Yüksel Nilüfer, Karataş Ayşegül, Baykara Tamer
Department of Pharmaceutical Technology, Faculty of Pharmacy, University of Ankara, Tandoğan, Ankara, Turkey.
Drug Dev Ind Pharm. 2003 Apr;29(4):387-95. doi: 10.1081/ddc-120018374.
Granules were prepared using three different binders, pregelatinized starch (PGS), gelatin (GEL), and polyvinylpyrrolidone (K30) by a fluidized bed method. As a quantitative measurement of mechanical strength or abrasion resistance, granules were subjected to a friability test for certain periods of time, and friability indexes (FI) as a function of time were calculated. The data obtained were analyzed by applying standard mathematical models. According to the derived parameters of the logistic and Weibull models, which fit best to the data, mechanical strength of granules made with K30 was observed to be lower than that of the granules of PGS and GEL which have similar values of model parameters. Flow properties, consolidation, and compressibility behaviors of unfriabled (UFR) and friabled (FR) granules, which were selected based upon their Weibull time parameter, were investigated as comparative. The flow rate of granules decreased due to diminishing particle size depending on binder type and friability, but the values of angle of repose were within the acceptable limits. Regarding consolidation behavior, the change of relative density vs. the number of taps, i.e., packing rate for FR granules of GEL was slower than that of its UFR form, whereas FR granules of PGS and K30 showed faster change in relative density compared to their UFR forms. According to the parameters obtained from the Heckel equation, PGS and K30 were found to produce softer, more plastic and readily deformable granules than GEL, and the compressibility of their FR forms was not influenced negatively.
采用流化床法,使用三种不同的粘合剂,即预胶化淀粉(PGS)、明胶(GEL)和聚乙烯吡咯烷酮(K30)制备颗粒。作为机械强度或耐磨性的定量测量,颗粒在一定时间内进行脆碎度测试,并计算脆碎度指数(FI)随时间的变化函数。对获得的数据应用标准数学模型进行分析。根据最适合数据的逻辑模型和威布尔模型的导出参数,观察到用K30制备的颗粒的机械强度低于PGS和GEL颗粒,它们的模型参数值相似。基于威布尔时间参数选择的未脆碎(UFR)和脆碎(FR)颗粒的流动性质、固结和压缩行为进行了比较研究。颗粒的流速因颗粒尺寸减小而降低,这取决于粘合剂类型和脆碎度,但休止角的值在可接受范围内。关于固结行为,GEL的FR颗粒的相对密度随敲击次数的变化,即堆积速率,比其UFR形式慢,而PGS和K30的FR颗粒与其UFR形式相比,相对密度变化更快。根据从赫克尔方程获得的参数,发现PGS和K30比GEL产生更软、更具塑性且易于变形的颗粒,并且它们的FR形式的压缩性没有受到负面影响。