Multicomponent Crystal of Trimethoprim and Citric Acid: Solid State Characterization and Dissolution Rate Studies

Umar, Salman; Farnandi, Rido; Salsabila, Hulwa; Zaini, Erizal

doi:10.3889/oamjms.2022.7920

Cited by 3 publications

(3 citation statements)

References 23 publications

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“…The thermodynamic changes occur when a substance heated or cooled is used to analyze thermal properties. The change in the melting point of the binary mixture of the active pharmaceutical ingredients and coformer likely indicates the presence of solid-state interactions [27].…”

Section: Differential Scanning Calorimetry Analysismentioning

confidence: 99%

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Formation and Characterization of Multicomponent Crystal of Trimethoprim and Mandelic Acid by Solvent Drop Grinding Method

et al. 2023

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Objective: To increase the solubility of trimethoprim by forming multicomponent crystals using mandelic acid as a coformer. Methods: Multicomponent crystals of trimethoprim and mandelic acid were prepared at a ratio of 1:1 mol by the Solvent Drop Grinding (SDG) method. Solid state characterization was carried out using Differential Scanning Calorimetry (DSC), Powder X-ray Diffraction (PXRD), Fourier Transform Infrared (FTIR) spectroscopy, Scanning Electron Microscope (SEM), and polarized microscope. The solubility test of trimethoprim was carried out in CO2-free distilled water using a sonicator for 5 min and then determined by High-Performance Liquid Chromatography (HPLC) using acetonitrile and phosphoric acid in a 10:90 ratio as the mobile phase and octadecylsilane (C18) as the stationary phase. Results: The results showed a decrease in the melting point and enthalpy of fusion on the DSC thermogram, a new peak in the X-ray diffraction pattern, and a slight shift of wave number in the FTIR spectroscopy. Those characterizations indicated that the multicomponent crystal formed a salt type. SEM analysis showed morphological changes and formation of new crystal habits. The polarization microscopy analysis showed birefringent with various colors in all samples. The solubility of multicomponent crystal is 2.73-times higher compared to intact trimethoprim. Conclusion: The formation of cocrystals of trimethoprim and mandelic acid by SDG method increased the solubility of trimethoprim.

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Section: Differential Scanning Calorimetry Analysismentioning

confidence: 99%

“…In this study, mandelic acid has high solubility in water that is estimated affect the increase in the solubility trimethoprim multicomponent crystals. The multicomponent crystals tend to be more hydrophilic and have better affinity in water, thus salt-based compounds will split into cationic and anionic ions [27].…”

Section: Solubility Testmentioning

confidence: 99%

Formation and Characterization of Multicomponent Crystal of Trimethoprim and Mandelic Acid by Solvent Drop Grinding Method

et al. 2023

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“…The presence of chemical interactions between glibenclamide and hydroxypropyl-β-cyclodextrin in the inclusion complex was indicated by the presence of a new transmittance peak or a shift. The presence of hydrogen bonds formed between two solids is indicated by a shift in wave number [21], namely the interaction between the carbonyl group of glibenclamide and the hydroxyl group of hydroxypropyl-β-cyclodextrin.…”

Section: Mol Inclusion Complex (D) 1:2 Mol Inclusion Complexmentioning

confidence: 99%

Characterization and Dissolution Rate Studies of Inclusion Complex of Glibenclamide and Hydroxypropyl-Β-Cyclodextrin Using Co-Grinding Method

Fadhila¹,

HALIM²,

ASSYIFA³

2022

Int J App Pharm

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Objective: Glibenclamide belongs to the 2nd generation sulfonylurea group as an oral antidiabetic with low solubility in water and high bioavailability in systemic circulation (Biopharmaceutical Classification System class II). This study aimed to increase the solubility and dissolution rate of glibenclamide by preparing an inclusion complex of Glibenclamide and Hydroxypropyl-β-cyclodextrin. Methods: Inclusion complexes were prepared by the co-grinding method in two ratios 1:1 and 1:2 mol. Characterizations of inclusion complex were carried out by Scanning Electron Microscopy (SEM), Fourier Transform Infrared (FT-IR) spectroscopy, Differential Scanning Calorimetry (DSC), X-ray Diffraction (XRD) analysis. Solubility test was carried out in CO2-free distilled water and dissolution rate was carried out in phosphate buffer pH 7.4. Results: The results of the SEM analysis showed changes in particle morphology. FT-IR spectroscopy shows a shift in wavenumber. DSC analysis showed a decrease in the melting point of the inclusion complex. XRD characterization results showed a decrease in the intensity of the inclusion complex. Solubility of inclusion complex of glibenclamide increased nine times 1:1 mol inclusion complex, twelve times 1:2 mol inclusion complex compared to intact glibenclamide. The dissolution of glibenclamide, inclusion complex 1:1, and inclusion complex 1:2 in phosphate buffer pH 7.4 medium at 60 min was 17.19%, 34.15% and 52.83% respectively. Conclusion: Based on the results of the study, it can be said that the glibenclamide inclusion complex with Hydroxypropyl-β-cyclodextrin successfully increases the solubility and dissolution rate of glibenclamide significantly.

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Preparation of Spray-Dried Multicomponent Crystals of Trimethoprim-Mandelic Acid and Its Physicochemical Characterization

FITRIANI,

SHINTANIA,

USMAN

et al. 2024

Int J App Pharm

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Objective: Trimethoprim is a wide-spectrum antimicrobial compound belonging to Class II of the Biopharmaceutics Classification System (BCS), with high permeability but low solubility. This study aimed to prepare a multicomponent crystal (MCC) of trimethoprim-mandelic acid to enhance the solubility of trimethoprim. Methods: MCC trimethoprim–mandelic acid was prepared by spray drying technique. Solid-state characterizations were performed by using PowX-ray diffraction (PXRD), Differential Scanning Calorimetry (DSC), Fourier-transform infrared (FT IR) spectroscopy, Scanning Electron Microscopy (SEM), and polarized microscopy. The solubility test was performed in distilled water. The amount of dissolved trimethoprim was analyzed by High-Performance Liquid Chromatography (HPLC) using acetonitrile and phosphoric acid 1 % (10:90 v/v) as the mobile phase. Results: MCC characterizations showed a different diffraction pattern from its intact materials according to PXRD analysis, a decrease in the melting point in the DSC thermogram, a shift of the wave number in the FT-IR spectra, and a new crystalline habit compared to the intact materials was presented by SEM analysis. The MCC also showed the color of interference under polarized microscopy, indicating the crystalline phase. The solubility of trimethoprim in MCC increased significantly by 3.98 times in comparison to intact trimethoprim. Conclusion: The MCC trimethoprim-mandelic acid by spray drying technique enhanced the solubility of trimethoprim.

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Multicomponent Crystal of Trimethoprim and Citric Acid: Solid State Characterization and Dissolution Rate Studies

Cited by 3 publications

References 23 publications

Formation and Characterization of Multicomponent Crystal of Trimethoprim and Mandelic Acid by Solvent Drop Grinding Method

Formation and Characterization of Multicomponent Crystal of Trimethoprim and Mandelic Acid by Solvent Drop Grinding Method

Characterization and Dissolution Rate Studies of Inclusion Complex of Glibenclamide and Hydroxypropyl-Β-Cyclodextrin Using Co-Grinding Method

Preparation of Spray-Dried Multicomponent Crystals of Trimethoprim-Mandelic Acid and Its Physicochemical Characterization

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