Journal of Thermal Analysis and Calorimetry, Год журнала: 2022, Номер 147(21), С. 11977 - 11989
Опубликована: Июнь 28, 2022
Язык: Английский
Crystal Growth & Design, Год журнала: 2022, Номер 22(7), С. 4165 - 4181
Опубликована: Июнь 8, 2022
Acefylline (ACF) is a stimulant xanthine derivative drug, which formulated as piperazine salt for the treatment of bronchial asthma. ACF falls under BCS class IV category low solubility and poor permeability, together limit bioavailability efficacy drug. In this work, binary ternary cocrystals, salts–cocrystals, their polymorphs are synthesized by cocrystallization with several coformers. Two different methods were adopted supramolecular assembly systems A.B.C: (1) first, adducts A.B or A.C crystallized grinding slurry components in suitable solvent then C was added continued; (2) all three taken ground together. The former method found to be superior affording salt/cocrystal. role laboratory seeding implicated explain variation crystallization results at stages project. Crystal structures product's solved single-crystal X-ray diffraction powder data structure solution. crystal show recurrence carboxylate–pyridinium imidazole–acid heterosynthons adducts. intermolecular interactions between coformer analyzed Hirshfeld surfaces, 2D fingerprint plots, an energy framework. permeability increases selected fast dissolution high ACF-PIP make improved crystalline formulation acefylline.
Язык: Английский
Процитировано
24
The Journal of Chemical Thermodynamics, Год журнала: 2023, Номер 190, С. 107206 - 107206
Опубликована: Ноя. 15, 2023
Язык: Английский
Процитировано
13
Pharmaceutics, Год журнала: 2025, Номер 17(3), С. 371 - 371
Опубликована: Март 14, 2025
Background: Fluconazole (FLZ) is a broad-spectrum anti-fungal drug presenting poor flowability, mechanical properties, and limited aqueous solubility. These issues pose challenges for the handling manufacturing of dosage forms FLZ. The current research aimed to develop fluconazole co-crystal (CC) improving its solubility, properties. (2) Methods: benzoic acid (FLZ-BA) was prepared using solvent evaporation technique. characterized content, activity, dissolution, stability. DSC (Differential Scanning Calorimetry), PXRD (Powder X-Ray Diffraction), SEM (Scanning Electron Microscopy), FTIR (Fourier Transmission Infrared) spectroscopy were carried out confirm formation. further evaluated their flow characteristics properties via CTC (compressibility, tabletability, compactibility), Heckel, Kawakita analysis. (3) Results: CC showed 69.51% content 13-fold greater solubility than pure thermogram sharp endothermic peak between parent components, distinct pattern observed, analysis revealed different morphology, confirming formation (new crystalline form). immediate release found more stable, less hygroscopic FLZ alone. better tabletability (tensile strength), compressibility, compactibility. Moreover, Heckel indicated deform plastically, favoring improved compression. (4) Conclusions: capabilities, stability, antifungal flowability make FLZ-BA suitable candidate preparation an form. study also application
Язык: Английский
Процитировано
0
Crystal Growth & Design, Год журнала: 2023, Номер 23(8), С. 5770 - 5784
Опубликована: Июль 3, 2023
Prothionamide (PRT) is used as an alternative to some first-line drugs in the treatment of multi drug-resistant tuberculosis. Suffering from its extremely low water solubility and physiological constraints, clinical use PRT restricted. The crystal engineering technique has been proven be a good way improve solubility, especially for salt formation. In this work, six colorful salts, i.e., maleate, besylate, tosylate, phthalate, edisylate, naphthalene disulfonate, were obtained first time identified with solid-state characterization methods. Hirshfeld surface independent gradient model based on partition calculation study weak interactions constitutions. With different counterions added into unit cell bonded cations through N+–H···O– hydrogen interactions, tremendous enhancement dissolution behavior was observed all salts when compared PRT. Solvation free energy lattice calculated rationalize increase values. Different colors exhibited studied detail molecular orbital caculation visualization technique. exploration landscape forms increased performance highly promising application tuberculosis treatment.
Язык: Английский
Процитировано
6
Pharmaceutical Research, Год журнала: 2024, Номер 41(8), С. 1737 - 1754
Опубликована: Июль 29, 2024
Язык: Английский
Процитировано
2
CrystEngComm, Год журнала: 2022, Номер 24(12), С. 2280 - 2290
Опубликована: Янв. 1, 2022
In this work, the effectiveness of thermal methods, liquid-assisted grinding, and crystallization by a slow evaporation technique for screening multicomponent crystals five quinolones with tyramine was investigated.
Язык: Английский
Процитировано
8
International Journal of Pharmaceutics, Год журнала: 2024, Номер 652, С. 123855 - 123855
Опубликована: Янв. 26, 2024
Язык: Английский
Процитировано
1
CrystEngComm, Год журнала: 2024, Номер 26(28), С. 3808 - 3822
Опубликована: Янв. 1, 2024
Virtual screening of pharmaceutical salts by the conductor-like model for realistic solvents (COSMO-RS) method to improve water solubility trimethoprim (TMP).
Язык: Английский
Процитировано
1
International Journal of Pharmaceutics, Год журнала: 2023, Номер 637, С. 122869 - 122869
Опубликована: Март 21, 2023
Язык: Английский
Процитировано
3
CrystEngComm, Год журнала: 2022, Номер 24(11), С. 2138 - 2148
Опубликована: Янв. 1, 2022
Two anhydrous forms and one monohydrate of a cocrystal axitinib glutaric acid were obtained, investigation their phase transition relationship as well characterization property evaluation was carried out.
Язык: Английский
Процитировано
5