Details

Autor(en) / Beteiligte

• Rao Khandavilli, U. B.
• Gangavaram, Swarupa
• Rajesh Goud, N.
• Cherukuvada, Suryanarayan
• Raghavender, S.
• Nangia, Ashwini
• Manjunatha, Sulur G.
• Nambiar, Sudhir
• Pal, Sharmistha

Titel

High solubility crystalline hydrates of Na and K furosemide salts

Ist Teil von

• CrystEngComm, 2014-01, Vol.16 (22), p.4842-4852

Erscheinungsjahr

2014

Quelle

Alma/SFX Local Collection

Beschreibungen/Notizen

• Novel sodium and potassium salts of the poorly soluble loop diuretic drug furosemide were prepared with the intent of improving drug solubility and bioavailability. Furo–Na salt was obtained as a trihydrate upon crystallization from aqueous NaOH solution, and furo–K salt crystallized as a monohydrate from KOH solution. Both salt hydrates were characterized by X-ray diffraction, DSC, TGA, and IR spectroscopy. An exothermic phase transition at 165 °C in the DSC heating curve of the furo–Na salt indicates the likelihood of polymorphism in its anhydrate phase. Based on solubility studies, furo–Na–trihydrate and furo–K–monohydrate in pH 7 phosphate buffer medium exhibited significantly higher aqueous solubilities of 41 mg mL −1 and 106 mg mL −1 compared to the free drug (0.01 mg mL −1 ). The physical stability of these fast dissolving salts under accelerated ICH conditions of 40 °C and 75% RH was modest, with furo–Na salt being stable for 2 weeks and furo–K salt for 1 week.