Salts of Mefenamic Acid With Amines: Structure, Thermal Stability, Desolvation, and Solubility

Boudiombo, Jacky S. Bouanga; Jacobs, Ayesha

doi:10.1016/j.xphs.2018.08.003

Cited by 5 publications

(2 citation statements)

References 19 publications

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“…All data proved that new salt cocrystals produced superior solubility and accelerated MA dissolution over the salt forms. 25,26 This finding is also comparable with the dissolution rate enhancement reported recently based on the use of salt cocrystals of sodium and potassium diclofenac with L-proline. 43,44 The salt cocrystals combined the advantages of salt and cocrystals to maintain the "parachute after the spring effect."…”

Section: Intrinsic Dissolution Testssupporting

confidence: 89%

“…To overcome the poor solubility, 22 and wettability, 23 MA has been generated as a salt with alkaline elements, 24,25 and amines. 26 The sodium salt was also proven to improve the lack of hardness and friability, 25 which may cause tablet capping and longitudinal cracks. 27 The other problem is that MA exhibits polymorphs that exhibit dissolution inconsistency, as polymorph II is more soluble than polymorph I.…”

Section: Introductionmentioning

confidence: 99%

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New Sodium Mefenamate – Nicotinamide Multicomponent Crystal Development to Modulate Solubility and Dissolution: Preparation, Structural, and Performance Study

Nugrahani

Fisandra

Horikawa

et al. 2021

Journal of Pharmaceutical Sciences

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A cocrystal of mefenamic acid (MA) -nicotinamide (NA) has been reported to increase the solubility of MA, but it still does not exceed the solubility of sodium mefenamate (SM). Accordingly, this research dealt with a new salt cocrystal arrangement of SM − NA. Cocrystal screening was performed, followed by powder and single-crystal preparation. Solvent drop grinding and slow evaporation at cold and ambient temperatures were employed to produce the multicomponent crystal. Two new salt cocrystals were found as hemihydrates and monohydrates, named SMN-HH and SMN-MH, respectively. SMN-MH single crystals were successfully isolated and structurally analyzed using a single crystal X-ray diffractometer. Pharmaceutical properties were investigated, including hydrate stability, solubility, and intrinsic dissolution. The experiments showed that the hemihydrate was stable under ambient humidity and temperature, and that the monohydrate rapidly changed to hemihydrate. Both hydrates improved the solubility and intrinsic dissolution of SM, but SMN-HH was superior. The data showed that SMN salt cocrystals combine the advantages of salt and cocrystals and show potential for dosage form development.

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