Abstract
As one of the commonly-used solid dosage forms, pharmaceutical tablets have been widely used to deliver active drugs into the human body, satisfying patient’s therapeutic requirements. To manufacture tablets of good quality, diluent powders are generally used in formulation development to increase the bulk of formulations and to bind other inactive ingredients with the active pharmaceutical ingredients (APIs). For formulations of a low API dose, the drug products generally consist of a large fraction of diluent powders. Hence, the attributes of diluents become extremely important and can significantly influence the final product property. Therefore, it is essential to accurately characterise the mechanical properties of the diluents and to thoroughly understand how their mechanical properties affect the manufacturing performance and properties of the final products, which will build a sound scientific basis for formulation design and product development. In this study, a comprehensive evaluation of the mechanical properties of the widely-used pharmaceutical diluent powders, including microcrystalline cellulose (MCC) powders with different grades (i.e., Avicel PH 101, Avicel PH 102, and DG), mannitol SD 100, lactose monohydrate, and dibasic calcium phosphate, were performed. The powder compressibility was assessed with Heckel and Kawakita analyses. The material elastic recovery during decompression and in storage was investigated through monitoring the change in the dimensions of the compressed tablets over time. The powder hygroscopicity was also evaluated to examine the water absorption ability of powders from the surroundings. It was shown that the MCC tablets exhibited continuous volume expansion after ejection, which is believed to be induced by (1) water absorption from the surrounding, and (2) elastic recovery. However, mannitol tablets showed volume expansion immediately after ejection, followed by the material shrinkage in storage. It is anticipated that the expansion was induced by elastic recovery to a limited extent, while the shrinkage was primarily due to the solidification during storage. It was also found that, for all powders considered, the powder compressibility and the elastic recovery depended significantly on the particle breakage tendency: a decrease in the particle breakage tendency led to a slight decrease in the powder compressibility and a significant drop in immediate elastic recovery. This implies that the particle breakage tendency is a critical material attribute in controlling the compression behaviour of pharmaceutical powders.
Highlights
Pharmaceutical tablets are one of the most preferred dosage forms for drug administration to treat diseases, providing quick therapies to satisfy patient demands [1,2]
Seven different pharmaceutical diluent powders were considered in this paper, including three microcrystalline cellulose (MCC) powders (FMC, Biopolymer, Philadelphia, PA, USA) with different grades, Avicel PH 102, Avicel PH 101 and DG
The Heckel yield pressure (Py ) was commonly used to describe powder compressibility as it was directly related to powder plastic behaviour [19,20] and the hardness of particles [21]
Summary
Pharmaceutical tablets are one of the most preferred dosage forms for drug administration to treat diseases, providing quick therapies to satisfy patient demands [1,2]. Narayan and Hancock [5] studied the relationship between the powder property and the roughness of the tablet surface using diluent powders, such as MCC, mannitol and lactose monohydrate. They concluded that deformation mechanisms affected the mechanical behaviour and surface roughness of the compacts. Akseli et al [6] investigated the Young’s modulus anisotropy of different tablets using the ultrasonic method They observed that the density of MCC tablets increased more rapidly during compression and more shear deformation took place comparing with lactose tablets.
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