一种流化床喷雾制粒技术在头孢克洛颗粒制备中的应用

目的:研究流化床制粒设备在头孢克洛颗粒制备中的应用.方法:采用正交试验法,选定进风温度、喷入粘合剂浓度、喷浆速度、进风量为考察因素,每个因素取3个水平,筛选头孢克洛颗粒流化床制粒的最佳工艺.结果:最佳工艺条件为粘合剂为10％PVPK30、进风温度70℃、喷入速度50mL· min-1,进风量为1400m3· h-1.结论:本方法生产工艺简单,自动化程度更高,是药物制剂现代化生产的一条良好途径.     

多指标综合评分法研究中药半浸膏片的制粒工艺

目的:以冠心平为模型药物,优选中药半浸膏片的制粒最佳工艺。方法:通过单因素考察,确定制粒的最佳粘合剂;采用L₉（3⁴）正交试验法,以粘合剂浓度、用量及软材搅拌时间作为考察因素,通过颗粒粉体学和片芯的几个质量指标的综合评分,优选出冠心平片的最佳（湿法）制粒工艺。结果:最佳工艺条件为:采用2%浓度的羟丙甲基纤维素浆溶液,用量为浸膏粉量的26%,软材混合时间为8 min。结论:确定的制粒工序生产工艺参数适用于冠心平片的制粒。     

粘合剂对药用炭吸着力的影响

研究不同粘合剂对药用炭颗粒吸着力的影响。方法 以淀粉、糊精、明胶和羧甲基纤维素钠(CMC-Na)为粘合剂,制成药用炭颗粒,根据中国药典2000版所载方法测定其吸着力。结果 不同含量的淀粉、糊精、明胶均会降低药用炭颗粒的吸着力,而8％～10％CMC-Na能增强药用炭颗粒的吸着力。结论 粘合剂可显著影响药用炭颗粒的吸着力,其中以CMC-Na比较理想。     

粘合剂对药用炭吸着力的影响

目的 研究不同粘合剂对药用炭颗粒吸着力的影响。方法 以淀粉、糊精、明胶和羧甲基纤维素钠（ＣＭＣ－Ｎａ）为粘合剂,制成药用炭颗粒,根据中国药典２０００版所载方法测定其吸着力。结果 不同含量的淀粉、糊精、明胶均会降低药用炭颗粒的吸着力,而８％～１０％ＣＭＣ－Ｎａ能增强药用炭颗粒的吸着力。结论 粘合剂可显著影响药用炭颗粒的吸着力,其中以ＣＭＣ－Ｎａ比较理想。     

肝清颗粒的制剂工艺研究

目的优选肝清颗粒的制剂工艺。方法以制粒情况、成型率、溶化性、休止角和吸湿率为评价指标,采用正交试验法优选制剂工艺条件。结果肝清颗粒最佳制粒工艺条件为：浸膏粉和混合辅料（糖粉：糊精=2.5：1）按5.7：6.3比例混匀,以65%糖浆为粘合剂,粘合剂用量为混粉总量的40%。制备的成品颗粒评价指标均符合要求。结论优选的肝清颗粒制剂工艺合理可行,成本低,为进一步制剂研究和临床应用提供了试验依据。     

金牡感冒片工艺研究

目的优选金牡感冒片的最佳制粒工艺。方法按L9（3^4）进行考察金牡感冒片的最佳成型工艺,即膏粉比、辅料（淀粉：糊精）、粘合剂淀粉浆浓度3个因素,以颗粒的外观、流动性,片芯外观、硬度为指标,筛选出最佳的成型工艺参数。结果以膏粉比1.1：1、辅料（淀粉：糊精=2：1）、粘合剂（9％淀粉浆）的制粒工艺为颗粒的最佳成型条件。结论优选的金牡感冒片制粒工艺稳定可靠、操作简便,为中试及放大生产提供科学的理论依据。     

小儿化痰止咳颗粒喷雾制粒工艺研究

目的探讨小儿化痰颗粒喷雾制粒工艺的最佳生产条件。方法采用正交设计法，以黏舍剂浓度、黏合剂用量、喷雾速度、制粒温度为可变因素，以合格颗粒收得率为指标，对影响因素进行研究。结果最佳生产条件为黏合剂明胶浓度为8．0％，用量为1．5％，喷雾速度为0.4kg／min，制粒温度为65℃。结论该生产工艺可操作性强，产品收得率高，质量稳定，适用于工业化生产。     

高速搅拌制粒工艺与片剂抗张强度的关系

考察了高速搅拌湿法制粒工艺中制粒及压片两步的处方、工艺因素与颗粒成片后片剂张强度的关系以及颗粒性质与片剂抗张强度的关系。结果表明,制粒一步中粘合剂用量及搅浆速度对抗张强度起正作用,原料粒度则起负作用,粘合剂加入速度对不同压力制的片剂抗张强度影响不同。而颗粒松密度及颗粒强度与片剂抗张强度亦有相关关系。压片时压片力及颗粒含水量对片剂的抗张强度起正     

补肾健脑颗粒制备工艺研究

目的 确定补肾健脑颗粒的制备工艺。方法 以颗粒得率、吸湿百分率为指标筛选颗粒的辅料，并采用L^9（3^4）正交试验法，以颗粒得率、溶解率为考核指标进行综合评分，考察快速搅拌制粒工艺中的几个影响因素。结果 最佳制剂工艺是乳糖用量为0．2％，制粒机转速比为快／慢，制粒时间为210s。结论 试验结果可为补肾健脑颗粒制备工艺的确定提供依据。     

益肾续骨颗粒的成型工艺研究

目的:确定益肾续骨颗粒剂的成型工艺条件.方法:考察不同辅料(乳糖、可溶性淀粉、糊精)对浸膏粉吸湿性的影响:用正交试验法优选制粒工艺条件.结果:3种辅料均可明显降低浸膏粉的吸湿性.最佳制粒工艺条件为:浸膏粉与糊精的配比为8:2,用80%乙醇为润湿剂,醇的用量为浸膏粉的4%.结论:本实验为益肾续骨颗粒确定了制粒工艺条件.     

药用炭片吸着力检查方法研究

目的建立测定药用炭片吸着力的分光光度法。方法利用药用炭对生物染色剂亚甲蓝的吸附特性,用分光光度法测定药用炭对亚甲蓝吸附的剩余量。结果亚甲蓝质量浓度与吸光度的线性范围为1.0～10.0μg/mL（r=0.99993,n=6）,回收率为98.5%,RSD为0.97%。结论分光光度法测定结果准确,可用于测定药用炭片吸着力。     

The granulation of binary mixtures: the effects of the composition of the granulating solution and the initial particle size of one component on granule properties.

The effect of total solvent volume and the presence of dissolved material (other than binder) in the granulating solution, on the properties of granules prepared from lactose: boric acid mixtures has been studied. The total volume of binder solution available to powder mixtures during massing determines the ultimate average size of granules produced. Part-dissolution of powders being granulated contributes significantly to the average granule size by increasing the total solution volume and reducing the amount of powder to be wetted. Although the amount of PVP (binder) dissolved in the granulating solution contributed very little to granule size at the concentration examined, the combined effect of total volume of solution and amount of PVP present in the granulating solution determines granule strength and porosity. The effect of the initial particle size of lactose in a binary mixture with boric acid differs from its effect reported for single component systems.     

基于流化床顶喷技术的巴戟天寡糖胶囊成型工艺研究

目的采用流化床顶喷制粒技术优化和建立中药巴戟天寡糖颗粒一次成型的工艺路线和工艺参数。方法采用单因素考察法,设定流化床顶喷包衣锅的主要工艺参数范围,将巴戟天水提取物喷至一定量的微晶纤维素粉末上,制备巴戟天寡糖颗粒,并分别测定其休止角、抹角、松密度、轻敲密度、压缩度和均一度等,计算流动性指数和平均粒径。结果当进风温度设定为40～45℃;进风压力设定为0．35～0．45bar;雾化压力设定为1．5～2．0bar;喷液速率设定为15～25r·min^-1范围时,制备的巴戟天寡糖颗粒可顺利灌装装量均一的胶囊。结论该工艺使制剂一次成型,具有生产周期短、生产效率高、辅料用量小和产品成本低等优点,在中药制剂的成型工艺中值得推广应用。     

头孢呋辛酯片干法制备工艺条件研究

目的:研究头孢呋辛酯片的干法制备工艺条件,确定制备方法。方法:以颗粒粒度、流动性及成品率为考察指标,筛选干法制粒的工艺条件,并进行质量考察和稳定性研究。结果:确定干法制粒三要素分别为液压压力2·5～3MPa、挤压速度15～20r·min-1、加料速度200～300g·min-1,控制压饼厚度1～2mm。循环干法制粒的合格颗粒(16～30目)可达90%以上,休止角约30°,流动顺畅,压片成品率约94%,经加速试验和长期稳定性试验考察,各项指标符合2005年版《中国药典》相关规定。结论:经筛选后的工艺参数及微调后的处方能适应干法制粒的要求,产品稳定性优于湿法样品,工艺重现性良好,生产周期缩短。     

对乙酰氨基酚口腔崩解片的研制

目的 以对乙酰氨基酚（扑热息痛）为模型药物制备新型口服速释剂型口腔崩解片。方法 以崩解时间为指标，采用正交试验筛选片剂的处方组成，并优化制备工艺。结果 以MCC／L-HPC 50：15作为崩解剂，部分制粒压片工艺制得的扑热息痛口腔崩解片，体外平均崩解时间为35s，置于口腔40s内可崩解，无砂砾感，片剂体外溶出度1min可达95％。结论 扑热息痛口腔崩解片于口腔内可迅速崩解，制备工艺简单可行，有效地改善了药物粉末的流动性，适宜于大生产。     

Process optimization for the enhanced stability of diclofenac potassium granules and capsules

This study aimed to investigate the effects of different process parameters on the physical properties, in vitro dissolution rate, and short and long-term stability of diclofenac potassium (DFP) granules and capsules. DFP granules exhibited low total amounts of impurities when prepared through the wet granulation method using a granulating solvent with a low water/ethanol ratio. The impurities of the wet DFP mass dried at 70 °C were higher than those dried at 50 °C or 60 °C. DFP granules were stable under strong light exposure during preparation. DFP granules prepared using a granulating solvent with a 1:4 water/ethanol ratio had a relatively smaller particle size and higher angle of repose than those prepared using granulating solvents with other water/ethanol ratios. The dissolution rate of DFP capsules prepared using four different water/ethanol ratios was less than 2% after 10 min of dissolution and increased to 95% within 30 min of dissolution. The total amount of drug impurities of DFP capsules prepared using a granulating solvent with 1:4 water/ethanol ratio was considerably lower than those of DFP capsules prepared using a granulating solvent with a 1:0 water/ethanol solvent ratio. Regardless of the water/ethanol ratio, the capsules showed poor stability when exposed to high temperature (60 °C) and strong light (4500±500 Lux) for 10 days, but were relatively stable at high humidity (92.5% RH). The results of the long-term stability (25±2 °C and 60%±10% relative humidity) study showed that DFP granules were more stable than DFP capsules, and were stable for 12 months. The type of encapsulating material did not affect the 2-month stability of DFP. DFP granules are sensitive to granulating solvent and drying temperature and DFP capsules should be stored away from high temperature and strong light.     

Improvement of the dissolution rate of artemisinin by means of supercritical fluid technology and solid dispersions

The purpose of this study was to enhance the dissolution rate of artemisinin in order to improve the intestinal absorption characteristics. The effect of: (1) micronisation and (2) formation of solid dispersions with PVPK25 was assessed in an in vitro dissolution system [dissolution medium: water (90%), ethanol (10%) and sodium lauryl sulphate (0.1%)]. Coulter counter analysis was used to measure particle size. X-ray diffraction and DSC were used to analyse the physical state of the powders. Micronisation by means of a jet mill and supercritical fluid technology resulted in a significant decrease in particle size as compared to untreated artemisinin. All powders appeared to be crystalline. The dissolution rate of the micronised forms improved in comparison to the untreated form, but showed no difference in comparison to mechanically ground artemisinin. Solid dispersions of artemisinin with PVPK25 as a carrier were prepared by the solvent method. Both X-ray diffraction and DSC showed that the amorphous state was reached when the amount of PVPK25 was increased to 67%. The dissolution rate of solid dispersions with at least 67% of PVPK25 was significantly improved in comparison to untreated and mechanically ground artemisinin. Modulation of the dissolution rate of artemisinin was obtained by both particle size reduction and formation of solid dispersions. The effect of particle size reduction on the dissolution rate was limited. Solid dispersions could be prepared by using a relatively small amount of PVPK25. The formation of solid dispersions with PVPK25 as a carrier appears to be a promising method to improve the intestinal absorption characteristics of artemisinin.     

冠心Ⅴ号颗粒制备工艺优选

目的：优选冠心Ⅴ号颗粒的制备工艺。方法采用正交试验法,对冠心Ⅴ号颗粒的醇水双提工艺条件进行优化,并进行制粒工艺研究。结果该颗粒的最佳醇提工艺为加6倍量75％乙醇,回流2 h,最佳水提工艺为加6倍量水,煎煮1．5 h,煎煮2次。稠膏与糊精按1∶3混合,润湿剂为90％乙醇。结论优选的冠心Ⅴ号颗粒制备工艺稳定可行。     

药用炭检验结果分析

目的对药品生产企业使用的药用炭进行质量考察。方法采用《中国药典》2010年版二部药用炭质量标准检验。结果市场上使用的药用炭质量堪忧。结论药用炭质量标准有待修订和完善,建议制定和规范我国药用辅料活性炭质量标准。