Cocrystal Construction Between Rosuvastatin Calcium and L-asparagine with Enhanced Solubility and Dissolution Rate

Vemuri, Venkata Deepthi; Srinivas, Leela

doi:10.4274/tjps.galenos.2021.62333

Cited by 4 publications

(2 citation statements)

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“…1-solublity and dissolution 1-Morphology SEM (Figure 3) scans revealed the change in the surface morphology of co-crystals compared to the pure EB and coformer . 6), while the major diffraction , the Asparagine peaks of 11.85°, 17.70°, 18.23°, 19.91°, 27.84°, and 43.15° ( 35) . Moreover the PXRD of EB2 showed a new intense peak at 2Ɵ of 12 o , (Figure 9) This result indicated the formation of new crystal lattice (34) .…”

Section: Figure (9) Pxrd Of Eb2mentioning

confidence: 99%

Amino Acid as Co-Crystal Coformer for Ebastine Solubility Enhancement

Salih¹,

Al-Khedairy²

2023

The Egyptian Journal of Hospital Medicine

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Background: Ebastine (EB) is a selective, nonsedating H1 antihistamine belonging to Class II(BCS); its insufficient water solubility limits its oral bioavailability. Cocrystal is one of the most modern techniques used to increase the solubility and dissolving rate of a medicine, among other physicochemical properties. Aim: The primary purpose of this study was to construct and assess EB cocrystal as an experiment to improve its solubility. Methods: Various processes, such as solvent evaporation and liquid asset grinding with varying molar ratios of amino acid as a co-former, have been used to produce cocrystals. The produced formulations were evaluated by yield %, drug content, saturation solubility, in vitro dissolution tests, Powder X-ray Diffraction (PXRD), and scanning electron microscopy. Results: Increased solubility by 364 times in distilled water with an improved dissolving profile. Conclusion: Due to its ability to enhance physicochemical and mechanical qualities, co-crystallization is a promising method for solid formation. Using unique hydrogen bond synthon motifs, co-crystals have been successfully produced from several medications and co-former

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Section: Figure (9) Pxrd Of Eb2mentioning

confidence: 99%

Amino Acid as Co-Crystal Coformer for Ebastine Solubility Enhancement

Salih¹,

Al-Khedairy²

2023

The Egyptian Journal of Hospital Medicine

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“…The absorption peaks that experienced changes in intensity and shift were the absorption peaks of the proton donor and acceptor groups of hydrogen bonds in the molecules of atorvastatin calcium and dipicolinic acid. Based on the results of the FTIR analysis it has been indicated that the atorvastatin calcium and dipicolinic acid molecules in the solids have formed intermolecular interactions, especially hydrogen bonds (Yaseen et al, 2017;Vemuri & Lankalapalli, 2021).…”

Section: Dsc Thermogrammentioning

confidence: 99%

Preparation of Atorvastatin Calcium-Dipicolinic Acid Multicomponent Solids by Liquid-Assisted Grinding Method to Increase Solubility

Wicaksono

Tsaniyah

Wisudyaningsih

et al. 2022

molekul

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Atorvastatin calcium is a cholesterol-lowering drug that is very potent but difficult to dissolve in water, so its bioavailability is low. In this study, atorvastatin calcium-dipicolinic acid multicomponent solids were prepared using the liquid-assisted grinding method to improve atorvastatin calcium's solubility. Characterization of multicomponent solids was carried out using powder x-ray diffraction (PXRD), differential scanning calorimetry (DSC), fourier transform infrared spectroscopy (FTIR), and scanning electron microscopy (SEM). Solubility test was carried out by shaking method using distilled water media. The results showed that the particles of atorvastatin calcium - dipicolinic acid multicomponent solids had an irregular shape with rough and porous surface topography. The multicomponent solids have a diffractogram with specific peaks of 2θ at 8.8, 9.9, 11.5, 16.7, 19.1, 21.2, 22.4, 23.4, and 27.7°. The DSC thermogram of multicomponent solids showed a sharp endothermic peak at 181.9 °C (∆H=17.69 J/g), indicating its melting point. The FTIR spectra of atorvastatin calcium-dipicolinic acid multicomponent solids indicated an intermolecular interaction that was thought to be a hydrogen bond between the molecules of atorvastatin calcium and dipicolinic acid. The results of the solubility test showed that the atorvastatin calcium-dipicolinic acid multicomponent solids had a significantly increased solubility (p<0.05) compared to the solubility of pure atorvastatin calcium.

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