Journal of Thermal Analysis and Calorimetry, Journal Year: 2022, Volume and Issue: 147(21), P. 11977 - 11989
Published: June 28, 2022
Language: Английский
Crystal Growth & Design, Journal Year: 2022, Volume and Issue: 22(7), P. 4165 - 4181
Published: June 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.
Language: Английский
Citations
24
The Journal of Chemical Thermodynamics, Journal Year: 2023, Volume and Issue: 190, P. 107206 - 107206
Published: Nov. 15, 2023
Language: Английский
Citations
13
Pharmaceutics, Journal Year: 2025, Volume and Issue: 17(3), P. 371 - 371
Published: March 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
Language: Английский
Citations
0
Crystal Growth & Design, Journal Year: 2023, Volume and Issue: 23(8), P. 5770 - 5784
Published: July 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.
Language: Английский
Citations
6
Pharmaceutical Research, Journal Year: 2024, Volume and Issue: 41(8), P. 1737 - 1754
Published: July 29, 2024
Language: Английский
Citations
2
CrystEngComm, Journal Year: 2022, Volume and Issue: 24(12), P. 2280 - 2290
Published: Jan. 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.
Language: Английский
Citations
8
International Journal of Pharmaceutics, Journal Year: 2024, Volume and Issue: 652, P. 123855 - 123855
Published: Jan. 26, 2024
Language: Английский
Citations
1
CrystEngComm, Journal Year: 2024, Volume and Issue: 26(28), P. 3808 - 3822
Published: Jan. 1, 2024
Virtual screening of pharmaceutical salts by the conductor-like model for realistic solvents (COSMO-RS) method to improve water solubility trimethoprim (TMP).
Language: Английский
Citations
1
International Journal of Pharmaceutics, Journal Year: 2023, Volume and Issue: 637, P. 122869 - 122869
Published: March 21, 2023
Language: Английский
Citations
3
CrystEngComm, Journal Year: 2022, Volume and Issue: 24(11), P. 2138 - 2148
Published: Jan. 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.
Language: Английский
Citations
5