Exploring Salts of Memantine with Inorganic Anions: From Polymorphism and Solid-State Transitions to Potential for Drug Formulations.

IF 4.5 2区 医学 Q2 MEDICINE, RESEARCH & EXPERIMENTAL
Molecular Pharmaceutics Pub Date : 2024-09-02 Epub Date: 2024-08-06 DOI:10.1021/acs.molpharmaceut.4c00670
Mihaela Tuksar, Edi Topić, Mirta Rubčić, Ernest Meštrović
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引用次数: 0

Abstract

This study examines pharmaceutically acceptable inorganic salts of memantine, specifically focusing on hydrogen sulfate, sulfate, and dihydrogen phosphate salts, with the aim of finding alternatives to the commonly used chloride salt in the treatment of Alzheimer's disease. Through comprehensive solid-state characterization, including powder X-ray diffraction, thermal analysis, and solubility testing, we unveil complex polymorphic behaviors, reversible solid-state transitions, and significant differences in solubility and stability among the salts. Notably, the hydrogen sulfate salt emerges as a promising candidate for drug formulations, offering improved solubility, nonhygroscopic nature, and favorable morphological characteristics compared to the existing chloride salt. This work establishes a foundation for further investigation into memantine salts as potential therapeutics with improved efficacy.

Abstract Image

探索美金刚的无机阴离子盐:从多态性和固态转变到药物制剂的潜力。
本研究探讨了美金刚的药用无机盐,特别关注硫酸氢盐、硫酸盐和磷酸二氢盐,目的是找到治疗阿尔茨海默病常用氯盐的替代品。通过全面的固态表征,包括粉末 X 射线衍射、热分析和溶解度测试,我们揭示了这些盐之间复杂的多态行为、可逆的固态转变以及在溶解度和稳定性方面的显著差异。值得注意的是,与现有的氯盐相比,硫酸氢盐具有更好的溶解性、非吸湿性和良好的形态特征,有望成为药物制剂的候选物质。这项工作为进一步研究美金刚盐作为潜在治疗药物并提高疗效奠定了基础。
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来源期刊
Molecular Pharmaceutics
Molecular Pharmaceutics 医学-药学
CiteScore
8.00
自引率
6.10%
发文量
391
审稿时长
2 months
期刊介绍: Molecular Pharmaceutics publishes the results of original research that contributes significantly to the molecular mechanistic understanding of drug delivery and drug delivery systems. The journal encourages contributions describing research at the interface of drug discovery and drug development. Scientific areas within the scope of the journal include physical and pharmaceutical chemistry, biochemistry and biophysics, molecular and cellular biology, and polymer and materials science as they relate to drug and drug delivery system efficacy. Mechanistic Drug Delivery and Drug Targeting research on modulating activity and efficacy of a drug or drug product is within the scope of Molecular Pharmaceutics. Theoretical and experimental peer-reviewed research articles, communications, reviews, and perspectives are welcomed.
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