2022
DOI: 10.1021/acsomega.1c05788
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Preferential Solvation Study of the Synthesized Aldose Reductase Inhibitor (SE415) in the {PEG 400 (1) + Water (2)} Cosolvent Mixture and GastroPlus-Based Prediction

Abstract: Benzyl-2-{2,4-dioxo-5-(4-prop-2-yl-1yloxyl)benzylidene)thiazolin-3-yl)}acetamide (SE415) is a novel aldose reductase inhibitor used in the management of diabetes mellitus (DM) and associated complications. Herein, the drug was solubilized (mole fraction solubility) in a "PEG 400 (polyethylene glycol 400) + water" mixture of various ratios at 298.15 K. We reported the preferential solvation of SE415 by PEG 400 using Kirkwood−Buff integrals, the thermodynamic functional parameter, in vitro dissolution, and Gastr… Show more

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Cited by 11 publications
(14 citation statements)
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“…However, this value is significantly different from real absorption of the commercial RST tablet, as reported in the literature . This difference can be correlated with poor aqueous solubility and physicochemical properties of the drug responsible to be degraded in gastric lumen . The drug is acidic in nature due to bearing the carboxylic functional group, and the p K a value is 4.0 (Table ).…”
Section: Resultsmentioning
confidence: 79%
See 1 more Smart Citation
“…However, this value is significantly different from real absorption of the commercial RST tablet, as reported in the literature . This difference can be correlated with poor aqueous solubility and physicochemical properties of the drug responsible to be degraded in gastric lumen . The drug is acidic in nature due to bearing the carboxylic functional group, and the p K a value is 4.0 (Table ).…”
Section: Resultsmentioning
confidence: 79%
“…Thus, the program permits us to investigate improved in vivo performance of RST containing the (PEG400 + water) mixture than the conventional dosage form in humans. 41 In general, poor aqueous solubility of a drug results in a slow dissolution process and subsequently low oral bioavailability. The present study aimed to increase RST solubility using biocompatible PEG400 as a cosolvent which may augment oral absorption and bioavailability in a normal healthy human (70 kg).…”
Section: Resultsmentioning
confidence: 99%
“…To date, many structurally unique ALR2Is have been created, and some have shown excellent ALR2 inhibitory action [68] . However, most ALR2Is have not yet achieved clinical success because of their adverse effects or pharmacokinetic complications [69,70] . Therefore, this research will summarize new insights into the properties and functions of some of the bis‐sulfide ( 5 a – i ) and bis‐sulfone ( 6 a – i ) derivatives by inhibiting the ALR2 enzyme and its potential role in the prevention of diabetes.…”
Section: Resultsmentioning
confidence: 99%
“…From the thermodynamic point of view, the driving force of the dissolution ( ) is a combination of both the enthalpy and entropy contributions [ 36 ]. As shown in Table 3 , the values of the solution enthalpies ( ) are positive in all the solvents (endothermic process) as a consequence of a larger crystal lattice energy of BCL as compared to the solvation energy.…”
Section: Resultsmentioning
confidence: 99%
“…The enthalpy factor (by the absolute value) exceeds essentially the entropy one in all the studied solvents, showing the enthalpy determined dissolution process. The positive entropy values in the organic solvents impact favorable dissolution (entropy-driven process) [ 36 ]. At the same time, a rather high value of in n-hexane levels the entropy effect and leads to low solubility in this solvent.…”
Section: Resultsmentioning
confidence: 99%