Thermodynamic solubility determination of khellin in eight mono-solvents at the range of 298.15 to 323.15 K

Shah, Raj P.; Bharate, Sonali S.

doi:10.1016/j.molliq.2022.118637

Cited by 6 publications

(3 citation statements)

References 32 publications

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“…The quantification of khellin was performed as per the UV-Visible spectrophoto-metric method reported by us previously. [31] Briefly, the drug was dissolved in methanol, and further dilutions of 20 and 40 μg/mL were obtained. The λ max of the resulting solutions was found to be 250 nm; however, the analysis was performed at 330 nm.…”

Section: Uv-visible Spectrophotometric Analysis Of Khellinmentioning

confidence: 99%

“…We investigated khellin polymorphs as critical information under the 'Chemistry Manufactring and Control (CMC)' section. [31] Furthermore, we developed amorphous solid dispersions of khellin with PEG 4000 to improve its solubility, thereby, dissolution performance. [24] In continuation with our efforts on this unique natural product, herein, our study hypothesis is to enhance the solubility and oral bioavailability of khellin by preparing SEDDS formulations.…”

Section: Introductionmentioning

confidence: 99%

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Self‐Emulsifying Drug Delivery of Khellin for Improving Its Oral Bioavailability

Shah,

Wazir,

Nandi

et al. 2023

ChemistrySelect

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Self‐emulsifying drug delivery system (SEDDS) is extensively used for enhancing the solubility, dissolution, and pharmacokinetics of poorly soluble drugs. Khellin is a natural product with multiple pharmacological activities and has inspired the discovery of two first‐in‐class drugs, amiodarone hydrochloride and sodium cromoglycate. The poor‐aqueous solubility is one of the limitations in developing this molecule. Herein, we aimed to improve the drug loading of khellin by developing its SEDDS formulation. A combination of castor oil, tetraethylene glycol, and Transcutol HP (10 : 30 : 60 v/v) was identified, inhibiting the drug‘s precipitation post‐dilution in an aqueous media. The optimized formulation, SB‐16KD, was characterized using 1H NMR, DSC, and FTIR to understand khellin‘s physical/chemical interaction with the formulation excipients. The in vitro dissolution studies of khellin in SB‐16KD correlated well with the oral pharmacokinetics in Wistar rats (1.6 vs. 1.7‐fold). The comparative oral pharmacokinetics of formulation against native khellin was performed at 45 mg/kg in Wistar rats. The results were promising, with 1.7‐fold higher plasma exposure by SEDDS formulation. Hence, the results warrant further developmental studies on SEDDS in dose reduction.

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Section: Uv-visible Spectrophotometric Analysis Of Khellinmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Self‐Emulsifying Drug Delivery of Khellin for Improving Its Oral Bioavailability

Shah,

Wazir,

Nandi

et al. 2023

ChemistrySelect

Self Cite

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show abstract

“…Chromone cores and its derivatives are extremely important due to its unique biological active . Hence, these backbones are usually found in many natural products and pharmaceutical drugs, such as Quercetin, Flavopiridol, and Genistein, etc. Based on these significant values, the synthesis of these scaffolds becomes a new field in heterocyclic chemistry.…”

Section: Introductionmentioning

confidence: 99%

Electrocatalytic Cascade Selenylation/Cyclization/Deamination of 2-Hydroxyaryl Enaminones: Synthesis of 3-Selenylated Chromones under Mild Conditions

Cen,

Liu,

et al. 2024

J. Org. Chem.

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Herein, we disclosed a highly efficient pathway toward 3-selenylated chromone derivatives via electrocatalytic cascade selenylation/cyclization/deamination of 2-hydroxyaryl enaminones with diselenides. This method showed mild conditions, easy operation, wide substrate scope, and good functional group tolerance. Furthermore, this electrosynthesis strategy was amendable to scale-up the reaction. Additionally, the preliminary experiments revealed that this reaction probably proceeded via a cation pathway instead of a radical pathway.

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The solubility determination and thermodynamic modeling of cis-3-(2,5-dimethylphenyl)-4-hydroxy-8-methoxy-1-azaspiro[4.5]dec-3-en-2-one (SI-VI) in binary mixed solvents from T = (288.15–328.15) K

Zuo

Liu

Zhao

et al. 2023

The Journal of Chemical Thermodynamics

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Thermodynamic solubility determination of khellin in eight mono-solvents at the range of 298.15 to 323.15 K

Cited by 6 publications

References 32 publications

Self‐Emulsifying Drug Delivery of Khellin for Improving Its Oral Bioavailability

Self‐Emulsifying Drug Delivery of Khellin for Improving Its Oral Bioavailability

Electrocatalytic Cascade Selenylation/Cyclization/Deamination of 2-Hydroxyaryl Enaminones: Synthesis of 3-Selenylated Chromones under Mild Conditions

The solubility determination and thermodynamic modeling of cis-3-(2,5-dimethylphenyl)-4-hydroxy-8-methoxy-1-azaspiro[4.5]dec-3-en-2-one (SI-VI) in binary mixed solvents from T = (288.15–328.15) K

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