Baicalein (Bai) is one of the most important bioactive
flavonoids isolated from the well-known traditional Chinese medicine
called “Huang Qin”. Though it has broad therapeutic
capability, the bioavailability is limited due to its poor solubility.
In this study, we aimed to modulate its solubility through cocrystallization.
Cocrystals of Bai with isoniazide (Inia),
isonicotinamide (Inam), caffeine (Caf),
and theophylline (Tph) were obtained. And different cocrystallization
methods lead to different cocrystal phases for Inam and Tph. These cocrystals were characterized using powder X-ray
diffraction, thermogravimetric analysis, differential scanning calorimetry,
dynamic vapor sorption, and Fourier transform infrared spectroscopy.
Among all the cocrystals studied, BaiCaf is found to
be superior in powder dissolution and pharmacokinetic behavior. Area
under the curve values of BaiCaf is improved by a factor
of 4.1, and the bioavailability of baicalein is thus expected to be
accordingly increased. Given that Caf is a central nervous
system stimulant available in many prescription and nonprescription
medications, BaiCaf can be a promising alternative solid
form of Bai to be developed.
A four-membered square-shaped H-bonding structure was successfully designed to synthesize vitamin D3 co-crystals. The co-crystallization process was found to be conformationally selective to result in topochemically stable materials.
Drug-drug co-crystallization could realize combination drugs at a molecular level. Two polymorphic co-crystals between VD2 and VD3 were successfully designed and synthesized. These enantiotropic polymorphs exhibit significantly different physicochemical stabilities.
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