A series of stable, metastable and unstable salts of Imatinib with improved solubility

Fang, Zhengyu; Zhang, Baoxi; Xing, Wenhui; Jia, Huiying; Wang, Xue; Gong, Ningbo; Lü, Yang; Du, Guanhua

doi:10.1016/j.cclet.2021.10.056

Cited by 11 publications

(4 citation statements)

References 28 publications

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“…45,46 (2) In some GEF salts/cocrystals, GEF exists in the cation form, enhancing its hydrophilicity and facilitating its dissolution. 47 (3) Since all CCFs are weak acids and GEF dissolution exhibits pH dependency, 10 higher solubility of GEF is observed in acidic media. The equilibrium solubility of GEF, GEF–3-HBA, GEF–FA, GEF–4-HBA, GEF–35DNB, and GEF–SA was 4.0, 229.55, 35.71, 156.02, 64.25, and 340.50 μg mL −1 , respectively.…”

Section: Resultsmentioning

confidence: 99%

Gefitinib salts/cocrystals with phenolic acids as a promising solid-state approach to improve solubility

Zou,

Meng,

Zhang

et al. 2024

CrystEngComm

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Section: Resultsmentioning

confidence: 99%

Gefitinib salts/cocrystals with phenolic acids as a promising solid-state approach to improve solubility

Zou,

Meng,

Zhang

et al. 2024

CrystEngComm

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“…Solubility equilibrium is a type of dynamic equilibrium that exists when a chemical drug in the solid state is in chemical equilibrium with a solution of that compound . The cocrystal technique is used to increase the solubility of insoluble drugs and is one of the effective methods to increase their aqueous solubility. , To check whether the cocrystal technique improved the solubility of naringenin, we tested the solubility of NAR, NOR, and cocrystal 3 in pure water, phosphate buffer (pH = 6.8), and dilute hydrochloric acid solution (pH = 1.2) separately, and the results are shown in Figure .…”

Section: Resultsmentioning

confidence: 99%

Cocrystal of Naringenin and Norfloxacin: Crystal Transformation, Solubility, and Antibacterial and Anticancer Activities

Zeng,

Zheng,

Qiu

et al. 2024

Crystal Growth & Design

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Drug cocrystals can modulate the physical and chemical properties of drugs, even complement each other’s strengths, and have a synergistic enhancement effect. Here, we reported a drug cocrystal prepared by norfloxacin (NOR) and naringenin (NAR), comprising an antibacterial drug and an antitumor active pharmaceutical ingredient. The cocrystal hydrate obtained by crystal transformation methods enhanced the antibacterial activity of NOR against one Gram-positive bacterium (Staphylococcus aureus), three Gram-negative bacteria (Escherichia coli, Dysentery bacillus, Pseudomonas aeruginosa), and one fungus (Candida albicans), improved the solubility of NAR, reduced the hygroscopicity of NOR, and enhanced the anticancer activity of NAR against human breast cancer cells MDA-MB-231. This combination has potential therapeutic synergy in clinical terms.

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“…Cocrystals and salts are long-known multi-component crystalline assemblies and have been attracting expanding interest among pharmaceutical scientists [17][18][19][20]. Cocrystals and/or salts are solids composed of two or more different molecular and/or ionic compounds in a definite stoichiometric ratio, and the difference is whether there is a proton transfer process [21,22].…”

Section: Introductionmentioning

confidence: 99%

Enhancing Solubility and Dissolution Rate of Antifungal Drug Ketoconazole through Crystal Engineering

Yu,

Zhang,

Liu

et al. 2023

Pharmaceuticals

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To improve the solubility and dissolution rate of the BCS class II drug ketoconazole, five novel solid forms in 1:1 stoichiometry were obtained upon liquid-assisted grinding, slurry, and slow evaporation methods in the presence of coformers, namely, glutaric, vanillic, 2,6-dihydroxybenzoic, protocatechuic, and 3,5-dinitrobenzoic acids. Single-crystal X-ray diffraction analysis revealed that the hydroxyl/carboxylic acid. . .N-imidazole motif acts as the dominant supramolecular interaction in the obtained solid forms. The solubility of ketoconazole in distilled water significantly increased from 1.2 to 2165.6, 321.6, 139.1, 386.3, and 191.7 μg mL−1 in the synthesized multi-component forms with glutaric, vanillic, 2,6-dihydroxybenzoic, protocatechuic, and 3,5-dinitrobenzoic acid, respectively. In particular, the cocrystal form with glutaric acid showed an 1800-fold solubility increase in water concerning ketoconazole. Our study provides an alternative approach to improve the solubility and modify the release profile of poorly water-soluble drugs such as ketoconazole.

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A series of stable, metastable and unstable salts of Imatinib with improved solubility

Cited by 11 publications

References 28 publications

Gefitinib salts/cocrystals with phenolic acids as a promising solid-state approach to improve solubility

Gefitinib salts/cocrystals with phenolic acids as a promising solid-state approach to improve solubility

Cocrystal of Naringenin and Norfloxacin: Crystal Transformation, Solubility, and Antibacterial and Anticancer Activities

Enhancing Solubility and Dissolution Rate of Antifungal Drug Ketoconazole through Crystal Engineering

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