Determination and correlation of solubility of efinaconazole in fifteen mono solvents and three binary mixed solvents at various temperatures

Lee, Seon-Kwang; Ha, Eun‐Sol; Jeong, Jisu; Kim, Sebin; Park, Heejun; Kim, Jeong-Soo; Yoo, Jin‐Wook; Moon, Hyung Ryong; Jung, Yunjin; Kim, Min‐Soo

doi:10.1016/j.molliq.2021.118148

Cited by 8 publications

(5 citation statements)

References 38 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Efinaconazole anti-fungal drug against onchomycosis, is a poorly soluble drug. It is being reported that efinaconazole is soluble in organic solvents (4) and has poor aqueous solubility, but using organic solvents in the formulation would worsen the discomfort of nails affected by onchomycosis. Purified neem gum has been proven to enhance the solubility of aceclofenac (3) and atorvastatin (12) .…”

Section: Discussionmentioning

confidence: 99%

“…(3) Efinaconazole is a triazole compound with anti-fungal activity, which belongs to BCS-II, it is poorly soluble or insoluble in water. (4) Onychomycosis, a nail infection primarily caused by dermatophytes, is treated topically with this antifungal medication. There are four approved classes of anti-fungal drugs for the treatment of onychomycosis: the allylamines, azoles, morpholines, and hydroxyl pyridinones.…”

Section: Introductionmentioning

confidence: 99%

See 1 more Smart Citation

Solubility Enhancement of Efinaconazole using Neem Gum and Evaluation of Antifungal Activity

Vaishnavi,

Reddy,

Bansal

et al. 2024

IJST

View full text Add to dashboard Cite

Objectives: Efinaconazole is an anti-fungal drug of BCS class II used for treating Onchomycosis. Neem gum known for its antifungal properties was purified and used as hydrophilic carrier. Solid dispersions by physical mixture and solvent evaporation method were prepared using purified Neem gum. Methods: The prepared solid dispersions in ratios 1:1, 1:3 and 1:6 were characterized for percentage yield, assay, solubility, and dissolution studies. The optimized solid dispersion SD6 was formulated as gel for ease of application. Gels were characterized for physico-chemical properties and in-vitro diffusion studies. The optimized gel was evaluated for anti-fungal activity. Findings: FTIR, DSC and XRD studies of optimized SD6 showed compatibility and amorphous nature respectively. G2 gel formulation containing SD6 solid dispersion showed 80.4±0.14% when compared to G1 56.76±0.34% release in 8hrs. Both the gels followed zero order and Higuchi release. Antifungal studies indicated more efficiency of G2 gel by zone of inhibition when compared with G1 containing only drug. G2 gel was found to be stable for one month. Novelty : In the present research work purified neem gum, which is natural carrier and neem known for its antifungal activity was used to enhance the solubility of drug and evaluate the antifungal activity of drug with purified neem gum. Conclusion: Hence it can be concluded, purified Neem gum can be used as hydrophilic carrier and as solubility of Efinaconazole was enhanced its antifungal activity was also increased. Keywords: Onchomycosis, Efinaconazole, Neem gum, Solid dispersions, Antifungal

show abstract

Section: Discussionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Solubility Enhancement of Efinaconazole using Neem Gum and Evaluation of Antifungal Activity

Vaishnavi,

Reddy,

Bansal

et al. 2024

IJST

View full text Add to dashboard Cite

show abstract

“…Apelblat and Manzurola put forward the modified Apelblat model according to the phase equilibrium theory, which is represented by a common empirical equation. This model was widely applied to correlate solubility with temperature. , ln nobreak0em0.25em⁡ x = A + B false( T / K false) + C 0.25em ln ( T / K ) In eq , x is the solubility of domiphen bromide in mono solvents, and A , B , and C are the three model parameters.…”

Section: Thermodynamic Modelsmentioning

confidence: 99%

Equilibrium Solubility of Domiphen Bromide in 12 Mono Solvents: Determination and Correlation

Shen,

Liu,

Yang

et al. 2024

J. Chem. Eng. Data

View full text Add to dashboard Cite

In this paper, the solubility of domiphen bromide in the range of 283.15−323.15 K was surveyed by the gravimetric method in 12 mono solvents of ethanol, N,, N,N-dimethylacetamide (DMA), N-methyl-2pyrrolidone (NMP), acetonitrile, and dimethyl sulfoxide (DMSO) at atmospheric pressure (0.1 MPa). The study results showed that the mole fraction solubility of domiphen bromide increased positively with increasing temperature. Among the selected 12 neat solvents, the solubility of domiphen bromide at 298.15 K followed the order 1-pentanol (0.1642) > n-butanol (0.1567) ≈ n-propanol (0.1572) ≈ ethanol (0.1569) > iso-butanol (0.1454) > iso-propanol (0.104515) > tert-butanol (0.08657) > NMP (0.05308) > DMF (0.04671) > DMSO (0.04505) > DMA (0.04156) > acetonitrile (0.009906). Thermodynamic models of the modified Apelblat model, the Yaws model, the Van't Hoff model, and the λh model were implemented to fit experimental solubility data of domiphen bromide, and the Yaws model yielded a relatively more accurate correlation result than the other three models by a comparison of the RAD and rmsd values. Experimental results would promote the separation and purification technology of drugs in the pharmaceutical industry.

show abstract

“…However, in pharmaceutical formulations, water is often combined with hydrophilic, non-aqueous solvents, one of which is ethanol [1,2]. In certain concentrations, ethanol can improve the solubility of hydrophobic drug substances [3,4] and ensure the efficacy of the antimicrobial preservative effect in liquid and semi-solid preparations [2,5].…”

Section: Introductionmentioning

confidence: 99%

“…Most scientific studies are dedicated to investigating the solubility of various active pharmaceutical substances in mixtures of water and ethanol. These include sulfadiazine, sulfamerazine and sulfamethazine [3], efinaconazole [4], urea [12], albendazole [19], zonisamide [20], baicalin [21], cefpiramide [22], 5-fluorouracil [23], and many others.…”

Section: Introductionmentioning

confidence: 99%

Study of the effect of ethanol on the properties of poloxamer 338 solutions by rotational viscometry and spin probe method

Liapunov,

Bezuglaya,

Liapunova

et al. 2024

ScienceRise: Pharmaceutical Science

View full text Add to dashboard Cite

The aim. Study the properties of 20 % solutions of poloxamer 338 (P338) in water and mixed solvents water-ethanol using rotational viscometry and the spin probe method at various temperatures. Materials and methods. 20 % m/m solutions of P338 in water and water – ethanol mixtures were the objects of research. The solutions were studied by rotational viscometry at various temperatures; the flow behaviour, lower yield stress (t0) and dynamic or apparent viscosity (η) were determined. Spin probes based on fatty acids, which differ in molecular structure, solubility, and radical localization, were added to the solutions. Electron paramagnetic resonance (EPR) spectra were obtained to determine their type and parameters. Results. Depending on the content, ethanol affects the rheological properties of 20 % solution of P338. The solution was demonstrated to be able to thermally induce sol → gel transition at 32 °C when ethanol content is 5 % m/m. The rheological parameters of the gel at 32 °C and 37 °C exhibit an increase (in comparison to the gel without ethanol), accompanied by a reduction in the packing density of polypropylene oxide (PPO) chains within the cores of P338 micelles. At an ethanol content of 10 % m/m, the gel formation temperature rises to 40 °C. At ethanol content of 15 % m/m and above, 20 % P338 solutions do not form gels at temperatures between 25 °C and 40 °C. The values of rotational correlation times (τ) and the order parameter (S) of fatty acid-based spin probes were observed to decrease with increasing ethanol content up to 30 % m/m; in the case of the ammonium salt of 5‑doxylstearic acid (5-DSA NH4 salt), the anisotropic EPR spectra transform, becoming a superposition of two triplets and subsequently a triplet. P338 solutions retain their ability to undergo thermally induced sol ↔ gel transitions as long as the EPR spectra of this probe exhibit anisotropy at temperatures ranging from 25 °C to 37 °C. As the concentration of ethanol in the solution increases, the solvation of the cores of P338 micelles by the dispersion medium of the solution also increases. Conclusions. It was demonstrated that ethanol, when added to the 20 % P338 solution, results in changes to the rheological properties of this solution. However, at the ethanol content of 5-10 % m/m, the ability of P338 to thermally induce sol → gel transition remains unaltered. The rheological properties of the 20 % P338 solution exhibit a correlation with the observed change in EPR spectra types for the 5-DSA NH4 salt. As the ethanol content in the solution increases, the solvation of P338 micelle cores by the dispersion medium increases, accompanied by decreased density and orderliness of the PPO chains packing in the micelle cores

show abstract

Determination and correlation of solubility of efinaconazole in fifteen mono solvents and three binary mixed solvents at various temperatures

Cited by 8 publications

References 38 publications

Solubility Enhancement of Efinaconazole using Neem Gum and Evaluation of Antifungal Activity

Solubility Enhancement of Efinaconazole using Neem Gum and Evaluation of Antifungal Activity

Equilibrium Solubility of Domiphen Bromide in 12 Mono Solvents: Determination and Correlation

Study of the effect of ethanol on the properties of poloxamer 338 solutions by rotational viscometry and spin probe method

Contact Info

Product

Resources

About