Factors affecting performance and manufacturability of naproxen Liqui-Pellet.

Matthew Lam, Ali Nokhodchi
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引用次数: 8

Abstract

Aim: Liqui-Pellet is potentially an emerging next-generation oral pill, which has shown promising results with unique advantages as well as displaying potential for commercial feasibility. Since Liqui-Pellet technology is still in its infancy, it is important to explore the parameters that can affect its performance, particularly the drug release rate. Therefore, the aim of this study is to investigate thoroughly the effect of Avicel PH101 (carrier) and Aerosil 300 (coating material) ratio (R-value) in Liqui-Pellet.

Methods: Key parameter for Liqui-Pellet formulation in this study was the ratio of carrier and coating material. Tests were carried out to assess the physicochemical properties of different formulations. This involved looking into particle size, robustness, flowability, solid-state and drug release profile. The morphology of Liqui-Pellet was investigated by SEM.

Results: It is found that R-value does not have a major effect on the success of Liqui-Pellet production. However, R-value does seem to have an effect on Liqui-Pellet size at a certain water content level and a slight effect on the drug release rate. A decrease in Avicel PH101 concentration and an increase in Aerosil 300 concentration in Liqui-Pellet formulations can reduce Liqui-Pellet size and slightly increase drug release rate by 9% after 2 h. The data shows Liqui-Pellet is resistant to friability, able to achieve exceptional flow property and have smooth surfaces, which is critical for applying coatings technology. Such properties are ideal in terms of commercial manufacturing. The XRPD and DSC both show the reduction in formulation crystallinity, which is expected in Liqui-Pellet formulation as a result of solubility of the drug in the co-solvent used in the preparation of Liqui-Pellets.

Conclusion: Overall it seems that R-value can affect Liqui-Pellet drug release rate and size but not on the production success rate.

Abstract Image

Abstract Image

Abstract Image

影响萘普生液丸性能及可生产性的因素。
目的:liquid - pellet是一种潜在的新一代口服药丸,具有独特的优势和潜在的商业可行性。由于液体颗粒技术仍处于起步阶段,探索影响其性能的参数,特别是药物释放速度是很重要的。因此,本研究的目的是深入研究Avicel PH101(载体)和Aerosil 300(涂层材料)的比例(r值)对液体颗粒的影响。方法:以载体与包衣材料的配比为主要处方参数。进行了试验,以评估不同配方的物理化学性质。这包括观察颗粒大小,坚固性,流动性,固体状态和药物释放概况。用扫描电镜研究了液相球团的形貌。结果:发现r值对液丸生产的成功与否影响不大。然而,在一定含水量水平下,r值似乎对液丸大小有影响,对药物释放速度有轻微影响。降低Avicel PH101浓度和增加Aerosil 300浓度可以减小液体颗粒的尺寸,并在2小时后略微增加9%的药物释放率。数据显示,液体颗粒具有抗脆性,能够实现卓越的流动性能,表面光滑,这对于应用涂层技术至关重要。这种特性在商业制造方面是理想的。XRPD和DSC都显示了配方结晶性的降低,这是液体颗粒配方中预期的,因为药物在制备液体颗粒时使用的共溶剂中的溶解度。结论:总体上看,r值对液体颗粒的释药速度和大小有影响,但对生产成功率没有影响。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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