Solubility and preferential solvation of nimodipine and azlocillin drug compounds in (ethanol + ethyl acetate) mixtures

IF 16.4 1区 化学 Q1 CHEMISTRY, MULTIDISCIPLINARY
Adel Noubigh, Mustafa Jaipallah Abualreish, Lotfi Ben Tahar
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Abstract

This research focuses explicitly on the solubility of azlocillin and nimodipine in mixed binary solvents. This is relevant for pharmaceutical companies involved in developing and formulating these drugs. At a constant pressure of 101.2 kPa and temperatures ranging from 283.15 K to 323.15 K, the mole fraction equilibrium solubility of nimodipine and azlocillin in binary solvents (ethanol + ethyl acetate) was determined experimentally by gravimetric method. The results demonstrated that azlocillin and nimodipine solubility improved with higher ethanol mole fractions in mixed solvent systems. Among the three thermodynamic models, the experimental solubility data was best explained by the van't Hoff-Jouyban-Acree (V-J-A) model, followed by the Jouyban-Acree (J-A) model. The greatest RAD and RMSD values occur when two variables are compared to one another (RMSD) were 4.96 × 10−2 and 10.62 × 10−4 for azlocillin and 1.463 × 10−2 and 2.393 × 10−4 for nimodipine, respectively. The preferential solvation parameter \({\delta x}_{1,drug}\) is more significant than zero for nimodipine and azlocillin in the respective ranges of 0.60 < xE < 1 and 0.60 − 0.65 < xE < 1. This indicates that these two studied drug compounds prefer solvated by ethanol over ethyl acetate under these conditions. These results offer valuable perspectives for researchers in the pharmaceutical sciences, especially regarding the comprehension of drug compound solubility and solvation behavior in mixed solvent systems.

Abstract Image

尼莫地平和阿洛西林药物化合物在(乙醇+乙酸乙酯)混合物中的溶解度和优先溶解度
这项研究明确侧重于阿洛西林和尼莫地平在混合二元溶剂中的溶解度。这与参与开发和配制这些药物的制药公司息息相关。在 101.2 kPa 的恒压和 283.15 K 至 323.15 K 的温度范围内,采用重量法实验测定了尼莫地平和阿洛西林在二元溶剂(乙醇+乙酸乙酯)中的摩尔分数平衡溶解度。结果表明,在混合溶剂体系中,乙醇摩尔分数越高,阿洛西林和尼莫地平的溶解度越高。在三种热力学模型中,范特霍夫-焦班-阿克里(V-J-A)模型对实验溶解度数据的解释效果最好,其次是焦班-阿克里(J-A)模型。当两个变量相互比较时,最大的 RAD 值和 RMSD 值(RMSD)分别为:阿唑西林为 4.96 × 10-2 和 10.62 × 10-4,尼莫地平为 1.463 × 10-2 和 2.393 × 10-4。尼莫地平和阿洛西林的优先溶解参数({\delta x}_{1,drug}/)分别在 0.60 < xE < 1 和 0.60 - 0.65 < xE < 1 的范围内比零更显著。这表明在这些条件下,乙醇比乙酸乙酯更适合溶解这两种药物化合物。这些结果为制药科学研究人员提供了宝贵的视角,尤其是在理解药物化合物在混合溶剂体系中的溶解度和溶解行为方面。
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来源期刊
Accounts of Chemical Research
Accounts of Chemical Research 化学-化学综合
CiteScore
31.40
自引率
1.10%
发文量
312
审稿时长
2 months
期刊介绍: Accounts of Chemical Research presents short, concise and critical articles offering easy-to-read overviews of basic research and applications in all areas of chemistry and biochemistry. These short reviews focus on research from the author’s own laboratory and are designed to teach the reader about a research project. In addition, Accounts of Chemical Research publishes commentaries that give an informed opinion on a current research problem. Special Issues online are devoted to a single topic of unusual activity and significance. Accounts of Chemical Research replaces the traditional article abstract with an article "Conspectus." These entries synopsize the research affording the reader a closer look at the content and significance of an article. Through this provision of a more detailed description of the article contents, the Conspectus enhances the article's discoverability by search engines and the exposure for the research.
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