Department of Pharmacy, Drug Transport and Delivery Research Group, University of Tromsoe, 9037 Tromsø, Norway.
AAPS PharmSciTech. 2010 Mar;11(1):18-26. doi: 10.1208/s12249-009-9349-4. Epub 2009 Dec 15.
The objective of this study was to evaluate possible usefulness of pectins for direct compression of tablets. The deformation behavior of pectin grades of different degree of methoxylation (DM), namely, 5%, 10%, 25%, 35%, 40%, 50%, and 60% were, examined in terms of yield pressures (YP) derived from Heckel profiles for both compression and decompression and measurements of elastic recovery after ejection. All pectin grades showed a high degree of elastic recovery. DM 60% exhibited most plastic deformation (YP 70.4 MPa) whereas DM 5% (104.6 MPa) and DM 10% (114.7 MPa) least. However, DM 60% gave no coherent tablets, whereas tablet tensile strengths for DM 5% and DM 10% were comparable to Starch 1500. Also, Heckel profiles were similar to Starch 1500. For sieved fractions (180-250 and 90-125 mum) of DM 25% and DM 40% originating from the very same batch, YPs were alike, indicating minor effects of particle size. These facts indicate that DM is important for the compaction behavior, and batch-to-batch variability should also be considered. Therefore, pectins of low degree of methoxylation may have a potential as direct compression excipients.
本研究旨在评估果胶在直接压片中的潜在用途。我们考察了不同甲氧基化程度(DM)的果胶等级(5%、10%、25%、35%、40%、50%和 60%)的变形行为,通过 Heckel 图谱得出的压缩和解压屈服压力(YP)以及压片后弹性恢复的测量来进行评估。所有果胶等级都表现出高度的弹性恢复。DM 60%表现出最大的塑性变形(YP 为 70.4 MPa),而 DM 5%(104.6 MPa)和 DM 10%(114.7 MPa)的变形最小。然而,DM 60%无法压制成均匀的片剂,而 DM 5%和 DM 10%的片剂拉伸强度与 Starch 1500 相当。此外,Heckel 图谱与 Starch 1500 相似。对于来自同一批次的 DM 25%和 DM 40%的过筛部分(180-250 和 90-125 µm),YP 相似,表明粒径的影响较小。这些事实表明,DM 对压缩行为很重要,批次间的变异性也应考虑在内。因此,低甲氧基化程度的果胶可能具有作为直接压片赋形剂的潜力。