Denduyver Phaedra, Birk Gudrun, Ambruosi Alessandra, Vervaet Chris, Vanhoorne Valérie
Laboratory of Pharmaceutical Technology, Department of Pharmaceutics, Ghent University, Ottergemsesteenweg 460, 9000 Ghent, Belgium.
Merck KGaA, Frankfuter Str. 250, 64293 Darmstadt, Germany.
Pharmaceutics. 2024 Jun 25;16(7):854. doi: 10.3390/pharmaceutics16070854.
Binder selection is a crucial step in continuous twin-screw wet granulation (TSWG), as the material experiences a much shorter residence time (2-40 s) in the granulator barrel compared to batch-wise granulation processes. Polyvinyl alcohol (PVA) 4-88 was identified as an effective binder during TSWG, but the potential of other PVA grades-differing in polymerization and hydrolysis degree-has not yet been studied. Therefore, the aim of the current study was to evaluate the potential of different PVA grades as a binder during TSWG. The breakage and drying behavior during the fluidized bed drying of drug-loaded granules containing the PVA grades was also studied. Three PVA grades (4-88, 18-88, and 40-88) were characterized and their attributes were compared to previously investigated binders by Vandevivere et al. through principal component analysis. Three binder clusters could be distinguished according to their attributes, whereby each cluster contained a PVA grade and a previously investigated binder. PVA 4-88 was the most effective binder of the PVA grades for both a good water-soluble and water-insoluble formulation. This could be attributed to its high total surface energy, low viscosity, good wettability of hydrophilic and hydrophobic surfaces, and good wettability by water of the binder. Compared to the previously investigated binders, all PVA grades were more effective in the water-insoluble formulation, as they yielded strong granules (friability below 30%) at lower L/S-ratios. This was linked to the high dispersive surface energy of the high-energy sites on the surface of PVA grades and their low surface tension. During fluidized bed drying, PVA grades proved suitable binders, as the acetaminophen (APAP) granules were dried within a short time due to the low L/S-ratio, at which high-quality granules could be produced. In addition, no attrition occurred, and strong tablets were obtained. Based on this study, PVA could be the preferred binder during twin screw granulation due to its high binder effectiveness at a low L/S-ratio, allowing efficient downstream processing. However, process robustness must be controlled by the included excipients, as PVA grades are operating in a narrow L/S-ratio range.
粘合剂的选择是连续双螺杆湿法制粒(TSWG)中的关键步骤,因为与间歇式制粒工艺相比,物料在制粒机筒体内的停留时间要短得多(2 - 40秒)。聚乙烯醇(PVA)4 - 88在TSWG过程中被确定为一种有效的粘合剂,但其他在聚合度和水解度上不同的PVA等级的潜力尚未得到研究。因此,本研究的目的是评估不同PVA等级在TSWG过程中作为粘合剂的潜力。还研究了含PVA等级的载药颗粒在流化床干燥过程中的破碎和干燥行为。对三种PVA等级(4 - 88、18 - 88和40 - 88)进行了表征,并通过主成分分析将它们的属性与Vandevivere等人先前研究的粘合剂进行了比较。根据其属性可以区分出三个粘合剂簇,每个簇包含一个PVA等级和一种先前研究的粘合剂。对于水溶性和水不溶性制剂,PVA 4 - 88都是PVA等级中最有效的粘合剂。这可能归因于其高总表面能、低粘度、对亲水和疏水表面良好的润湿性以及粘合剂对水的良好润湿性。与先前研究的粘合剂相比,所有PVA等级在水不溶性制剂中更有效,因为它们在较低的液固比下就能得到强度高的颗粒(脆碎度低于30%)。这与PVA等级表面高能位点的高分散表面能及其低表面张力有关。在流化床干燥过程中,PVA等级被证明是合适的粘合剂,因为由于液固比低,对乙酰氨基酚(APAP)颗粒能在短时间内干燥,在此条件下可以生产出高质量的颗粒。此外,没有发生磨损,并且得到了强度高的片剂。基于这项研究,由于PVA在低液固比下具有高粘合剂效能,能够实现高效的下游加工,因此它可能是双螺杆制粒过程中的首选粘合剂。然而,由于PVA等级在较窄的液固比范围内运行,工艺稳健性必须通过所包含的辅料来控制。