Solubility enhancement of atorvastatin calcium and ethanol-mediated transition with some surfactants

IF 1.2 4区 化学 Q4 CHEMISTRY, PHYSICAL Physics and Chemistry of Liquids Pub Date : 2023-05-22 DOI:10.1080/00319104.2023.2210252
Hadi Foroughi, E. Rahimpour, M. Kouhkan, Anahita Fathi Azarbayjani, A. Jouyban
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Abstract

ABSTRACT Atorvastatin calcium (ATC) is a class II BCS blockbuster synthetic cholesterol-lowering drug. The aim of this work is to examine the solubility of ATC in ethanol and water mixtures at room temperature and to study the effect of various concentrations of Tween 80 and benzalkonium chloride (BAC) on drug solubility in aqueous mixtures of ethanol. ATC shows maximum solubility in ethanol + water mixtures at a ratio of w1 = 0.7 ethanol. The addition of a surfactant changed the drug solubility profile relative to the surfactant type and its concentration. XRD and DSC results indicate that a high concentration of BAC may induce the formation of ATC solvate which influenced the melting point and solubility of the drug. Surfactant type and concentration influence the morphology, nucleation, and growth of drug crystals. A high concentration of BAC accelerates crystal habits and its relative growth rate while Tween 80 slows its growth rate.
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一些表面活性剂增强阿托伐他汀钙和乙醇介导过渡的溶解度
阿托伐他汀钙(ATC)是一类BCS重磅级合成降胆固醇药物。本研究的目的是在室温下考察ATC在乙醇和水混合物中的溶解度,并研究不同浓度的t80和苯扎氯铵(BAC)对乙醇水溶液混合物中药物溶解度的影响。ATC在w1 = 0.7乙醇的乙醇+水混合物中溶解度最大。表面活性剂的加入改变了与表面活性剂类型和浓度相关的药物溶解度分布。XRD和DSC结果表明,高浓度BAC可诱导ATC溶剂化物的形成,从而影响药物的熔点和溶解度。表面活性剂的种类和浓度影响药物晶体的形态、成核和生长。高浓度的BAC加速了晶体习性和相对生长速度,而Tween 80则减缓了晶体生长速度。
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来源期刊
Physics and Chemistry of Liquids
Physics and Chemistry of Liquids 化学-物理:凝聚态物理
CiteScore
3.30
自引率
8.30%
发文量
43
审稿时长
6-12 weeks
期刊介绍: Physics and Chemistry of Liquids publishes experimental and theoretical papers, letters and reviews aimed at furthering the understanding of the liquid state. The coverage embraces the whole spectrum of liquids, from simple monatomic liquids and their mixtures, through charged liquids (e.g. ionic melts, liquid metals and their alloys, ions in aqueous solution, and metal-electrolyte systems) to molecular liquids of all kinds. It also covers quantum fluids and superfluids, such as Fermi and non-Fermi liquids, superconductors, Bose-Einstein condensates, correlated electron or spin assemblies. By publishing papers on physical aspects of the liquid state as well as those with a mainly chemical focus, Physics and Chemistry of Liquids provides a medium for the publication of interdisciplinary papers on liquids serving its broad international readership of physicists and chemists.
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