Structural aspects, solid-state properties, and solubility performance of pharmaceutical sertraline-based organic salts

Diniz, Luan F.; Tenório, Juan C.; Ribeiro, Cauê; Carvalho, Paulo S.

doi:10.1016/j.molstruc.2022.134293

Cited by 10 publications

(3 citation statements)

References 42 publications

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“…The HCQ‐NDSA salt formation has been characterized by the SO3 − stretching bands at the 1270–1562 cm −1 region. [ 19 ] Further, a considerable shift in ─N─H/O─H stretching frequencies was observed, which was attributed to the involvement of different hydrogen bond interactions and the presence of water molecules in the crystal structures of prepared salts. The infrared spectra of each HCQ salt with free base and counterions were shown in Figure , and stretching frequencies corresponding to the functional groups involved in salts were listed in Table 3 .…”

Section: Resultsmentioning

confidence: 99%

Exploring New Solid Forms of Antirheumatic Drug Hydroxychloroquine: Novel Salts with Sustained‐Release Performance

Ji,

Wu,

Hong

et al. 2024

Cryst. Res. Technol.

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Hydroxychloroquine sulfate is a common drug for the treatment of rheumatoid arthritis. However, the disadvantage of this drug is that it needs to be taken continuously for 3–6 months to be effective and compliance of patients is poor. In this work, four new salt forms of hydroxychloroquine are successfully prepared whose crystal structures and properties are confirmed by a series of solid‐state characterization methods, including infrared spectroscopy, single crystal X‐ray diffraction, powder X‐ray diffraction, thermal analysis, and dynamic vapor sorption analysis. The hygroscopicity, stability, equilibrium solubility, and intrinsic dissolution rate of the four new salts are also tested. The moisture absorption, solubility, and intrinsic dissolution rate of newly prepared salts are significantly reduced, and the dissolution rates of 1‐hydroxy‐2‐naphthoate and 1,5‐naphthalenedisulfonate salts are only 1/158 and 1/335 of that of the therapeutically used sulfates, respectively. It is expected that they are potentially useful to be developed into a sustained‐release formulation, which can greatly improve the dosing compliance for rheumatoid arthritis treatment.

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Section: Resultsmentioning

confidence: 99%

Exploring New Solid Forms of Antirheumatic Drug Hydroxychloroquine: Novel Salts with Sustained‐Release Performance

Ji,

Wu,

Hong

et al. 2024

Cryst. Res. Technol.

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“…The hydrated salts CVD nitrate (CVD-NO3) and CVD sulfate (CVD-SO4) were prepared by the anion-exchange method. , CVD hydrochloride (CVD-HCl) was used as a precursor of these salts and has been prepared, as previously reported . CVD-HCl and the sodium salt of the acid former were taken in a 1:1 stoichiometric ratio and dissolved in 15 mL of a 40% ethanol/water mixture by heating to 60 °C.…”

Section: Methodsmentioning

confidence: 99%

Pharmaceutical Salts of Carvedilol with Increased Solubility as an Approach for Enhancing the Drug Action

Pereira,

Diniz,

W. Lehmann

et al. 2024

Crystal Growth & Design

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Carvedilol (CVD) is a β-blocker antihypertensive drug commonly used to treat cardiovascular disorders. Since the poor oral bioavailability of CVD can be improved directly by the enhancement of the active pharmaceutical ingredient solubility, we have focused on the development of more soluble multicomponent crystals (MCCs), i.e., by employing anhydrous and hydrated salts, of CVD. Using solvent evaporation and anion exchange as crystallization methods, eight MCCs containing CVD and salt formers recognized as safe and often used in pharmaceutical routines were successfully prepared. An in-depth crystallographic description of these MCCs was conducted through X-ray diffraction (single-crystal X-ray diffraction, PXRD) and thermal (differential scanning calorimetry, thermogravimetric analyses) techniques. Structurally, the inclusion of polar counterions and water molecules in the crystal structures generates ionic 3D arrangements with the sets of CVD+/anion/(n)H2O or CVD+/anion H-bonded to each other in meticulous assemblies. From the equilibrium solubility study in conditions that resemble physiological ones, it was verified that all CVD salts had substantial enhancements in API solubility (up to 25-fold) compared to pure CVD. These outcomes reinforce the potential of the MCCs synthesized herein to optimize the low oral bioavailability of CVD.

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“…Salt modification is a common strategy used in the pharmaceutical industry to optimize the properties of drugs. It involves the conversion of a drug’s active pharmaceutical ingredient (API) into a salt form via reactions with an appropriate acid or base [ 26 ]. Salt modification of drugs has several key points worth noting.…”

Section: Current Techniques To Improve Drug Solubility For Drug Desig...mentioning

confidence: 99%

Advancing Drug Delivery Paradigms: Polyvinyl Pyrolidone (PVP)-Based Amorphous Solid Dispersion for Enhanced Physicochemical Properties and Therapeutic Efficacy

Rusdin,

Mohd Gazzali,

Ain Thomas

et al. 2024

Polymers

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Background: The current challenge in drug development lies in addressing the physicochemical issues that lead to low drug effectiveness. Solubility, a crucial physicochemical parameter, greatly influences various biopharmaceutical aspects of a drug, including dissolution rate, absorption, and bioavailability. Amorphous solid dispersion (ASD) has emerged as a widely explored approach to enhance drug solubility. Objective: The objective of this review is to discuss and summarize the development of polyvinylpyrrolidone (PVP)-based amorphous solid dispersion in improving the physicochemical properties of drugs, with a focus on the use of PVP as a novel approach. Methodology: This review was conducted by examining relevant journals obtained from databases such as Scopus, PubMed, and Google Scholar, since 2018. The inclusion and exclusion criteria were applied to select suitable articles. Results: This study demonstrated the versatility and efficacy of PVP in enhancing the solubility and bioavailability of poorly soluble drugs. Diverse preparation methods, including solvent evaporation, melt quenching, electrospinning, coprecipitation, and ball milling are discussed for the production of ASDs with tailored characteristics. Conclusion: PVP-based ASDs could offer significant advantages in the formulation strategies, stability, and performance of poorly soluble drugs to enhance their overall bioavailability. The diverse methodologies and findings presented in this review will pave the way for further advancements in the development of effective and tailored amorphous solid dispersions.

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Structural aspects, solid-state properties, and solubility performance of pharmaceutical sertraline-based organic salts

Cited by 10 publications

References 42 publications

Exploring New Solid Forms of Antirheumatic Drug Hydroxychloroquine: Novel Salts with Sustained‐Release Performance

Exploring New Solid Forms of Antirheumatic Drug Hydroxychloroquine: Novel Salts with Sustained‐Release Performance

Pharmaceutical Salts of Carvedilol with Increased Solubility as an Approach for Enhancing the Drug Action

Advancing Drug Delivery Paradigms: Polyvinyl Pyrolidone (PVP)-Based Amorphous Solid Dispersion for Enhanced Physicochemical Properties and Therapeutic Efficacy

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