离心造粒法制备益胃微丸的研究

目的制备益胃微丸。方法采用离心造粒法制备益胃微丸,考察处方和工艺因素对微丸收率的影响,并采用正交试验设计法和筛分法对影响微丸收率的主要因素进行筛选优化。结果在微丸起模过程中,主机转速、黏合剂的加入速度和加入量及喷枪喷雾条件对起模微丸的收率具有较为显著的影响。经正交设计试验和筛分法优化得微丸起模的最佳处方和工艺参数为:提取物与淀粉比例为1:2,黏合剂为3%聚乙稀吡咯烷酮无水乙醇(PVP),主机转速为200r.min-1,鼓风流量为10×20L.min-1,喷气流量为15L.min-1,喷气压力为0.5mPa,喷浆泵转速为20r.min-1。结论在优化条件下采用离心造粒法可制得表面较为光滑、圆整度较高的益胃微丸,1000～400μm微丸的收率达87.1%。     

离心造粒法制备中药浸膏微丸的影响因素

采用离心造粒法制备了万氏牛黄清心微丸,并以粒径分布、休止角、松密度为指标考察了影响微丸成型过程的处方因素和工艺因素.采用优化处方工艺制得了外观和体外释药行为良好的产品.     

离心造粒法制备中药益脂微丸

目的研究中药益脂微丸制备工艺参数,解决微丸制备中难题。方法采用离心造粒法制备中药益脂微丸,以收率和微丸中有效成分含量为指标,优化了影响成丸过程的处方因素和工艺因素。结果丹皮酚和中药浸膏等原料分别经粉碎过筛160目以上,再加30%微晶纤维素混匀,以水作为润湿剂,主机转速200r.min-1,喷浆泵转速5r.min-1制备微丸。结论所得产品外形美观,稳定性好,有效成分含量均匀并且合格。     

离心造粒法制备贯叶连翘提取物微丸

目的：采用离心造粒法制备贯叶连翘提取物微丸。方法：以目标微丸收率、休止角、脆碎度等为指标考察影响微丸成型过程的处方因素和工艺因素。结果：成丸的优化处方和主要工艺参数为：贯叶连翘提取物与微晶纤维素（MCC）比例为1：1,黏合剂为75％的乙醇;主机旋转变频为35Hz（约为250r·min^-1）,风机变频为12Hz,喷枪压力为0．05Mpa,喷浆蠕动泵转速为10—12r·min^-1（约为70～85ml·min^-1）,供粉速度调至最大（约16g·min^-1）。结论：在优化奈件下采用离心造粒法可制得表面光滑、圆整度较高的贯叶连翘提取物微丸,粒径在18～24目范围内的微丸收率达80％以上;以槲皮素为指标成分,30min累积溶出度大于90％．     

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。     

卡托普利缓释胶囊的制备

目的运用离心造粒法制备卡托普利缓释胶囊。方法采用离心造粒法,以微晶纤维素为辅料,3%羟丙甲基纤维素为粘合剂制备丸芯,以粒径分布、圆整度、脆碎度为指标,对丸芯进行质量评价。以Eudragit NE30D为包衣材料,以释放度为指标,对包衣液处方及包衣条件进行优化,制备卡托普利缓释微丸。优化后工艺条件为：包衣温度20~25℃,硫化条件50℃,24h。结论与结论包衣增重分别为2%和7%的微丸,按2∶5的比例配比,所得微丸体外释放性质良好。将包衣微丸按比例装入胶囊,制得缓释胶囊。     

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。     

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。     

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.验证实验证明,最优处方工艺的重现性良好.结论:采用星点设计-效应面法实现黄肝微丸制备工艺优化,该工艺简便易行,微丸载药量高、成型性好.     

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。     

复方格列吡嗪缓释胶囊中盐酸二甲双胍缓释微丸薄膜衣处方的筛选

目的:筛选盐酸二甲双胍缓释微丸薄膜衣处方。方法:以体外释放度为主要考察指标,采用单因素筛选法,初步确定薄膜衣的处方,再利用正交试验对其进行优化;测定所制备的缓释胶囊的体外释放度,并与微丸进行比较。结果:优化处方为薄膜材料Eudragit NE30D∶Eudragit L30D55=10∶1,加入聚合物量40%的滑石粉及0.25%的十二烷基硫酸钠。缓释胶囊缓释性优于微丸。结论:所制备的缓释胶囊可持续24h释放药物,达到缓释要求。     

Evaluation and simultaneous optimization of some pellets characteristics using a 3(3) factorial design and the desirability function

A 3(3) full factorial design study has been employed in order to investigate the effect of three variables on size, size distribution and three shape parameters, namely roundness, elongation and e(R), of pellets prepared in a fluid bed rotor granulator with the wet granulation technique. The first variable was a formulation variable, the % w/w content of microcrystalline cellulose (MCC) and the other two variables were processing variables, the temperature of inlet air and the spray rate of the granulation liquid. The analysis of variance showed that the three variables had a significant effect (P<0.05) on pellet size and the shape factors, while only the spray rate influenced the particle size distribution. Significant interactions between the factors, for the size and the shape, were also found. The multiple regression analysis of the results led to equations that adequately describe the influence of the independent variables on the selected responses. Furthermore, the desirability function was employed in order to optimize the process under study. It was found that the optimum values of the responses could be obtained at the low levels of the % w/w content of MCC and temperature of inlet air and at the high level of the spray rate.     

离心造粒包衣法制备洛索洛芬钠缓释微丸及体外释放度考察

目的:制备洛索洛芬钠缓释微丸。方法:采用离心造粒包衣法制备洛索洛芬钠微丸。首先制备微晶纤维素空白母核和洛索洛芬钠含药素丸,并在此基础上进行丙烯酸树脂水分散体(Eudragit NE30D、Eudragit L30D-55)包衣,并对包衣微丸的释药特征进行探讨。结果:微晶纤维素(MCC)空白母核32～40目的收率约78.6%,含药素丸18～24目收率约88.2%,使用Eudragit NE30D和Eudragit L30D-55比例是20:1的包衣液,包衣增重10%。包衣干燥后,即得洛索洛芬钠缓释微丸,洛索洛芬钠缓释胶囊体外释药行为较好地符合Higuchi方程。结论:在优化的工艺条件下可制得表面光滑、圆整度高的洛索洛芬钠缓释微丸。     

Optimatization of pellet preparation is CF-granulator with factorial design

Lithium carbonate-containing pellets were made in a laboratory-scale centrifugal granulator in order to investigate the effects of the process parameters (rotor rotation speed, slit airflow rate and spray air rate) on the pellet shape and size distribution. The size distribution and the shape parameters (roundness, roughness, rectangularity and sphericity) of the pellets were measured, and an optimization parameter was then calculated from these shape parameters. The experiment was carried out and evaluated according to a 2(3) full factorial design. All three variables were found to exert a significant effect on the pellet shape. With use of the signs and magnitudes of the coefficients of the variables in the fitted linear model, the direction of the gradient was determined; two control measurements were made. These proved the accuracy of the applied model and the direction of the gradient. Overall, a high rotor rotation speed and low slit airflow rate and spray air rate furnished the best value of the optimization parameter.     

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。     

Preparation and in vitro/in vivo evaluation of sustained-release metformin hydrochloride pellets.

In this study, metformin hydrochloride (MH) sustained-release pellets were successfully prepared by centrifugal granulation. Seed cores preparation, drug layering, talc modification and coating of polymeric suspensions were carried out in a centrifugal granulator. Talc modification was performed before coating in order to overcome the high water solubility of metformin. The influence of surface modification by talc, the effects of Eudragit types and ratios, as well as the correlation between in vitro release and in vivo absorption were investigated in detail. Experimental results indicated that talc modification made a decisive contribution to controlling the drug release by avoiding drug dumping. Three dissolution media: 0.1 M HCl, distilled water and pH 6.8 phosphate buffer were employed to determine the in vitro release behaviors of the above metformin hydrochloride pellets. The relative bioavailability of the sustained-release pellets was studied in 12 healthy volunteers after oral administration in a fast state using a commercially available immediate release tablet (Glucophage) as a reference. Following coating with a blend of Eudragit L30D-55 and Eudragit NE30D (1:20), at 7% or 10% coating level, respectively (referred to as F-2, F-3), the pellets acquired perfect sustained-release properties and good relative bioavailability. The Cmax, Tmax and relative bioavailability for F-2 and F-3 coated pellets were 1.21 microg/ml, 6 h, 97.6% and 1.65 microg/ml, 8 h, 165%, respectively. Combined use of two Eudragit polymers with different features as coating materials produced the desired results. Restricted delivery of metformin hydrochloride to the small intestine from differently coated pellets resulted in increased relative bioavailability and a sustained release effect. The adoption of several different pH dissolution media established a better relationship between the in vitro release and in vivo absorption of the sustained-release pellets.