盐酸小檗碱微丸的制备方法研究

目的 制备盐酸小檗碱微丸,尝试通过制备新剂型提高药物的生物利用度.方法 采用挤出滚圆法制备盐酸小檗碱微丸,通过对挤出速率、润湿剂用量、滚圆转速等主要影响因素进行考察,优化微丸的制备工艺.结果 采用润湿剂1% CMC-Na 90 ml,挤出速率40 r/min,滚圆转速800 r/min,滚圆时间2.5 min制备微丸.制得的微丸球粒圆整度高,粒度均匀,表面光滑,结构紧密,具有一定的硬度,粒径范围0.47～0.78 mm,平均粒径(0.64±0.08)mm.结论 挤出滚圆法制备盐酸小檗碱微丸简便可行、重复性良好、质量可控.     

通脉复方微丸多元释药系统中川芎酚酸速释单元的制备工艺研究

目的:优选通脉复方微丸多元释药系统中川芎酚酸速释单元的处方和制备工艺。方法:采用单因素试验,以微丸圆整度为指标,考察润湿剂种类与用量、载药量、微粉硅胶用量;以累积溶出百分率为指标,考察崩解剂种类、崩解剂用量。以微丸的圆整度和收率的综合评分为指标,以挤出频率、滚圆频率、滚圆时间为考察因素,采用正交试验优选挤出滚圆法制备工艺。结果:川芎酚酸速释微丸处方总量以50g计算,主药20g,微粉硅胶2g,微晶纤维素26g,崩解剂为羧甲基淀粉钠2g,润湿剂为1%CaCl223mL。采用挤出滚圆法制备,其挤出频率20Hz,滚圆频率50Hz,滚圆时间6min。结论:优选工艺合理,制得的制剂稳定,为通脉复方微丸多元释药系统的制备奠定了基础。     

尼群地平缓释微丸的制备及体外释放影响因素考察

目的:对影响尼群地平缓释微丸中药物体外释放的制备工艺因素进行考察。方法:采用挤出滚圆法制备尼群地平缓释微丸,通过体外释放度试验,对影响缓释微丸中药物释放的润湿剂乙醇浓度及用量、挤出速度、滚圆转速及滚圆时间等因素进行考察,优化制备工艺条件。结果:润湿剂用量及乙醇浓度对药物体外释放影响显著,乙醇浓度应在35%以下,用量宜控制在44mL左右。挤出速度、滚圆转速及滚圆时间等对药物体外释放有一定的影响,分别以48r.min-1、1400r.min-1、5min为宜。结论:采用上述制备工艺,可制得释药速度符合要求的尼群地平缓释微丸。     

星点设计-效应面法优化黄肝微丸的制备工艺

目的:采用挤出滚圆法制备黄肝微丸,筛选最佳处方工艺.方法:用挤出滚圆造粒机制备黄肝微丸;以微丸的粉体学性质及得率为指标,在单因素试验基础上,通过星点设计-效应面法优化制备工艺.结果:制备黄肝微丸的最佳工艺为:挤出速度33 Hz,滚圆速度29 Hz,滚圆时间为12 min,所得微丸的圆整度好、大小均匀、收率高.验证实验证...     

通脉复方微丸多元释药系统中葛根黄酮速释单元的制备工艺研究

目的:制备葛根黄酮速释微丸,并对其制备工艺进行研究。方法:首先以熔融法将葛根黄酮组分制备成固体分散体,考察了载体及其比例对溶出度的影响。以葛根黄酮固体分散体作为主药制备微丸,考察了处方中润湿剂、载药量、辅料等因素对葛根黄酮微丸收率、圆整度、溶出度的影响;采用正交试验设计,筛选出葛根黄酮速释微丸的最佳制备工艺。结果:葛根黄酮速释微丸处方为主药20 g,乳糖5 g,微晶纤维素25 g,润湿剂为30%的乙醇。采用挤出滚圆法制备,最佳工艺条件为挤出频率25 Hz,滚圆频率30 Hz,滚圆时间6 min。结论:葛根黄酮速释微丸制备工艺科学合理,制剂稳定,为通脉复方微丸多元释药系统的制备奠定了基础。     

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...     

挤出滚圆和缓释包衣法制备止痛缓释微丸的研究

目的:优选中药止痛缓释微丸的制备工艺条件。方法:采用挤出滚圆工艺制备微丸,Surelease缓释包衣技术制备缓释微丸,采用析因设计对缓释包衣工艺参数进行了筛选。结果:确定了制剂处方及最佳工艺参数,润湿剂与物料的比例为0.55∶1,物料细度为100目,包衣增重4%,致孔剂用量为15%。结论:该工艺合理可行。     

挤出滚圆法制备盐酸索他洛尔骨架缓释微丸

目的制备盐酸索他洛尔骨架缓释微丸,研制盐酸索他洛尔新剂型。方法采用挤出滚圆法制备盐酸索他洛尔骨架缓释微丸,考察润湿剂用量、挤出速度及滚圆速度对释放度的影响。结果 120 mL 3%PVP K30水溶液作为润湿剂(物料固定为400 g),以挤出速度35 r.min-1,滚圆速度500 r.min-1(1 min)进行盐酸索他洛尔缓释微丸的制备,制剂稳定性良好。结论本方法制备盐酸索他洛尔骨架缓释微丸工艺可靠,质量可控。     

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。     

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。     

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。     

不同方法制备阿托伐他汀钙微丸的比较研究

目的:考察并比较不同方法与设备制备阿托伐他汀钙微丸的可行性。方法:分别选用挤出滚圆制丸法、离心造粒粉末层积载药、流化床混悬液载药3种方法制备阿托伐他汀钙微丸,以粒径分布和收率、载药率、含量均匀度、圆整度和表面光洁度、脆碎度、休止角等作为评价指标,比较并评价了所制备微丸的质量与工艺。结果:3种方法制得的微丸各项评价指标良好,各自表现出一定的优势。结论:挤出滚圆制丸法和流化床混悬液载药均能制备出质量较好的阿托伐他汀钙微丸,两者均适用于工业化生产。     

盐酸可乐定脉冲释药微丸的制备工艺研究

目的研究盐酸可乐定脉冲释药微丸的制备方法。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。结果各考察因素均对药物的释放影响显著。优选工艺结果为,含药丸芯采用微晶纤维素,溶胀层材料采用低取代羟丙纤维素,控释层采用乙基纤维素水分散体,溶胀层和控释层包衣增重分别为10％和15％。制备的微丸时滞时间为4．2h左右,时滞后1h内累积释药百分率达到90％。结论盐酸可乐定微丸在体外具有有脉冲释药特性。     

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.     

Powdered cellulose as excipient for extrusion-spheronization pellets of a cohesive hydrophobic drug.

This study compared a powdered cellulose (PC) and a microcrystalline cellulose (MCC) as sole excipients in the preparation of furosemide pellets by extrusion-spheronization. Pellets prepared with PC and 25 or 50% furosemide showed smaller mean size, a broader particle size distribution, similar sphericity, greater surface roughness and higher friability than equivalent pellets prepared with MCC. Furosemide release rate was markedly higher from PC pellets, which may be attributable to their higher micropore volume.     

Use of fine particle ethylcellulose as the diluent in the production of pellets by extrusion-spheronization

The effect of small ethylcellulose particle size on the manufacture and properties of pellets produced by extrusion-spheronization was investigated. A factorial design revealed the effects of microcrystalline cellulose (MCC), polyethylene oxide (PEO), water, and spheronization speed and time on pellet properties. Response surface modeling allowed optimization of the responses with expansion to a central composite design. Pellet yield, size, shape, friability and drug release profile were studied, along with surface and interior morphology. Pellets were spherical irrespective of the formulation and process variables and exhibited physical and mechanical characteristics appropriate for further processing. Yield in the 12/20 mesh cut was lower with FPEC than observed with coarse particle ethylcellulose (CPEC), but FPEC-containing pellets were more rugged and the PEO to obtain optimal pellets was lower for FPEC compared to CPEC. Immediate release products were obtained and ethylcellulose particle size was of no consequence to drug release. Observed responses for the optimized product agreed with predicted values, demonstrating the success of the optimization procedure. These results suggest that FPEC is a good diluent for extrusion-spheronization.     

Controlled drug release from Gelucire-based matrix pellets: experiment and theory

The aim of this work was to elucidate the underlying drug release mechanisms from lipidic matrix pellets, using theophylline and Gelucire 50/02 as model drug and carrier material, respectively. Pellets were prepared by two different techniques: melt-solidification and extrusion-spheronization. The effects of different formulations and processing parameters on the resulting drug release kinetics in 0.1N HCl and phosphate buffer pH 7.4 were studied and the obtained results analyzed using adequate mathematical models in order to get further insight into the underlying mass transport mechanisms. The type of preparation technique was found to strongly affect the underlying drug release mechanisms. Drug release from pellets prepared by the melt-solidification method was primarily controlled by pure diffusion, whereas drug release from pellets prepared by the extrusion-spheronization method was purely diffusion-controlled only at early time points. After approximately 2h, the pellets started to disintegrate, resulting in decreased diffusion pathway lengths and, thus, increased drug release rates. Furthermore, the curing conditions significantly affected the theophylline release kinetics, whereas varying the initial drug loading from 20 to 50% (w/w) resulted only in a slight increase in the relative drug release rate. Interestingly, the effects of the size of pellets prepared by the melt-solidification method on the resulting drug release kinetics could be quantitatively predicted using an analytical solution of Fick's second law of diffusion. These predictions could be verified by independent experiments.     

Waxy corn starch: a potent cofiller in pellets produced by extrusion-spheronization

The purpose of this study was to assess the usefulness of waxy corn (maize) starch as a cofiller and diluent in pellets produced by aqueous extrusion-spheronization. Waxy corn starch was combined with microcrystalline cellulose (MCC) in the range of 20-50% of the entire composition. Pellets containing ordinary corn starch or lactose with MCC were used as reference. The shape of pellets was characterized using an optical microscopic image analysis system. The surface and cross-sectional structure were investigated by means of scanning electron microscopy (SEM). The replacement of ordinary corn starch by waxy corn starch made it possible to increase the amount of starch from 20 to 40%. The pellets containing 50% waxy corn starch were of poorer quality but superior to those containing 30% corn starch. The surface structure became slightly more irregular with respect to the amount of either starch, and a cavity was formed inside the pellet during the spheronization. The origin of starch did not affect the surface structure of the pellets. Waxy corn starch is a potential cofiller: the amount of MCC can be reduced in pellets produced by extrusion-spheronization by using waxy corn starch as a cofiller. This enables the reduction of the manufacturing cost of pellets with low drug load.     

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。     

降脂灵颗粒质量标准研究

目的建立降脂灵颗粒质量标准。方法采用TLC法对处方中枸杞子、黄精、山楂、决明子进行定性鉴别;并采用HPLC法测定山楂中熊果酸的含量。结果薄层色谱均检出枸杞子、黄精、山楂、决明子;熊果酸在0.000262～0.003144μg范围呈良好的线性关系,r=0.9996;平均加样回收率为100.6%,RSD=1.41%。结论定性定量方法简便、准确、重现性好。提高后质量标准能更有效地控制该药品内在质量。