Lack of dependence of mechanical properties of baicalein cocrystals on those of the constituent components

Abstract

Three baicalein (BAI) cocrystals with nicotinamide (NCT), caffeine (CAF), and isoniazid (ISN) exhibited excellent tabletability despite the markedly different tabletability of the coformers.

Cocrystallization of Curcumin with Benzenediols and Benzenetriols via Rapid Solvent Removal

“…While the tabletability of the CUR–PYR cocrystal is comparable with that of PYR, all other four cocrystals exhibited higher tabletability than corresponding coformers as well (Figure S6). The synergistic effects again confirmed the effectiveness of improving tabletability by cocrystallization. ,− Such effects likely have their origins in unique crystal structures of the cocrystals in relation to the coformers …”

“…24,59−62 Such effects likely have their origins in unique crystal structures of the cocrystals in relation to the coformers. 63 3.7. Significance of the Study.…”

Insights into Cocrystallization and Coamorphization Engineering Techniques in the Delivery of Traditional Chinese Medicine: Formation Mechanism, Solid-State Characterization, and Improved Pharmaceutical Properties

“…PXRD is widely employed to detect the formation of cocrystals and identify the purity by comparing the experimental diffraction pattern of a cocrystal phase with the pattern simulated based on SCXRD data. For example, the cocrystal of baicalein and caffeine at an equimolar ratio could be synthesized by slow evaporation, 152 the slurry method, 152 or rotary evaporation, 136 and the phase purity was further confirmed through the comparison of the experimental PXRD pattern and the calculated one. In this case, the peak intensity is not usually taken account since it can be affected by various factors, such as morphology, particle size, instrument sensitivity, etc.…”

“…To successfully develop its tablet formulation, three cocrystal systems of baicalein with isoniazid in a 1:1 molar ratio, with caffeine in a 2:1 molar ratio, and with nicotinamide in a 1:1 molar ratio were synthesized. 136 All of these cocrystals showed significantly improved tabletability (Figure 7), which is proposed to be attributed to the improved plastic deformation induced by parallel molecular layers connected through weak hydrogen bonds. In addition, strong, three-dimensional intermolecular interactions in the crystal network structure contribute to improve the tabletability, compressibility, and compactibility of materials.…”

“…For example, baicalein extracted from Huang-Qin ( Scutellaria baicalensis Georgi ) has a high dose in commercial dosage form (≥200 mg) and shows extremely poor compressibility under pressure. To successfully develop its tablet formulation, three cocrystal systems of baicalein with isoniazid in a 1:1 molar ratio, with caffeine in a 2:1 molar ratio, and with nicotinamide in a 1:1 molar ratio were synthesized . All of these cocrystals showed significantly improved tabletability (Figure ), which is proposed to be attributed to the improved plastic deformation induced by parallel molecular layers connected through weak hydrogen bonds.…”