Improving Tabletability of Excipients by Metal-Organic Framework-Based Cocrystallization: a Study of Mannitol and CaCl2

Puerarin-Na Chelate Hydrate Simultaneously Improves Dissolution and Mechanical Behavior

“…To overcome the influence of mechanical anisotropy in a given crystallographic orientation, CTC (compressibility, tabletability, compactibility) analysis is one of the effective methods for evaluating the bulk deformability of the random orientation in solid materials. ,, Compressibility is measured by plotting the porosity as a function of the compression pressure. , The compressibility plot (Figure A) presents that PUE-Na had higher porosities than PUEM, suggesting that PUE-Na had a lower bonding area (BA) and weaker compressibility than PUEM . The interparticulate lower BA of PUE-Na might correlate with the higher elastic recovery value ( r e ) 5 (Table ).…”

“…Compactibility represents the functional change of tensile strength against tablet porosity . The compactibility plot (Figure C) displays that the tensile strength (σ) of PUE-Na at a given porosity was much higher than that of PUEM, suggesting its stronger interparticulate bonding strength (BS) over PUEM.…”

“…It was found that each PUE molecule was linked to the surrounding water molecules through seven hydrogen bonds in the PUEM unit cell, while in the PUE-Na unit cell, the interaction between each PUE molecule and water molecules included 13 hydrogen bonds (2 charge assisted hydrogen bonds and 11 OH···O hydrogen bonds) and 6 Na–O coordinated bonds (Figure S2 and Tables S2 and S3). The noncovalent bonds follow the average bond energy order of coordinated bonds > charge assisted hydrogen bonds > OH···O hydrogen bonds. , Thus, PUE-Na would release higher noncovalent bond energy in the dehydration progress than PUEM, leading to its higher dehydration enthalpic energy.…”

“…10,55,56 Compressibility is measured by plotting the porosity as a function of the compression pressure. 5,57 The compressibility plot (Figure 8A) presents that PUE-Na had higher porosities than PUEM, suggesting that PUE-Na had a lower bonding area (BA) and weaker compressibility than PUEM. 58 The interparticulate lower BA of PUE-Na might correlate with the higher elastic recovery value (r e ) 5 (Table 3).…”

“…More than 80% of active pharmaceutical ingredients (APIs) are formulated in solid forms . The different molecular stacking and periodicity in the interstructure of solid drugs will generate different solid forms (e.g., amorphous, polymorph, solvate, salt, and cocrystal), which always exhibit obvious distinguishable properties, such as solubility, flowability, mechanical property, and hygroscopicity . The differences in these physicochemical properties might have significant effects on their manufacturability, stability, in vitro dissolution, and even in vivo drug absorption after oral administration .…”