基于数学模型研究SuperTab 40LL对麝香缓释微片压缩特性的影响

Study on effect of SuperTab 40LL on compression characteristics of musk sustained-release mini-tablets based on mathematical models

该文选择复合型乳糖SuperTab 40LL为填充剂,研究西黄方多单元释药系统中麝香缓释微片的制备。分别设计含不同比例的SuperTab 40LL和MCC的麝香缓释片处方,于不同压力下压片,通过Walker、Heckel和Ryshkewitch-Duckworth方程,表征不同处方的压缩性和成型性,通过Kawakita方程,描述不同处方的流动性,结合SuperTab 40LL和MCC的外观形态及微片的抗张强度,全面分析SuperTab 40LL对麝香缓释微片压缩成型性的影响。结果表明,Heckel方程能较好的描述SuperTab 40LL的压缩变化过程,Kawakita和Ryshkewitch-Duckworth方程适用于药物粉体和辅料直接压片过程。SuperTab 40LL作为一种新型辅料,具有良好的流动性和压缩成型性,在压缩过程中可发生粒子破碎和塑性形变,增加了粒子间的接触面积和结合位点,使混合粉体易于聚集成型。MCC表现出协同作用,SuperTab 40LL与其联合应用有效改善了麝香缓释粉体的流动性和可压性,当两者比例为2∶1时,可制备出载药高、成型好的缓释微片,达到设计目标。

In this paper, co-processed lactose SuperTab 40 LL was selected as fillers to study the preparation of musk sustained-release mini-tablets in the Xihuang multiple-unit drug release system. Musk sustained-release tablets containing different proportions of SuperTab 40 LL and MCC were prepared under various pressures, and then the compressibility and compactibility of these prescriptions were evaluated by Walker, Heckel and Ryshkewitch-Duckworth equations. In addition, the fluidity of the prescriptions was evaluated by parameters of Kawakita equation. There was a comprehensive analysis of the effect of SuperTab 40 LL on musk sustained-release mini-tablets combined with the appearance of SuperTab 40 LL and their tensile strength. The results shown that SuperTab 40 LL had better compression process through the Heckel equation, and the direct compression process of drug powders with excipients can be analyzed by the Kawakita and Ryshkewitch-Duckworth equations. As a new type of co-processed lactose, SuperTab 40 LL had a good fluidity and compactibility. SuperTab 40 LL may undergo particle crushing and plastic deformation during the compression process, which increased the contact area and bonding sites between the particles, and aggregated and shaped the mixed powder easy. Moreover, MCC showed a synergistic effect, and the combined application with SuperTab 40 ll could effectively improve the fluidity and compressibility of the musk sustained-release powder. When the ratio of SuperTab 40 LL and MCC was 2∶1, musk sustained-release mini-tablets had a high drug loading capacity and good compactibility in line with the design objectives.