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Solubility Measurement and Various Solubility Parameters of Glipizide in Different Neat Solvents

机译:格列吡嗪在不同净溶剂中的溶解度测量和各种溶解度参数

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Glipizide (GLZ) is an oral hypoglycemic agent, which is a weakly aqueous soluble drug. The solubility values of GLZ in various neat solvents are scarce in the literature. Hence, the solubility of GLZ in 12 different neat solvents, namely, “water, methanol, ethanol, isopropanol (IPA), 1-butanol, 2-butanol, ethylene glycol (EG), propylene glycol (PG), poly(ethylene glycol)-400 (PEG-400), ethyl acetate (EA), dimethyl sulfoxide (DMSO), and Transcutol-HP (THP)”, at “T = 298.2–318.2 K” and “p = 0.1 MPa” was measured. The recorded solubilities of GLZ were correlated by “van’t Hoff and Apelblat models” using root-mean-square deviation (RMSD). The overall RMSD was obtained as 1.21 and 1.40% for “Apelblat and van’t Hoff models”, respectively. Different solubility parameters of all studied materials including drug and solvent were calculated to find the best solvent for GLZ. The solubilities of GLZ (expressed in mole fraction) have been found highest in DMSO (2.81 × 10–2), followed by THP, EA, 2-butanol, 1-butanol, IPA, PEG-400, ethanol, PG, methanol, EG, and water (1.98 × 10–4) at “T = 318.2 K”. All investigated solubility parameters of GLZ were recorded very close to the DMSO. “Apparent thermodynamic analysis” showed an “endothermic and entropy-driven dissolution” of GLZ in the 12 different neat solvents. The highest molecular interactions were recorded in GLZ–DMSO compared to other combinations. Overall, DMSO has been considered as the best solvent for the solubilization of GLZ.
机译:格列吡嗪(GLZ)是一种口服降糖药,是一种水溶性较弱的药物。 GLZ在各种纯溶剂中的溶解度值在文献中很少。因此,GLZ在12种不同的纯溶剂中的溶解度,即“水,甲醇,乙醇,异丙醇(IPA),1-丁醇,2-丁醇,乙二醇(EG),丙二醇(PG),聚乙二醇)-400(PEG-400),乙酸乙酯(EA),二甲基亚砜(DMSO)和Transcutol-HP(THP)”,在“ T = 298.2–318.2 K”和“ p = 0.1 MPa”下进行了测量。使用“ van’t Hoff和Apelblat模型”,使用均方根偏差(RMSD)将GLZ的溶解度关联起来。对于“ Apelblat和van’t Hoff模型”,总的RMSD分别为1.21和1.40%。计算了所有研究材料(包括药物和溶剂)的不同溶解度参数,以找到适用于GLZ的最佳溶剂。发现GLZ的溶解度(以摩尔分数表示)在DMSO中最高(2.81×10–2),其次是THP,EA,2-丁醇,1-丁醇,IPA,PEG-400,乙醇,PG,甲醇, EG和水(1.98×10–4)在“ T = 318.2 K”处。记录的所有GLZ溶解度参数都非常接近DMSO。 “表观热力学分析”显示了GLZ在12种不同的纯溶剂中的“吸热和熵驱动溶解”。与其他组合相比,在GLZ–DMSO中记录了最高的分子相互作用。总体而言,DMSO被认为是GLZ增溶的最佳溶剂。

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