顶喷式流化床包衣效果的影响因素研究

选择平均粒径为250μm的石英砂作为模型,分别用Eudragit NE30D水分散体与Eudragit RL乙醇溶液包衣,用正交设计考察流化床顶喷过程中各因素对包农效果的影响.结果表明,用Eudragit NE30D水分散体包衣时,包衣液流速和雾化压力对包衣效果影响较大,用Eudragit RL乙醇溶液包衣时则是增塑剂浓度的影响较大.     

流化床对过氧化氢包合物的防潮包衣研究

目的对过氧化氢的尿素包合物进行防潮包衣,并考察其防潮效果。方法利用共沉淀法制备过氧化氢尿素包合物,并用流化床顶喷对其颗粒进行防潮包衣,用正交设计考察包衣过程中各因素对包衣效果的影响。结果确定最佳条件为包衣液固含量10%,流速1.2 mL·min-1,雾化压力0.40bar,进风温度40℃,在此条件下所得产品包衣效率约为84%。结论流化床顶喷防潮包衣效率高,包衣后过氧化氢包合物稳定性提高。     

流化床包衣制备微囊技术的发展及应用

流化床包衣是基于物理机械原理使粉末性、结晶性药物形成微囊的主要方法。该方法实用性较强，适用于工业化规模生产。由于被包囊药物有较大的比表面积，制备过程中经常会发生粒了粘连和静电吸附的现象，解决该问题是流化床包衣技术的关键，需要对囊心物性质、包衣液处方、喷液方式以及各种工艺参数进行控制和优化。镜下衣膜形态、微囊粒径、药物溶出行为是评价微囊质量的三个主要指标。目前，该技术在掩盖药物苦味、减少胃肠道刺激、增加药物稳定性方面已经有成功应用。     

流化床颗粒包衣法制备替米沙坦氢氯噻嗪片

目的 采用流化床颗粒包衣法制备替米沙坦氢氯噻嗪片,并对其稳定性进行考察。方法 采用流化床一步造粒工艺制备替米沙坦颗粒,然后将替米沙坦颗粒进行不同包衣增重后与氢氯噻嗪以及合适的辅料混合,用普通旋转压片机进行压片制备替米沙坦氢氯噻片,并利用正交试验设计,优化替米沙坦氢氯噻嗪片处方;用HPLC进行含量和杂质检测,通过加速试验和长期试验考察片剂稳定性和溶出度。结果 该方法制备的替米沙坦氢氯噻嗪片质量稳定。羧甲基淀粉钠外加用量20.4 mg、氢氧化钠用量8.5 mg溶出指标最为理想,最终优化的处方与原研制剂溶出特征一致。结论 以流化床颗粒包衣法制备的替米沙坦氢氯噻嗪片质量稳定,工艺较双层片简单,具有可行性。     

一盘珠颗粒薄膜包衣前后的质量差异

［摘要］目的考察一盘珠颗粒薄膜包衣前后的溶化性和外观性状及吸湿性的差异。方法分别取已包衣和未包衣颗粒在水浴中保温并持续搅拌观察溶化情况和比较包衣前后颗粒的外观性状、口感及测定包衣前后颗粒在空气环境中暴露不同时间的含水量。结果颗粒经过薄膜包衣,其溶化性较好,颗粒粒度、外观圆整和均匀度、口感较优,吸湿性大大降低。结论一盘珠颗粒包衣后的质量优于包衣前的质量。     

压缩颗粒的防潮包衣技术

压缩颗粒的包衣防潮技术在中药制剂工艺方面的应用，有效地解决了颗粒粘结、防潮的工艺技术问题及制刺的稳定性，减少了制剂内包装质量的成本，具有操作简单、成本低廉及较好的可实施性。     

颗粒包衣工艺提高鱼腥草素钠的稳定性

目的:对鱼腥草素钠(SH)进行颗粒包衣,提高其稳定性。方法:采用羟丙甲基纤维素(HPMC)为包衣材料,用流化床项喷技术对SH颗粒进行包衣,以收率为指标,考察了包衣增重、增塑剂用量、包衣温度、黏合剂等因素对包衣收率的影响,筛选包衣处方及优化制备工艺参数,并通过稳定性考察包衣后鱼腥草素钠的稳定性。结果:优化后的包衣处方是包衣增重为15%,增塑剂用量为5%,包衣温度为60℃。包衣颗粒中SH含量是(86.6±0.4)%(g/g,n=9)。SH包衣颗粒在高温、高湿条件下放置10 d,稳定性很好。结论:SH原料颗粒经过HPMC包衣后能有效提高其稳定性。     

盐酸二甲双胍流化床制粒工艺的影响因素研究

摘 要 目的：研究流化床制粒工艺参数对盐酸二甲双胍颗粒物理性质的影响。方法: 以盐酸二甲双胍颗粒物理性质作为评价指标,采用单因素试验法分别考察了流化床制粒过程中的设备因素（喷枪高度、喷枪孔径）和工艺参数（黏合剂用量、进风温度、进风速度、进液速度、雾化压力）对其产生的影响。结果: 设备因素中喷枪高度、喷枪孔径对颗粒物理性质影响较小,工艺参数中黏合剂用量、进风温度、进风速度、进液速度、雾化压力对颗粒物理性质影响均较大。结论: 流化床制粒工艺中黏合剂用量、进风温度、进风速度、进液速度、雾化压力对盐酸二甲双胍颗粒会产生较大影响,可按照颗粒性质要求进行控制。     

影响薄膜包衣的工艺因素

目的探讨影响薄膜包衣的工艺因素。方法用糖衣锅进行实验性薄膜包衣。结果片芯表面光滑、平整,硬度足够,选用雾化性能好的喷枪、控制包衣液的流量、喷枪和送热风位置选择恰当、以及包衣温度适宜是提高包衣效果的几个工艺因素。结论此法适用于高效包衣机。     

布洛芬包衣缓释颗粒释药动力学及体内外相关性研究

在研制出布洛芬速释处方的基础上,用乙基纤维素为材料对颗粒进行包衣,考察其体外释药动力学,并观察了颗粒大小、包衣厚度、pH值和压力诸因素对释药速率的影响。结果表明,包衣量较少时,释药过程更符合Higuchi方程;包衣量较大时,更符合零级动力学。在相同包衣量条件下,释药速率随颗粒的增大而减慢;当颗粒大小相同时,则随着包衣量增大释药速率减慢;释药速率随pH值的降低而显著减慢;包衣颗粒压片后,释药速率增大。经7名健康志愿受试者实验表明,体内外相关性显著。     

Suppression of Agglomeration in Fluidized Bed Coating. III. Hofmeister Series in Suppression of Particle Agglomeration

Purpose. Fourteen kinds of salts consisting of various cations and anions in the Hofmeister series were used as additives for suppression of particle agglomeration in the fluidized bed coating. We attempted to clarify the relationship between the suppression effect of the salts and the Hofmeister series of their consistent ions. Methods. Fluidized bed coating was carried out with hydroxypropyl-methyl cellulose (HPMC) aqueous coating solution containing the salts and Celphere® as core particles. To elucidate the salting-out power of the salts for HPMC, the transmittance of the coating solutions at 600 nm was measured at various temperatures and the phase separation temperature (T_PS) was determined from the values at 50% transmittance. Results. A high suppression effect was observed when the salts including high order ions in the Hofmeister series were added to the coating solution. T_PS decreased in the presence of the salts except for sodium iodide and sodium thiocyanate and lowered with the higher order ion in the Hofmeister series. The particle agglomeration was suppressed with decrease in T_PS of the HPMC aqueous coating solution. Conclusions. It has been suggested that the suppression effect of a salt on the particle agglomeration depended on the salting-out power of the salt. We regard sodium citrate and potassium citrate as very useful pharmaceutical additives for the suppression of particle agglomeration in actual pharmaceutical coating.     

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。     

流化床制粒影响因素的探讨

讨论了流化床制粒的影响因素和生产中易出现的问题.     

超临界反溶剂流化床制备西罗莫司微米颗粒

目的 使用超临界反溶剂流化床(supercritical anti-solvent fluidized bed,SASFB)包覆技术制备西罗莫司微米颗粒,考察颗粒形貌和体外溶出度。方法 以乳糖为载体,选取温度、压力、药液浓度3个工艺参数,通过正交试验对西罗莫司微米颗粒工艺进行优化。结果 药液浓度对西罗莫司包覆率的影响最大,压力次之,温度最小,最佳的工艺条件为温度45℃,压力8 MPa,药液浓度1 mg·mL^-1。SASFB制备的西罗莫司亚微米颗粒均匀分散在载体表面,溶出度在20 min时,分别是超临界反溶剂样品和原料药的2.29和5.04倍,包覆率可达74.1%。结论 SASFB是一种新型的一步制备西罗莫司微米颗粒的药物制剂技术。     

The Prediction of Variability Occurring in Fluidized Bed Coating Equipment. II. The Role of Nonuniform Particle Coverage as Particles Pass Through the Spray Zonemr

The purpose of this work was to evaluate the relative importance of particle circulation and particle-to-particle mass coating distribution on the overall mass coating distribution obtained in a Wurster process. A series of batch coating experiments was carried out over a range of operating conditions, in order to evaluate the particle-to-particle variation in the mass distribution of coating material deposited during batch coating operations. Results showed that the major component of variance was due to the variation in the amount of coating received per particle per pass through the spray zone. The variation in the number of times a particle passed through the spray zone was considerably less important. Two models were developed to explain the results of the experimental program. The first model categorized particles moving through the spray zone as either receiving coating or not. Thus, the distribution of coating material per particle per pass is described by a Bernoulli probability distribution. Using this picture of the spray process, the number of particles receiving coating during any given pass through the spray zone was found to vary between 2 and 6%. A second model was developed to explain the major cause of variation. This model explains the variation in terms of the hindering or sheltering effect that particles close to the source of the spray have on particles farther away. Although the agreement of model predictions with experimental results is only fair, it is believed that this model captures the main cause of particle-to-particle variation occurring in batch coating operations and thus is the first model to explain this phenomenon.     

The Prediction of Variability Occurring in Fluidized Bed Coating Equipment. I. The Measurement of Particle Circulation Rates in a Bottom-Spray Fluidized Bed Coater

The purpose of this work was to investigate the effect that changes in design and process variables had on the movement of particles around a fluidized bed coating apparatus. To measure the mean and variance of the particle cycle time distribution (CTD), the number of passages taken by a magnetic tracer particle through the spray zone was measured by a detector coil wound around the partition. The reproducibility of the measurement technique was tested by taking repeated measurements of the tracer particle movement, using similar bed operating conditions, and the method was found to give reproducible results. A series of experiments was carried out by varying operating conditions such as the partition gap, fluidizing air rate, and partition diameter and length, and measuring the change in the rate at which the tracer particle circulated in the coating device. The results of the experiments showed that, over the range of parameters tested in this work, the partition gap had the strongest influence on the rate of particle circulation. Moreover, for the 6-in.-diameter Wurster process used in the current work, the mean circulation time for the 1.1-mm-diameter Nu-Pareil particles was found to vary over the range of 2.2–10.4 sec. In addition, the mean and standard deviation of the CTD could be linearly correlated over a wide range of operating conditions, with a correlation coefficient of 0.80. Finally, an estimate of the variability in mass coating uniformity was made based on the results from the cycle time distributions. It was concluded that the effect of variability in the CTD could account for only a small fraction of the variability in the observed mass coating distribution.     

采用显微图像测量薄膜包衣厚度

采用显微图像测量薄膜包衣厚度.以薄膜包衣厚度和均匀性为指标,考察包衣工艺参数.