Abstract：
Direct compression is a tableting technique that involves a few steps in non-demanding manufacturing conditions. High strength and rapid disintegration of tablet formulations were previously achieved through the addition of cellulose nanofibers (CNFs), which have recently attracted attention as a high-performance biomass material. However, CNF addition results in greater variation in tablet weight and drug content, potentially due to differences in particle size between CNF and other additives. Herein, we used pulverized CNF to evaluate the effect of CNF particle size on the variation in tablet weight and drug content. Tablet formulations consisted of CNF with different particle sizes (approximately 100 µm [CNF100] and 300 µm [CNF300], at 0, 10, 30, or 50%), lactose hydrate, acetaminophen, and magnesium stearate. Ten powder formulations with different particle sizes and CNF concentrations were prepared; thereafter, the tablets were produced using a rotary tableting press with a compression force of 10 kN. The variation in weight and drug content as well as the tensile strength, friability, disintegration time, and drug dissolution of tablets were evaluated. CNF100 addition to the tablets reduced the weight and drug content variation to a greater extent than CNF300 addition. Using CNF300, we produced tablets of sufficient strength and short disintegration time. These properties were also achieved with CNF100 addition. Our findings suggest that adding CNF of small particle size to the tablet formulation can reduce the variation in weight and drug content while maintaining high strength and short disintegration time.
摘要：
直接压缩是一种压片技术,其涉及在非苛刻的制造条件下的几个步骤。片剂制剂的高强度和快速崩解先前通过添加纤维素纳米纤维(CNFs)来实现,最近作为一种高性能生物质材料引起了人们的关注。然而,添加CNF会导致片剂重量和药物含量的更大变化，可能是由于CNF和其他添加剂之间的粒径差异。在这里，我们使用粉碎的CNF来评估CNF粒径对片剂重量和药物含量变化的影响。片剂制剂由不同粒径的CNF组成（约100μm[CNF100]和300μm[CNF300]，在0、10、30或50%)，乳糖水合物，对乙酰氨基酚,和硬脂酸镁。制备了10种具有不同粒径和CNF浓度的粉末制剂；此后，使用旋转压片机以10kN的压缩力生产片剂。重量和药物含量以及拉伸强度的变化，脆性,崩解时间,评价片剂的药物溶出度。向片剂中添加CNF100比添加CNF300更大程度地减少了重量和药物含量变化。使用CNF300,我们生产具有足够强度和短崩解时间的片剂。这些性质也通过添加CNF100来实现。我们的发现表明，在片剂中添加小粒径的CNF可以减少重量和药物含量的变化，同时保持高强度和短崩解时间。
