Division of Product Quality Research, Office of Testing and Research, Office of Pharmaceutical Quality, Center for Drug Evaluation and Research, U.S. Food and Drug Administration, 10903 New Hampshire ave., Silver Spring, MD 20903, USA.
Division of Product Quality Research, Office of Testing and Research, Office of Pharmaceutical Quality, Center for Drug Evaluation and Research, U.S. Food and Drug Administration, 10903 New Hampshire ave., Silver Spring, MD 20903, USA; Department of Chemical and Biochemical Engineering, Rutgers, The State University of New Jersey.
Int J Pharm. 2022 Jul 25;623:121964. doi: 10.1016/j.ijpharm.2022.121964. Epub 2022 Jun 25.
This study aimed at understanding the effect of screw design on the critical characteristics of granules and tablets of an extended-release (ER) formulation for twin screw granulation process. The screw design parameters assessed included number of kneading elements (KEs) per kneading zone, distance separating kneading zones, staggering angle (SA) of kneading elements and number of sizing elements (SEs). These input variables were varied using a design of experiment (DoE) approach to manufacture granules. Particle size distribution (PSD), flow and bulk properties of the granules, breaking strength and dissolution of tablets manufactured using these granules were characterized. The results of least square fitting showed that KEs, SA, and SEs of the screws significantly (p -values < 0.05) affected the PSD, cohesion, compressibility (CPS), conditioned bulk density (CBD) and permeability of the granules. The KEs and SEs significantly (p -value < 0.05) affected the dissolution, which was attributed to their effects on CPS and CBD of the granules. The distance between kneading zones had no significant effect on granules and tablet characteristics. These results may be used to further study the interaction of the identified critical screw design parameters with other processing parameters for continuous manufacturing of this ER matrix-based tablet formulation.
本研究旨在了解螺杆设计对双螺杆造粒工艺中缓释(ER)制剂颗粒和片剂关键特性的影响。评估的螺杆设计参数包括每个捏合区的捏合元件(KE)数量、捏合区之间的距离、捏合元件的交错角(SA)以及定径元件(SE)的数量。使用实验设计(DoE)方法来制造颗粒,对这些输入变量进行了变化。对颗粒的粒径分布(PSD)、流动性和堆积特性、片剂的断裂强度和溶出度进行了表征。最小二乘拟合的结果表明,螺杆的 KE、SA 和 SE 显著(p 值 < 0.05)影响颗粒的 PSD、内聚性、可压缩性(CPS)、条件堆积密度(CBD)和渗透性。KE 和 SE 显著(p 值 < 0.05)影响了片剂的溶出度,这归因于它们对颗粒 CPS 和 CBD 的影响。捏合区之间的距离对颗粒和片剂特性没有显著影响。这些结果可用于进一步研究已确定的关键螺杆设计参数与其他加工参数之间的相互作用,以实现这种 ER 基质片剂制剂的连续制造。