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使用粉末流变学评估助流剂对酮洛芬片剂黏附倾向的影响。

Evaluating the effect of glidants on tablet sticking propensity of ketoprofen using powder rheology.

作者信息

Parekh Bhavin V, Saddik Joseph S, Patel Devang B, Dave Rutesh H

机构信息

Arnold and Marine Schwartz College of Pharmacy and Health Sciences, Long Island University, Brooklyn, NY, USA; Natoli Institute for Industrial Pharmacy Research and Development, Long Island University, Brooklyn, NY, USA.

Pfizer Inc., Groton, CT, USA.

出版信息

Int J Pharm. 2023 Mar 25;635:122710. doi: 10.1016/j.ijpharm.2023.122710. Epub 2023 Feb 9.

Abstract

Punch sticking has been a leading drawback that has challenged successful tablet manufacturing since its initial conception. Due to the capricious nature of the complication, this can arise during any phase of the development process. Even now, identifying such a problem is a prerequisite during the initial stage of development. The present study evaluated the role of Aerosil®200, talc, and Syloid®244 as glidants in varying amounts ranging from 0.0 percent to 2.0 percent w/w on tablets sticking relatively to five different metal surfaces, with ketoprofen as the model drug. Powder rheology is a predictable technique used to calculate the sticking index. The sticking index of each formulation in comparison to each metal coupon was identified by calculating the kinematic angle of internal friction and the angle of wall friction using the shear cell test and wall friction test, respectively. Interestingly, glidants were found to reduce the sticking propensity of the powder blend in a concentration-dependent manner. In addition, the compression study validated the expected sticking tendency ranking order. According to the research data, the sticking index could effectively be utilized to envisage the possibility of tablet sticking, i.e., by selecting the formulation's excipient and their percentages or selecting appropriate punched metal surfaces in the tableting process.

摘要

自最初构思以来,冲模粘冲一直是片剂成功生产面临的主要障碍。由于这种复杂情况的反复无常,它可能在开发过程的任何阶段出现。即便如此,在开发的初始阶段识别此类问题仍是一项先决条件。本研究以酮洛芬为模型药物,评估了不同用量(0.0%至2.0%w/w)的气相二氧化硅®200、滑石粉和Syloid®244作为润滑剂对片剂在五种不同金属表面上的粘性的影响。粉末流变学是一种用于计算粘性指数的可预测技术。通过分别使用剪切池试验和壁面摩擦试验计算内摩擦运动角和壁面摩擦角,确定了每种配方与每个金属试片相比的粘性指数。有趣的是,发现润滑剂以浓度依赖的方式降低了粉末混合物的粘性倾向。此外,压缩研究验证了预期的粘性趋势排序。根据研究数据,粘性指数可有效地用于预测片剂粘冲的可能性,即在压片过程中通过选择配方的辅料及其百分比或选择合适的冲压金属表面来实现。

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