Solution thermodynamics and solubility prediction of glibenclamide in Transcutol + water co-solvent mixtures at 298.15–333.15 K

Abstract

Solution thermodynamics and solubility of glibenclamide (GBN) in binary co-solvent mixtures of Transcutol + water at temperature range of 298.15-333.15 K were investigated in present study. The modified Apelblat model was used to predict the solubility of GBN in co-solvent mixtures at various temperatures. The highest and lowest solubility of GBN were observed in pure Transcutol and pure water, respectively. Moreover, all co-solvent mixtures had highest solubility at 333.15 K. The experimental solubility data of GBN was correlated well with the modified Apelblat model at each temperature studied with relative absolute deviation in the range of 0.008-5.903 %. The correlation coefficients in co-solvent mixtures were observed in the range of 0.995-0.999 which indicated good fitting of experimental data with calculated one. The enthalpies and entropies for GBN dissolution were observed in the range of 2.012-38.215 kJ mol(-1) and 6.748-114.709 J mol(-1) K(-1), respectively indicating its dissolution is endothermic and an entropy-driven process. These results indicated that Transcutol can be used as a co-solvent in preformulation studies and formulation development of GBN.

Thermodynamics of the solubility of reserpine in {{2-(2-ethoxyethoxy)ethanol + water}} mixed solvent systems at different temperatures

“…The solubility of bioactive reserpine was found to increase with increase in mass fraction of 2-(2-ethoxyethoxy)ethanol in {2-(2-ethoxyethoxy)ethanol + water} mixed solvent systems at each temperature investigated (figure 2). These results are in accordance with previously published solubility values of other poorly water-soluble drugs such as paracetamol, diclofenac sodium, glibenclamide, risperidone, tadalafil, isoniazid analogue and thiosemicarbazone derivative in {2-(2-ethoxyethoxy)ethanol + water} mixed solvent systems [9][10][11][12][13][14][15].…”

“…The temperature was controlled with a thermostatic bath equipped with biological shaker. After 72 h, all the samples were taken out from the biological shaker and allowed the solute particles to settle for 2 h [9][10][11]. The samples were centrifuged at 5000 rpm for 15 min in order to remove fine particles.…”

“…The accuracy of the method was observed to be (98.60 to 100.40)%. The experimental mole fraction solubility (x e ) of reserpine in each co-solvent mixture was calculated as reported in literature [10,11].…”

“…Weak water-solubility of drugs is the main barrier for their formulation development [7,8]. Recently, 2-(2-ethoxyethoxy)ethanol (Transcutol Ò ) has been investigated as an efficient co-solvent for solubility enhancement of several poorly water-soluble drugs [9][10][11][12][13][14][15]. Various attempts via co-precipitation, solid dispersion and co-solvency approach have been made in order to enhance solubility and dissolution rate enhancement of reserpine [7,8,[16][17][18].…”

Measurement, correlation and thermodynamics of solubility of metronidazole in 2-(2-ethoxyethoxy)ethanol+water cosolvent mixtures at (298.15 to 333.15)K

“…Ethanol, PG and polyethylene glycol-400 (PEG-400) have been reported as commonly used cosolvents for formulation development and solubilization of poorly water-soluble compounds [12][13][14][15][16][17]. Recently, 2-(2-ethoxyethoxy)ethanol (Transcutol) has also been investigated as an efficient and alternative cosolvent of ethanol, PG and PEG-400 in solubilization of various poorly water-soluble drugs such as paracetamol, diclofenac sodium, glibenclamide, risperidone, tadalafil, thiosemicarbazones and isoniazid analogs [9,12,[18][19][20][21][22][23]. To the best of our knowledge, the temperature dependent solubility data of MTZ in 2-(2-ethoxyethoxy)ethanol + water cosolvent mixtures has not been reported in any pharmacopeia/encyclopedia/literature.…”