【摘 要】
：
As a promising new solid form, cocrystal has been increasingly drawn more attention to improve pharmaceutical properties of active pharmaceutical ingredients (API) including solubility, dissolution ro
【机 构】
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State Key Laboratory of Quality Research in Chinese Medicine, Institute of Chinese Medical Sciences,
【出 处】
：
第二届全国生物颗粒学术研讨会、第三届国际工业药学和临床药学研讨会暨第一届岭南国际药学大会
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As a promising new solid form, cocrystal has been increasingly drawn more attention to improve pharmaceutical properties of active pharmaceutical ingredients (API) including solubility, dissolution rote and bioavailability.In this study, GEN and ISO are selected as the API and cocrystal former (CCF) respectively to discover the new cocrystal system with stoichiometric diversity.GEN belongs to the isoflavones, which has demonstrated good anti-oxidant, anti-inflammatory, anti-bacterial and anti-tumour activities.As a biopharmaceutical classification system class Ⅱ agent, the low solubility hindered clinical application of GEN.Differential calorimetric scanning (DSC) was used to screen cocrystals prepared by liquid assisted grinding.Compared to the thermal profiles of the physical mixture of GEN and ISO, a new peak with the melting temperature of ~220℃ could be observed using GEN to ISO at 1∶1 molar ratio, which is different from the cocrystal previously reported at 1∶2 molar ratio.However, no pure 1∶1 cocrystal could be synthesized by liquid assisted, neat assisted, fast evaporation, slow evaporation, or microwave irradiation method.Using polymer assisted grinding (POLAG), powder X-ray diffraction (PXRD) results showed that the intensity of the cocrystal characteristic peaks enhanced significantly,which may be due to that the additive polymer modified the cocrystallization rate and therefore enhanced the formation and purity of 1∶1 GEN-ISO cocrystal.Financial support from the Macao Science and Technology Development Fund (112/2013/A3) is gratefully acknowledged.
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