Thommes Markus, Kleinebudde Peter
Institute of Pharmaceutics and Biopharmaceutics, Heinrich-Heine-University, Duesseldorf, Germany.
Eur J Pharm Biopharm. 2006 May;63(1):59-67. doi: 10.1016/j.ejpb.2005.10.002. Epub 2005 Dec 2.
Microcrystalline cellulose (MCC) is commonly used as an excipient in extrusion/spheronisation process. However, MCC has several disadvantages as lack of disintegration and drug adsorption. Therefore, kappa-carrageenan was investigated to substitute MCC in pelletising processes. Formulations with 20% of pelletisation aid (kappa-carrageenan or MCC) and acetaminophen as a model drug have been produced. Different fillers (lactose, mannitol, maize starch and dicalciumphosphate dihydrate) at fractions of 0, 20, 40 and 80% were evaluated and the properties of the resulted pellets were determined (e.g. yield, aspect ratio, mean Feret diameter, 10% interval fraction, tensile strength and release profile). kappa-Carrageenan has proven to be a suitable substitute as pellets with sufficient quality were produced. The pellet batches of different formulations were characterised by high yield, spherical pellet shape and narrow pellet size distribution. The distinguished behaviour between kappa-carrageenan and MCC pellets was the lower tensile strength and the faster release of kappa-carrageenan pellets. For the various types and fractions of fillers only minor effects to the pelletisation process and pellet properties were noticed. From the practical view these effects are neglectable indicating a robust formulation and process.
微晶纤维素（MCC）通常用作挤出/滚圆法工艺中的辅料。然而，MCC存在一些缺点，如缺乏崩解性和药物吸附性。因此，研究了κ-卡拉胶以在制粒过程中替代MCC。制备了含20%制粒助剂（κ-卡拉胶或MCC）和对乙酰氨基酚作为模型药物的制剂。评估了0%、20%、40%和80%比例的不同填充剂（乳糖、甘露醇、玉米淀粉和二水磷酸氢钙），并测定了所得颗粒的性质（如收率、纵横比、平均费雷特直径、10%区间分数、拉伸强度和释放曲线）。已证明κ-卡拉胶是一种合适的替代品，因为制备出了质量足够的颗粒。不同制剂的颗粒批次具有高产率、球形颗粒形状和窄的颗粒尺寸分布的特点。κ-卡拉胶颗粒和MCC颗粒之间的显著差异在于κ-卡拉胶颗粒的拉伸强度较低且释放较快。对于各种类型和比例的填充剂，仅观察到对制粒过程和颗粒性质有轻微影响。从实际角度来看，这些影响可以忽略不计，表明制剂和工艺具有稳健性。
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