添加增塑剂后微晶纤维素球的可塑性增加

Artūrs Paulausks, Tetiana Kolisnyk, V. Mohylyuk
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摘要

压实压力会导致药物发生不理想的固态多晶型转变、碎裂、包衣颗粒完整性丧失以及微生物存活率和活力下降。因此,增加可塑性的辅料可作为减少压实压力不良影响的一种选择。本研究旨在通过在干燥的微晶纤维素(MCC)中添加特选的增塑剂来提高其可塑性(降低平均屈服压力;Py)。柠檬酸二乙酯 (DEC)、水和甘油是考虑使用的增塑剂。通过计算溶解度参数来预测 MCC 与增塑剂的混溶性(可能的增塑作用)。通过溶剂法获得了含 5.0 重量%的水、5.2 重量%的 DEC 和 4.2 重量%的甘油的增塑剂 MCC 球体,然后进行溶剂蒸发。使用 TGA、DSC、pXRD、傅立叶变换红外光谱、压力-位移曲线和模内 Heckel 图对添加增塑剂的配方进行了表征。根据模内赫克尔分析得出 Py 值,并将其作为塑性参数。与未增塑的 MCC(Py = 136.5 兆帕)相比,从 DEC(124.7 兆帕)到水(106.6 兆帕)和甘油(99.9 兆帕),增塑剂负载配方的塑性增加(Py 下降),这完全符合根据溶解度参数预测的混溶性相似度顺序。因此,水和甘油能够使非塑化 MCC 球体的 Py 值分别降低 16.3% 和 30.0%。这项可行性研究表明,可以通过在 MCC 中添加特选增塑剂来改变其可塑性。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
The Increase in the Plasticity of Microcrystalline Cellulose Spheres’ When Loaded with a Plasticizer
Compaction pressure can induce an undesirable solid-state polymorphic transition in drugs, fragmentation, loss of coated pellet integrity, and the decreased viability and vitality of microorganisms. Thus, the excipients with increased plasticity can be considered as an option to decrease the undesirable effects of compaction pressure. This study aims to increase the plasticity (to reduce the mean yield pressure; Py) of dried microcrystalline cellulose (MCC) by loading it with a specially selected plasticizer. Diethyl citrate (DEC), water, and glycerol were the considered plasticizers. Computation of solubility parameters was used to predict the miscibility of MCC with plasticizers (possible plasticization effect). Plasticizer-loaded MCC spheres with 5.0 wt.% of water, 5.2 wt.% of DEC, and 4.2 wt.% glycerol were obtained via the solvent method, followed by solvent evaporation. Plasticizer-loaded formulations were characterised by TGA, DSC, pXRD, FTIR, pressure-displacement profiles, and in-die Heckel plots. Py was derived from the in-die Heckel analysis and was used as a plasticity parameter. In comparison with non-plasticized MCC (Py = 136.5 MPa), the plasticity of plasticizer-loaded formulations increased (and Py decreased) from DEC (124.7 MPa) to water (106.6 MPa) and glycerol (99.9 MPa), and that was in full accordance with the predicted miscibility likeliness order based on solubility parameters. Therefore, water and glycerol were able to decrease the Py of non-plasticized MCC spheres by 16.3 and 30.0%, respectively. This feasibility study showed the possibility of modifying the plasticity of MCC by loading it with a specially selected plasticizer.
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