Picker-Freyer Katharina M, Brink Diana
Martin-Luther-University Halle-Wittenberg, Institute of Pharmaceutical Technology and Biopharmacy, Halle/Saale, Germany.
AAPS PharmSciTech. 2006 Sep 8;7(3):75. doi: 10.1208/pt070375.
The aim of this study was to analyze the process of tablet formation and the properties of the resulting tablets for 3 N-deacetylated chitosans, with a degree of deacetylation of 80%, 85%, or 90%. Material properties, such as water content, particle size and morphology, glass transition temperature, and molecular weight were studied. The process of tablet formation was analyzed by 3-D modeling, Heckel analysis, the pressure time function, and energy calculations in combination with elastic recovery dependent on maximum relative density and time. The crushing force and the morphology of the final tablets were analyzed. Chitosans sorb twice as much water as microcrystalline cellulose (MCC), the particle size is comparable to Avicel PH 200, a special type of MCC, the particles look like shells, and the edges are bent. Molecular weight ranges from 80,000 to 210,000 kDa, the glass transition temperature (Tg) was not dependent on molecular weight. The chitosans deform ductilely as MCC; however, plastic deformation with regard to time and also pressure plasticity are higher than for MCC, especially for Chit 85, which has the lowest crystallinity and molecular weight. At high densification, fast elastic decompression is higher. 3-D modeling allowed the most precise analysis. Elastic recovery after tableting is higher than for MCC tablets and continues for some time after tableting. The crushing force of the resulting tablets is high owing to a reversible exceeding of Tg in the amorphous parts of the material. However, the crushing force is lower compared with MCC, since the crystallinity and the Tg of the chitosans are higher than for MCC. In summation, chitosans show plastic deformation during compression combined with high elasticity after tableting. Highly mechanically stable tablets result.
本研究的目的是分析3种脱乙酰度为80%、85%或90%的N-脱乙酰壳聚糖的压片过程及所得片剂的性质。研究了材料性质,如水含量、粒度和形态、玻璃化转变温度和分子量。通过三维建模、赫克尔分析、压力-时间函数以及结合依赖于最大相对密度和时间的弹性恢复的能量计算来分析压片过程。分析了最终片剂的压碎力和形态。壳聚糖的吸水量是微晶纤维素(MCC)的两倍,粒度与一种特殊类型的MCC即微晶纤维素PH 200相当,颗粒看起来像贝壳,边缘弯曲。分子量范围为80,000至210,000 kDa,玻璃化转变温度(Tg)不依赖于分子量。壳聚糖与MCC一样发生延性变形;然而,相对于时间的塑性变形以及压力可塑性均高于MCC,尤其是脱乙酰度为85%的壳聚糖,其结晶度和分子量最低。在高密度化时,快速弹性减压更高。三维建模实现了最精确的分析。压片后的弹性恢复高于MCC片剂,并且在压片后会持续一段时间。由于材料无定形部分的Tg可逆性超过,所得片剂的压碎力较高。然而,与MCC相比,压碎力较低,因为壳聚糖的结晶度和Tg高于MCC。总之,壳聚糖在压缩过程中表现出塑性变形,压片后具有高弹性。由此得到机械稳定性高的片剂。