含阿魏酸的川芎效应组分缓释微丸的 制备及性质考察

目的:以流化床包衣法制备含阿魏酸的川芎效应组分(ACC)的缓释微丸.方法:采用挤出-滚圆法制备ACC速释微丸,以阿魏酸的体外释放度为考察指标,优化ACC缓释微丸的包衣液处方,并评价该缓释微丸的粉体学性质和缓释效果.结果:ACC缓释微丸圆整度好,在12 h内体外缓慢释药,尤特奇(Eudragit RS 100)的用量是影响微丸释药的主要因素.结论:制备的ACC缓释微丸在体外达到较好的缓释效果.     

一种治疗哮喘复方中药颗粒剂不同制粒工艺的比较

 目的比较治哮喘复方中药颗粒剂的3种制剂工艺,评价不同制粒工艺优缺点。方法以外观、流动性、粒径分布、吸湿性和溶化时间为指标评价湿法制粒、流化床一步法制粒,高速剪切制粒3种制粒工艺制得颗粒的优劣。结果流化床一步制粒法制粒工艺简单,制得颗粒的外观、流动性、粒径分布和溶化性均优于湿法制粒和高速剪切制粒,仅吸湿性稍差。结论综合考虑各个指标,3种工艺制得的颗粒中以流化床一步法制得颗粒最好。     

The Development of a Microwave Fluid-Bed Processor. I. Construction and Qualification of a Prototype Laboratory Unit

The static bed- and planetary-type microwave dryers currently available to process pharmaceutical materials are not designed to use hot-air fluidization for the purpose of maximizing microwave energy inputs and particle drying. To take advantage of the benefits offered by fluidization, a 1-kg Uni-Gatt laboratory fluid bed processor was modified to support microwave-assisted fluid bed drying of several representative pharmaceutical granulations. The construction, design features, and validation of this new microwave fluid bed processor are presented.     

不同包衣条件下银杏缓释微丸体外释放考察

目的考察不同包衣条件下银杏缓释微丸的体外释放。方法采用单因素考察及正交设计法。结果以丙烯酸树脂EudragitRL30D和EudragitRS30D为包衣材料,质量比为4∶1,包衣增重10 % (w) ,增塑剂的用量为2 0 % (w ) ,无需熟化,可满足2 4h缓释的要求。结论包衣量、衣膜中两种丙烯酸树脂的配比和包衣温度是影响药物释放的关键因素     

流化床包衣法制备硝苯地平缓释微丸

 目的 根据液相层积原理,采用流化床包衣法制备了硝苯地平缓释微丸。 方法 采用离心造粒装置制备了硝苯地平速释微丸,将制得的微丸采用微型流化床以 Eudragit^? NE30D 包衣制得了 24 h 释药的硝苯地平缓释微丸。 结果 所得缓释微丸体外释放符合一级释放与 Higuchi 方程。 结论 液相层积法制得微丸体外释放符合缓控释制剂的要求。     

泮托拉唑钠肠溶缓释微丸的制备

 目的以丙烯酸树脂(Eudragit)为包衣材料,制备泮托拉唑钠(PAZ-Na)肠溶缓释微丸,并对其体外释药性能以及粉体学性质进行考察。方法采用溶液上药法(流化床底喷装置)制备PAZ-Na微丸,用Eudragit RS/RL作为缓释包衣材料,制备缓释微丸;用EudragitL 100-55作为肠溶包衣材料,利用微型流化床进行包衣,制备肠溶缓释微丸,并通过单因素实验优化处方及其工艺条件,建立HPLC测定微丸中PAZ-Na,且测定了包衣微丸体外释放度。结果制备的肠溶缓释微丸质量良好,在pH1.2盐酸溶液中2h的释放度<10%;在PBS(pH6.8)中,释放曲线符合一级动力学方程,具有明显的缓释特征。结论PAZ-Na肠溶缓释微丸具有良好的体外缓释效果,制备工艺简单,重现性良好。     

Mechanics of Pharmaceutical Pellets—Constitutive Properties,Deformation, and Breakage Behavior

To ensure robust manufacturing of unit-based oral solid dosage forms with minimal structural imperfections and high mechanical reliability across subsequent processing unit operations (e.g., withstanding mechanical stresses during coating, optional axial compression, handling, packaging, storage, and transport conditions), process design should include consideration of precise limits of accurate micro, macro, and bulk properties of the constituent pellets. This communication presents a comprehensive intricate database of micromechanical properties' and breakage probability distribution functions of pellets, illustrating the stiffening and strengthening effects of coatings and the softening and weakening effects of structural moisture. Further insights such as the (contact) history-dependent softening during decompression, strain hardening on repeated stressing, strength recovery by drying, and the fragmentation pattern by cracking are also presented. The contents herein are based on conveniently performable lab-scale diametrical compression measurements on model microcrystalline cellulose pellets—demonstrating feasibility of the approach and validity of the contribution.     

Enhanced dissolution,stability and physicochemical characterization of ATRA/2-hydroxypropyl-β-cyclodextrin inclusion complex pellets prepared by fluid-bed coating technique

The aim of this work was to prepare stable all-trans-retinoic acid (ATRA)/2-hydroxypropyl-β-cyclodextrin (HPCD) inclusion complex pellets with industrial feasible technology, the fluid-bed coating technique, using PVP K30 simultaneously as binder and reprecipitation retarder. The coating process was fluent with high coating efficiency. In vitro dissolution of the inclusion complex pellets in 5% w/v Cremopher EL solution was dramatically enhanced with no reprecipitation observed, and significantly improved stability against humidity (92.5% and 75% RH) and illumination (4500 lx ± 500 lx) was achieved by HPCD inclusion. Differential scanning calorimetry and powder X-ray diffractometry confirmed the absence of crystallinity of ATRA. Fourier transform-infrared spectrometry revealed interaction between ATRA and HPCD adding evidence on inclusion of ATRA moieties into HPCD cavities. Solid-state ¹³C NMR spectrometry indicated possible inclusion of ATRA through the polyene chain, which was the main reason for the enhanced photostability. It is concluded that the fluid-bed coating technique has the potential use in the industrial preparation of ATRA/HPCD inclusion complex pellets.     

Comparative study of the uniformity of coating thickness of pellets coated with a conventional Wurster chamber and a swirl generator-equipped Wurster chamber

This study evaluated the performance of two bottom-spray coaters and the effect of pellet-size variability on coating uniformity. A conventional Wurster chamber was used for the first group of trials, and a Wurster chamber with a novel swirl-flow generator design was used for the second. The results confirmed that when using a conventional Wurster coating chamber, pellets with a smaller diameter receive significantly less coating material compared to those with larger diameters. The swirl generator-equipped Wurster chamber achieved close to uniform coating thickness regardless of pellet size. The ratio (M_S) of the mass of dye deposited in the coating layer to pellet surface area indicates that coating was much more evenly distributed using the swirl-flow coater. Coating thickness was also analyzed using SEM micrographs and the results were in close agreement with the M_S factor values. Inter-particle coating mass variation was also lower in case of swirl-flow coater. The results of this study show that a swirl-flow coater is suitable for coating particles of variable size. They also showed an improvement in coating process yield when using the swirl-flow coater.     

溴吡斯的明缓释微丸的制备及处方优化

目的：制备溴吡斯的明缓释微丸,并对处方进行优化。方法：采用流化床包衣技术,分别以不同黏度的乙基纤维素为包衣材料制备缓释微丸,以体外释放度为指标,采用均匀设计优化处方。结果：当PEG为12.8%,邻苯二甲酸二乙酯（DEP）为22.7%,增重为21.6%时,微丸的累积释放度与参比释放曲线相比相似因子（f₂）为86.5,释放曲线符合一级动力学方程。结论：采用流化床包衣技术制备的缓释微丸累积释放度达到释放要求。