Schmid Wolfgang, Picker-Freyer Katharina M
Institute of Pharmacy, Martin-Luther-University Halle-Wittenberg, Halle, Germany.
Eur J Pharm Biopharm. 2009 May;72(1):165-72. doi: 10.1016/j.ejpb.2008.10.006. Epub 2008 Oct 21.
The aim of the study was to evaluate the suitability of alginates for Soft Tableting. For this purpose the compaction properties of alginates, varying in molecular weight, guluronic acid/mannuronic acid ratio and salt, were investigated and compared to MCC. Based on the mechanical properties, the suitability of the tested excipients for Soft Tableting was predicted. In order to test the prediction the tested materials were used to tablet enteric coated pellets, which served as a pressure sensitive material. The tableting behaviour was analysed by the 3-D modeling technique. The tablet properties were analysed by determining the elastic recovery and the compactibility. Alginates in general deformed elastically. The compression behaviour depended on the chemical composition of the alginates with sodium alginates being more elastic than potassium alginates. Tablets containing alginates with low guluronic acid content exhibited higher elasticity than tablets with alginates having a low mannuronic acid content. The plasticity of potassium alginates was higher than for sodium alginates. However, the plasticity of all tested alginates was lower than the plasticity of MCC. The compactibility of the tested alginates was sufficient. The proposed prediction, which states that tableting excipients with higher elasticity are more suitable for tableting sensitive materials than plastic excipients, was valid for the tested materials. The elastic alginates inflicted less damage on the pellets than the plastic MCC. Thus, all alginates were more appropriate for tableting pressure sensitive materials than MCC.
本研究的目的是评估藻酸盐用于软压片的适用性。为此,研究了不同分子量、古洛糖醛酸/甘露糖醛酸比例和盐的藻酸盐的压缩特性,并与微晶纤维素(MCC)进行比较。基于力学性能,预测了受试辅料用于软压片的适用性。为了验证该预测,将受试材料用于压制肠溶包衣微丸,其作为压敏材料。通过三维建模技术分析压片行为。通过测定弹性回复率和可压性来分析片剂性能。藻酸盐总体上发生弹性变形。压缩行为取决于藻酸盐的化学组成,海藻酸钠比海藻酸钾更具弹性。含有低古洛糖醛酸含量藻酸盐的片剂比含有低甘露糖醛酸含量藻酸盐的片剂表现出更高的弹性。海藻酸钾的可塑性高于海藻酸钠。然而,所有受试藻酸盐的可塑性均低于微晶纤维素。受试藻酸盐的可压性足够。所提出的预测,即弹性较高的压片辅料比塑性辅料更适合压制敏感材料,对受试材料是有效的。与塑性微晶纤维素相比,弹性藻酸盐对微丸造成的损伤更小。因此,所有藻酸盐比微晶纤维素更适合压制压敏材料。