Picker-Freyer Katharina M, Dürig Thomas
Martin-Luther-University Halle-Wittenberg, Institute of Pharmaceutics and Biopharmaceutics, Wolfgang-Langenbeck-Str 4, 06120 Halle/Saale, Germany.
AAPS PharmSciTech. 2007 Nov 9;8(4):E92. doi: 10.1208/pt0804092.
The aim of the study was to analyze hydroxypropylcellulose (HPC) in pure form and in excipient mixtures and to relate its physical and chemical properties to tablet binder functionality. The materials used were Klucel hydroxypropylcellulose grades ranging from low to high molecular weight (80-1000 kDa) of regular particle size (250 microm mean size) and fine particle size (80 microm mean size). These were compared with microcrystalline cellulose, spray-dried lactose, and dicalcium phosphate dihydrate. Thermal behavior of HPC was analyzed by modulated temperature differential scanning calorimetry (MTDSC). Tablets of the pure materials and of dry blends with 4% low viscosity, fine particle HPC and 30% high viscosity, fine particle HPC were produced on an instrumented eccentric tableting machine at 3 relative humidities. The 3-dimensional (3-D) model with the parameters time plasticity d, pressure plasticity e, and the twisting angle omega, the inverse of fast elastic decompression was compared with the Heckel method for characterization of compaction. Elastic recovery and compactibility were also studied. The results show that HPC tablet formation is characterized by high plastic deformation. The d, e, and omega values were markedly higher as compared with the reference materials. Plasticity was highest for the fine particle size HPC types. Maximum compactibility was observed for low molecular weight, fine particle size HPC. Tableting of the mixtures showed deformation, which was strongly influenced by HPC. Plasticity and crushing force of formed tablets was increased. In conclusion, HPC is characterized by strong plastic deformation properties, which are molecular weight and particle size dependent.
本研究的目的是分析纯形式以及辅料混合物中的羟丙基纤维素(HPC),并将其物理和化学性质与片剂粘合剂功能相关联。所使用的材料是不同分子量(80 - 1000 kDa)的常规粒径(平均粒径250微米)和细粒径(平均粒径80微米)的Klucel羟丙基纤维素等级产品。将这些产品与微晶纤维素、喷雾干燥乳糖和二水磷酸氢钙进行比较。通过调制温度差示扫描量热法(MTDSC)分析HPC的热行为。在一台带有仪器的偏心压片机上,于3种相对湿度条件下制备纯材料以及含有4%低粘度、细粒径HPC和30%高粘度、细粒径HPC的干混物片剂。将具有时间可塑性d、压力可塑性e和扭转角ω(快速弹性解压的倒数)参数的三维(3 - D)模型与Heckel方法进行比较,以表征压实情况。还研究了弹性恢复和可压性。结果表明,HPC片剂成型的特点是具有高塑性变形。与参比材料相比,d、e和ω值明显更高。细粒径HPC类型的可塑性最高。低分子量、细粒径HPC的可压性最高。混合物压片显示出变形,这受到HPC的强烈影响。成型片剂的可塑性和压碎力增加。总之,HPC的特点是具有强烈的塑性变形特性,这取决于分子量和粒径。