Shazly Gamal A, Haq Nazrul, Shakeel Faiyaz
Department of Pharmaceutics, College of Pharmacy, King Saud University, P.O. Box 2457, Riyadh, 11451, Kingdom of Saudi Arabia.
Arch Pharm Res. 2014 Jun;37(6):746-51. doi: 10.1007/s12272-013-0314-0. Epub 2013 Dec 17.
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.
本研究考察了格列本脲（GBN）在温度范围为298.15 - 333.15 K的Transcutol与水的二元共溶剂混合物中的溶液热力学及溶解度。采用修正的Apelblat模型预测GBN在不同温度下共溶剂混合物中的溶解度。GBN在纯Transcutol和纯水中的溶解度分别为最高和最低。此外，所有共溶剂混合物在333.15 K时溶解度最高。在所研究的每个温度下，GBN的实验溶解度数据与修正的Apelblat模型相关性良好，相对绝对偏差在0.008 - 5.903%范围内。共溶剂混合物中的相关系数在0.995 - 0.999范围内，表明实验数据与计算值拟合良好。GBN溶解的焓和熵分别在2.012 - 38.215 kJ mol⁻¹和6.748 - 114.709 J mol⁻¹ K⁻¹范围内，分别表明其溶解是吸热的且是熵驱动过程。这些结果表明，Transcutol可作为GBN制剂前研究和制剂开发中的共溶剂。
