Solubility Enhancement of the Nonsteroidal Anti-inflammatory Drug of Pelubiprofen Salts

Allu, Suryanarayana; An, Ji-Hun; Park, Bum Jun; Kim, Woo-Sik

doi:10.1021/acs.cgd.3c00639

Cited by 3 publications

(1 citation statement)

References 67 publications

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“…Regarding the supramolecular environment of anions (Supporting Information Figures S9d and S10d), each forms hydrogen bonds with the neighboring anions and in (Hmmn)(H 2 PO 4 )•H 2 O with two water molecules. In both salts, a bilayer type of supramolecular architecture is observed (Supporting Information Figures S11e and S12e), with the hydrate having a simpler hydrogen bonding network characterized by R 4 4 (12) rings formed between two anions and two water molecules, as well as two anions and two cations. Additionally, an infinite supramolecular chain C 2n 2n (8n) is formed by anions alone.…”

Section: Molecularmentioning

confidence: 99%

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

Tuksar,

Topić,

Rubčić

et al. 2024

Mol. Pharmaceutics

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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.

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Section: Molecularmentioning

confidence: 99%

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

Tuksar,

Topić,

Rubčić

et al. 2024

Mol. Pharmaceutics

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Fabrication and evaluation of stable amorphous polymer-drug composite particles via a nozzle-free ultrasonic nebulizer

Lee,

Han,

et al. 2024

International Journal of Pharmaceutics

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Study of the Polymorphic Transformation Mechanism and Crystal Habits Control of Peramivir from Dihydrate to Trihydrate

Ge,

Fu,

Cai

et al. 2024

Crystal Growth & Design

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Peramivir is an effective antiviral drug for treating influenza A and B with the trihydrate form as the solid serving. However, a small amount of dihydrate still exists during the manufacturing process in a few production batches. Focusing on the problem, this study successfully obtained a new dihydrate single crystal structure, a higher-quality trihydrate single crystal structure surpassing previously reported findings, and a novel anhydrous form designated as form A. A comprehensive comparison of the crystal structure, crystal habits, thermal analysis, desolvation behavior, solubility, Hirshfeld Surfaces analysis, and energy frameworks was studied between peramivir dihydrate and trihydrate to understand the processes of water molecules binding on and off. The transformation process among the three crystal forms and the amorphous form revealed that the trihydrate form exhibits the most stability. The study of the polymorphic transformation mechanism revealed that dihydrate crystals precipitate initially, dissolve thereafter, and then transform into trihydrate crystals during crystallization. The conversion rate was related strongly to the stirring speed, and increasing the stirring speed accelerated both dissolution and crystal transformation, resulting in a reduction in the duration of crystallization. The crystallization time from dihydrate to trihydrate was shortened from 10 to 5.5 h when the stirring speed was increased from 50 to 300 rpm. The contrasting crystal habits of peramivir dihydrate (long rod-shaped) and trihydrate (tetragonal-shaped) also provide a quick estimate of mixed crystals. These studies made the crystal process stable and controlled, and pure trihydrate was obtained in a shorter time in industrial production.

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Solubility Enhancement of the Nonsteroidal Anti-inflammatory Drug of Pelubiprofen Salts

Cited by 3 publications

References 67 publications

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

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

Fabrication and evaluation of stable amorphous polymer-drug composite particles via a nozzle-free ultrasonic nebulizer

Study of the Polymorphic Transformation Mechanism and Crystal Habits Control of Peramivir from Dihydrate to Trihydrate

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