Kolter K, Flick D
BASF Aktiengesellschaft, Product Development Pharma/Food, Ludwigshafen, Germany.
Drug Dev Ind Pharm. 2000 Nov;26(11):1159-65. doi: 10.1081/ddc-100100987.
The dry binding activity of copolyvidone (Kollidon VA 64), povidone (Kollidon 30), microcrystalline cellulose (Avicel PH-101), hydroxypropylmethylcellulose (HPMC) 2910 (Pharmacoat 606), and maltodextrin (Maldex 18) was investigated using a variety of formulations and methods. The effect of the dry binders in direct tableting and compaction was studied using a dicalcium phosphate formulation (water-insoluble ingredients) and a vitamin C formulation (water-soluble ingredients) applying three compression forces. The binder content was varied between 5% and 15% in both formulations, and the tablet properties were determined. All the tablets showed an improvement in mechanical properties (hardness, friability) with increasing dry binder concentration, with Kollidon VA 64 showing by far the greatest binding efficacy. A significant influence (prolongation) on drug release was observed only with HPMC 2910. The drying binding properties were analyzed for correlations with various powder and material properties. Especially, particle size, surface/surface structure, and plasticity were found to influence binding activity. The ideal dry binder should have small particles, high plasticity, and a large surface area.
使用多种制剂和方法研究了共聚维酮(聚乙烯吡咯烷酮共聚物,Kollidon VA 64)、聚维酮(聚乙烯吡咯烷酮,Kollidon 30)、微晶纤维素(Avicel PH - 101)、羟丙基甲基纤维素(HPMC)2910(Pharmacoat 606)和麦芽糊精(Maldex 18)的干粘合活性。使用磷酸氢钙制剂(水不溶性成分)和维生素C制剂(水溶性成分),施加三种压力,研究了干粘合剂在直接压片和压片中的作用。两种制剂中的粘合剂含量在5%至15%之间变化,并测定了片剂性质。随着干粘合剂浓度的增加,所有片剂的机械性能(硬度、脆碎度)均有所改善,其中Kollidon VA 64的粘合效果最为显著。仅观察到HPMC 2910对药物释放有显著影响(延长)。分析了干粘合性能与各种粉末和材料性质之间的相关性。特别是,发现粒径、表面/表面结构和可塑性会影响粘合活性。理想的干粘合剂应具有小颗粒、高可塑性和大表面积。