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.
関連文献
Interlayer coupling in two-dimensional titanium carbide MXenes
Chao Zhang, Jingyang Wang, Xiaohui Wang
DOI: 10.1039/C6CP01699E
Topography evolution of 500 keV Ar4+ ion beam irradiated InP(100) surfaces – formation of self-organized In-rich nano-dots and scaling laws
Indra Sulania, Dinesh C. Agarwal, Manish Kumar, Sunil Kumar, Pravin Kumar
DOI: 10.1039/C6CP03409H
Sunlight as an energetic driver in the synthesis of molecules necessary for life
Rebecca J. Rapf, Veronica Vaida
DOI: 10.1039/C6CP00980H
Free energy of solvation of carbon nanotubes in pyridinium-based ionic liquids
Vitaly V. Chaban, Eudes Eterno Fileti
DOI: 10.1039/C6CP03497G
Transition from exohedral to endohedral structures of AuGen− (n = 2–12) clusters: photoelectron spectroscopy and ab initio calculations
Sheng-Jie Lu, Lian-Rui Hu, Xi-Ling Xu, Hong-Guang Xu, Hui Chen, Wei-Jun Zheng
DOI: 10.1039/C6CP00373G
The unique Raman fingerprint of boron nitride substitution patterns in graphene
Marco Lorenz, Daniele Pullini, Mauro Sgroi
DOI: 10.1039/C6CP02101H
Photochemistry of nitrate chemisorbed on various metal oxide surfaces
Daniel M. B. Lesko, Ellen M. Coddens, Hannah D. Swomley, Rachel M. Welch, Jaya Borgatta, Juan G. Navea
DOI: 10.1039/C5CP02903A
Excited states in large molecular systems through polarizable embedding
Nanna Holmgaard List, Jógvan Magnus Haugaard Olsen, Jacob Kongsted
DOI: 10.1039/C6CP03834D
Hydrogen-doping induced reduction in the phase transition temperature of VO2: a first-principles study
Yuanyuan Cui, Lanli Chen, Yanfeng Gao
DOI: 10.1039/C5CP03267A
Relationships between the solution and solid-state properties of solution-cast low-k silica thin films
Chao-Ching Chiang, Chien-You Su, An-Chih Yang, Ting-Yu Wang, Wen-Ya Lee, Chi-Chung Hua, Dun-Yen Kang
DOI: 10.1039/C6CP04166C
こちらもおすすめ
1-{3-[5-(エチルカルボンイル)-2,4-ジメチル-1H-ピロロール-3-基]プロパニル}ピペリジン-4-カルボン酸について、適用される法規ガイドラインは何ですか?
この化合物はCAS番号1142209-81-1であり、GHS分類では corrosive (腐食性物質) と classified (分類物質) として指定され...
2,2-二氟-1,3-ベンゾジオキサン-5-カルボキシlic酸とは何ですか?
2,2-二氟-1,3-ベンゾジオキサン-5-カルボキシlic酸は、CAS番号656-46-2の化合物で、化学式はC8H4F2O4です。この化合物は白色の結晶性粉...
8-氯-4-色原酮の代替品はありますか?
8-氯-4-色原酮(CAS番号: 49701-11-3)の代替品には、他の色原酮類似物や、構造が似ている化合物があります。例えば、8-メチル-4-色原酮や、他の...
エチル6,6-ジメチル-4,5,6,7-テトラヒドロ-1H-インドアゼー-3-カルボキシレートとは何ですか?
エチル6,6-ジメチル-4,5,6,7-テトラヒドロ-1H-インドアゼー-3-カルボキシレートは、CAS番号1233243-56-5を有する化合物です。これは有...
4-叔丁基-6-氯-嘧啶に適用される法規ガイドラインは何ですか?
4-叔丁基-6-氯-嘧啶はCAS番号3435-24-3で、GHS分類では毒性物質とみなし、GHSの危険性分類が適用されます。REACH規則では登録が必要で、Eu...
維库溴铵杂质Bはどのように合成されますか?
維库溴铵杂质Bは、アンドロステンデンから始まり、一連の合成反応、包括的な選択性と高い収率で合成されます。具体的には、ブロミド化、酸化、ジマーゼ反応、アミド化など...
2-(4-氟苄基)-吡咯烷の物理化学的性質は何ですか?
CAS番号350017-04-8の2-(4-氟苄基)-吡咯烷は、結晶性の白色粉末です。分子量は199.17 g/molで、水に溶けにくいです。化学反応では比較的...
3-喹啉甲醛(2-チロール-8-エチル)は安全ですか?
3-喹啉甲醛(2-チロール-8-エチル)は一定の毒性を持つため、取扱には注意が必要です。使用する際は適切な防護具を着用し、密閉容器で保管・搬送し、直接的な接触を...
エチル3-(ヒドロキシメチル)-1H-ピロール-2-カルボキシレートはどのように保存すればよいですか?
エチル3-(ヒドロキシメチル)-1H-ピロール-2-カルボキシレートは、室温(25℃)以下で保存し、直射日光を避け、乾燥した環境で保管することが推奨されます。ま...
掲載誌
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.














