2023 Volume 71 Issue 5 Pages 326-333
This review highlights the cocrystals of active pharmaceutical ingredients (APIs) derived from traditional Chinese medicines (TCMs) in categories, ∆pKa rule, preparation, characterization, and physicochemical properties, reported in 113 literature reports. It is founded that the formation of all of the cocrystals is in accordance with ∆pKa rule. Three preparation methods such as evaporation cocrystallization, grinding method, and suspension method, are used most, accounting for 44, 27, and 16%, respectively. Almost all cocrystals are characterized by powder X-ray diffraction (PXRD). Thermal analysis techniques are used for 81% of cocrystals, and more than half of cocrystals are characterized by IR. Forty-four percent of cocrystals are determined by single crystal X-ray diffraction (SXRD) since it is difficult to get the single crystals of cocrystals. Most cocrystals of APIs in TCMs exhibit 1–10 folds enhancement in solubility, dissolution, dissolution rate, and bioavailability, and a few of them are increased by dozens or even hundreds of times in these properties. This review provides a meaningful reference for more and more APIs in TCMs prepared for pharmaceutical cocrystals in future.
