TY - JOUR
T1 - The ubiquity of the tabletability flip phenomenon
AU - Wang, Zijian
AU - Wang, Chenguang
AU - Bahl, Deepak
AU - Sun, Changquan Calvin
N1 - Publisher Copyright:
© 2023 Elsevier B.V.
PY - 2023/8/25
Y1 - 2023/8/25
N2 - The plasticity of materials plays a critical role in adequate powder tabletability, which is required in developing a successful tablet product. Generally, a more plastic material can develop larger bonding areas when other factors are the same, leading to higher tabletability than less plastic materials. However, it was observed that, for a solid form of a compound with poorer tabletability, a mixture with microcrystalline cellulose (MCC) can actually exhibit better tabletability, a phenomenon termed tabletability flip. Hence, there is a chance that a solid form with poor tabletability could have been erroneously eliminated based on the expected tabletability challenges during tablet manufacturing. This study was conducted to investigate the generality of this phenomenon using two polymorph pairs, a salt and free acid pair, a crystalline and amorphous solid dispersion pair, and a pair of chemically distinct crystals. Results show that tabletability flip occurred in all six systems tested, including five pairs of binary mixtures with MCC and one pair in a realistic generic tablet formulation, suggesting the broad occurrence of the tabletability flip phenomenon, where both compaction pressure and the difference in plasticity between the pair of materials play important roles.
AB - The plasticity of materials plays a critical role in adequate powder tabletability, which is required in developing a successful tablet product. Generally, a more plastic material can develop larger bonding areas when other factors are the same, leading to higher tabletability than less plastic materials. However, it was observed that, for a solid form of a compound with poorer tabletability, a mixture with microcrystalline cellulose (MCC) can actually exhibit better tabletability, a phenomenon termed tabletability flip. Hence, there is a chance that a solid form with poor tabletability could have been erroneously eliminated based on the expected tabletability challenges during tablet manufacturing. This study was conducted to investigate the generality of this phenomenon using two polymorph pairs, a salt and free acid pair, a crystalline and amorphous solid dispersion pair, and a pair of chemically distinct crystals. Results show that tabletability flip occurred in all six systems tested, including five pairs of binary mixtures with MCC and one pair in a realistic generic tablet formulation, suggesting the broad occurrence of the tabletability flip phenomenon, where both compaction pressure and the difference in plasticity between the pair of materials play important roles.
KW - Bonding area
KW - Generality
KW - Mixture
KW - Plasticity
KW - Tabletability flip
UR - http://www.scopus.com/inward/record.url?scp=85166511323&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=85166511323&partnerID=8YFLogxK
U2 - 10.1016/j.ijpharm.2023.123262
DO - 10.1016/j.ijpharm.2023.123262
M3 - Article
C2 - 37495026
AN - SCOPUS:85166511323
SN - 0378-5173
VL - 643
JO - International journal of pharmaceutics
JF - International journal of pharmaceutics
M1 - 123262
ER -