Enhancement of nalidixic acid solubility via cosolvency and solid dispersion

Tous, S. Shawky; Sayed, A.M. El; Mohsen, Mirzaei; Agban, Michael N.; Boushra, M.F.

doi:10.1016/s1773-2247(12)50057-2

Cited by 9 publications

(6 citation statements)

References 21 publications

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“…From this, it can be concluded that the solubility with reference in the case of methanol and ethanol was higher in methanol. Similar results are reported regarding the solubility of the anti-inflammatory drug celecoxib, which contains heteroatoms in its structure, for which a higher solubility in methanol than that in ethanol was found, this solubility being influenced by the aforementioned 14,21 .…”

Section: Resultssupporting

confidence: 86%

“…It should be noted that the polarity of the solvent is a function of the solubilization capacity 12 , this means that the solubility presented in practical terms should be greater in the smallest amount of the polar solvent. This characteristic may be due to the presence of the particular solvent and also to their ability to form hydrogen bonds with the heteroatoms of the drug 21 . From this, it can be concluded that the solubility with reference in the case of methanol and ethanol was higher in methanol.…”

Section: Resultsmentioning

confidence: 99%

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Effect of Solvent Behavior of Nalidixic Acid by Ultraviolet Spectroscopy

Muñoz¹,

Palacio²,

Rivas³

2020

J. Chil. Chem. Soc.

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One of the most widely used pharmaceuticals of the antibiotic type is quinolones. Nalidixic acid belongs to this family of antibiotics and it is widely used in both human and veterinary medicine. The main objective of this work is to show the behavior of nalidixic acid in co-solvent mixtures, in order to study soon the removal of this antibiotic in aqueous solutions or mixtures of water with solvents. The study was carried out by preparing a standard solution containing 25 mg of nalidixic acid in 50 mL in different solvent mixtures. Subsequently, 20 mg L-1 solutions were prepared using the same mixture of solvents (acetone: water, methanol: water and ethanol: water) to be scanned for wavelengths by UV-Vis spectroscopy. The spectra showed signal displacement in all the mixtures when there was an increase concerning to the water contents due to the interaction of the water with the acid group of the antibiotic. While in mixtures of methanol: water and ethanol: water solutions, there is a variation of the absorption band intensities. As a conclusion, it can be said that it is important to consider the solubility capacity of this antibiotic in different solvents for the purposes of removal studies of this type of emerging contaminants of the antibiotic type.

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Section: Resultssupporting

confidence: 86%

Section: Resultsmentioning

confidence: 99%

Effect of Solvent Behavior of Nalidixic Acid by Ultraviolet Spectroscopy

Muñoz¹,

Palacio²,

Rivas³

2020

J. Chil. Chem. Soc.

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“…This might have somehow attributed to a reduction in particle size and an upsurge in the surface area thus resulting in a better dissolution rate. 46 From cumulative percent of drug release pattern, among the PMs, F4 and F8 gave better drug release percent but S4 and S8 had given the best cumulative percent of drug release after 60 minutes (Figure 2c). Increasing the concentration of KIR and KF90 upturn the solubility of RVT both in PMs and SDs.…”

Section: Resultsmentioning

confidence: 94%

Evaluation of in vitro Dissolution Profile and Physicochemical Characterization of Polymer Based Formulations of Sparingly Soluble Rosuvastatin

Sikdar

Nazir

Alam

et al. 2021

Dhaka Univ. J. Pharm. Sci

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Rosuvastatin (RVT) is a BCS class II antilipidemic crystalline drug, which exhibits low bioavailability due to its very poor aqueous solubility; therefore, it is challenging to develop a proper formulation of RVT. To enhance solubility and bioavailability of this API, an attempt has been made by implementing solid dispersion technique. Solid dispersion (SD) technique is a solubility enhancing technique where one or more active entities are dispersed in an inert medium (matrix or carrier) at solid state. In this study, different ratios of Kollicoat® IR (KIR) and Kollidon® 90F (KF90) polymers were used with API to prepare various formulations by physical mixing (PM) and SD approaches; here solvent evaporation technique was used whereas methanol was used as solvent which was completely evaporated from the homogenously dispersed system by placing in a water-bath at 60-65°C and then in oven for 30 minutes at 50 °C. Among the formulations, RVT-KF90 SD formulations showed the most promising result in in-vitro study in terms of drug release profile (78.04 – 99.21%) in comparison to pure RVT (63.1%) and physical mixing of RVT with those polymers. USP dissolution apparatus type II was used at 37°C ± 0.5°C with 50 rpm to conduct the in-vitro experiment. The experiment also unraveled that the dissolution of RVT improved with increasing the amounts of polymers. Subsequently, stability of the developed formulations was conducted by Fourier transforms infrared spectroscopy (FTIR) and differential scanning calorimetry (DSC) as well as scanning electron microscopy (SEM). The results obtained from FTIR ensured no involvement of any significant drug-excipient interaction. Moreover, the DSC study signified thermal stability at high temperature. Besides, the SEM micrograph illustrated homogenous distribution of RVT in the polymer and transformation of crystal-like RVT into amorphous formulations. Dhaka Univ. J. Pharm. Sci. 20(2): 199-211, 2021 (December)

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“…Despite its high potency as antibacterial agents, nalidixic acid has already limited solubility in water. 648 Therefore, it comes as no surprise that the MIC value determination of the light-controlled derivatives had to be performed at low concentrations (64 μg mL −1 ) due to solubility restrictions. 647 In another study, using photoswitchable hydantoin 649 and phytochrome, 650 it was shown that the limiting water-solubility can be improved by transforming the carboxylic acids to sodium salts ( Fig.…”

Section: Illustrative Examples Of Photoswitches In Aqueous Mediamentioning

confidence: 99%