Experimental and thermodynamic study of solubility, partition and solvation of climbazole DOI
Svetlana V. Blokhina, Angelica Sharapova, Marina V. Ol’khovich

et al.

Journal of Thermal Analysis and Calorimetry, Journal Year: 2022, Volume and Issue: 147(21), P. 11977 - 11989

Published: June 28, 2022

Language: Английский

Synthesis of Ternary Cocrystals, Salts, and Hydrates of Acefylline with Enhanced Dissolution and High Permeability DOI
Suryanarayana Allu, Abhijit Garai, Владимир В. Чернышев

et al.

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

Investigation on the solvent and temperature effect of climbazole solubility DOI

Wenxi Song,

Na Wang, Mingzhe Tan

et al.

The Journal of Chemical Thermodynamics, Journal Year: 2023, Volume and Issue: 190, P. 107206 - 107206

Published: Nov. 15, 2023

Language: Английский

Citations

13

Development and Evaluation of Fluconazole Co-Crystal for Improved Solubility and Mechanical Properties DOI Creative Commons
Ritu Rathi, Inderbir Singh, Tanikan Sangnim

et al.

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

Colorful Prothionamide Salt Forms with Enhancement in Water Solubility and Dissolution Behavior DOI
Weijie Ji, Junyi Jiang, Minghuang Hong

et al.

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

Thermal method usage features for multicomponent crystal screening DOI
Denis E. Boycov, Alex N. Manin, Ksenia V. Drozd

et al.

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

Preparation and characterization of new salts of tioconazole. Comparison of their dissolution performance DOI
Aldana B. Moroni, Elena Pérez‐Mayoral, Diego F. Lionello

et al.

International Journal of Pharmaceutics, Journal Year: 2024, Volume and Issue: 652, P. 123855 - 123855

Published: Jan. 26, 2024

Language: Английский

Citations

1

Theoretical and experimental study of pharmaceutical salts: A case of Trimethoprim DOI
Liang Zhang, Di Wu, Menglong Zhang

et al.

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

Multi-component Crystal Strategy for Improving Water Solubility and Antifungal Activity of Climbazole DOI

Wenxi Song,

Na Wang,

Ao Li

et al.

Pharmaceutical Research, Journal Year: 2024, Volume and Issue: 41(8), P. 1737 - 1754

Published: July 29, 2024

Language: Английский

Citations

1

Characterization of the hydrochloride salt hemihydrate as a new salt of the antifungal agent tioconazole DOI
Aldana B. Moroni, Elena Pérez‐Mayoral, Diego F. Lionello

et al.

International Journal of Pharmaceutics, Journal Year: 2023, Volume and Issue: 637, P. 122869 - 122869

Published: March 21, 2023

Language: Английский

Citations

3

Two anhydrous forms and one monohydrate of a cocrystal of axitinib and glutaric acid: characterization, property evaluation and phase transition study DOI

Bo-Ying Ren,

Xia-Lin Dai, Jia‐Mei Chen

et al.

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