A novel drug–drug cocrystal of tegafur and myricetin: optimized properties of dissolution and tabletability
文献情報
Min Zhang, Dai-Lin Gu, Jian-Feng Zhen, Tong-Bu Lu, Xia-Lin Dai, Jia-Mei Chen
Tegafur (TGF) is a broad-spectrum anti-tumor drug, but it suffers from fast metabolism and consequently poor oral absorption. Myricetin (MYR) is a flavonoid with anti-tumor activity and it has the potential to reverse the TGF resistance, but exhibits poor solubility and low oral bioavailability. In order to simultaneously optimize the physicochemical properties of TGF and MYR, and provide a solution for constructing a fixed-dose combination with better performance, a drug–drug cocrystal (TGF–MYR) was synthesized and comprehensively characterized. The cocrystal effectively improves the dissolution performance of MYR and delays the drug release of TGF, which is beneficial for reducing their solubility difference and improving the formulation compatibility. Moreover, the cocrystal demonstrates significantly improved tabletability compared to pure TGF and is less hygroscopic than pure MYR, as well as having good stability, which indicated there were good prospects for the development of TGF and MYR combined formulations in the future.
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CrystEngComm

CrystEngComm is the forum for the design and understanding of crystalline materials. We welcome studies on the investigation of molecular behaviour within crystals, control of nucleation and crystal growth, engineering of crystal structures, and construction of crystalline materials with tuneable properties and functions. We publish hypothesis-driven research into… how crystal design affects thermodynamics, phase transitional behaviours, polymorphism, morphology control, solid state reactivity (crystal-crystal solution-crystal, and gas-crystal reactions), optoelectronics, ferroelectric materials, non-linear optics, molecular and bulk magnetism, conductivity and quantum computing, catalysis, absorption and desorption, and mechanical properties. Using Techniques and methods including… Single crystal and powder X-ray, electron, and neutron diffraction, solid-state spectroscopy, spectrometry, and microscopy, modelling and data mining, and empirical, semi-empirical and ab-initio theoretical evaluations. On crystalline and solid-state materials. We particularly welcome work on MOFs, coordination polymers, nanocrystals, host-guest and multi-component molecular materials. We also accept work on peptides and liquid crystals. All papers should involve the use or development of a design or optimisation strategy. Routine structural reports or crystal morphology descriptions, even when combined with an analysis of properties or potential applications, are generally considered to be outside the scope of the journal and are unlikely to be accepted.