粒径均匀，硬度合格，流动性好，无骨架结构，释放完全。     

盐酸氨溴索口腔崩解片制备工艺研究

目的设计制备盐酸氨溴索口腔崩解片。方法选用进口崩解剂,采用正交试验设计处方,用直接压片法制备盐酸氨溴索口腔崩解片。结果最佳处方为：微晶纤维素（进口）与甘露醇（1：3）;6%交联聚乙烯吡咯烷酮（进口）;0.8%枸橼酸为泡腾崩解剂;2%阿司帕坦;2%粉末香精。结论制备的盐酸氨溴索口腔崩解片矫味效果良好,崩解迅速,口感好。     

Influence of cellulose powder structure on moisture-induced degradation of acetylsalicylic acid.

The stability of crystalline acetylsalicylic acid (ASA) powder in binary mixtures with cellulose powders was investigated to reveal information about the influence of the cellulose structural properties on the moisture-induced ASA degradation. Different cellulose powder samples were manufactured and characterized by X-ray diffraction and N2 BET gas adsorption. The degradation patterns in ASA/cellulose mixtures were monitored as a function of salicylic acid increase versus time under various relative humidity conditions at 50 degrees C. The crystallinity index of cellulose samples varied between approximately 49 and 95%. The results indicated that cellulose powder with the lowest crystallinity index exhibited lower degradation rates than the samples with the higher crystallinity index. It should be noted that higher ASA degradation rates were observed in the samples with comparably lower moisture contents. This effect was most pronounced in the 1:3 (w/w), ASA/cellulose mixtures, whereas in 3:1 (w/w), ASA/cellulose mixtures the effect was less obvious. The findings emphasise the importance of cellulose structural organisation when governing the moisture's partition between cellulose and ASA during the hydrolytic degradation.