Concentrated liquid pharmaceutical formulations of furosemide
Inventors
Grossi, Alfredo • KOSTRABA, BRITT • OGUNLEYE, OLATOKUMBO O. LUCA • Terry, Shannon • KOPPENHAGEN, Franciscus
Assignees
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Publication Number
US-11559535-B2
Publication Date
2023-01-24
Expiration Date
Abstract
Disclosed herein, in part, are liquid pharmaceutical formulations comprising furosemide or a pharmaceutically acceptable salt thereof, one or more pharmaceutically acceptable excipients, and a pharmaceutically acceptable buffer. Methods of treating congestion, edema, fluid overload, or hypertension in a patient in need thereof are also provided.
Core Innovation
The patent discloses concentrated liquid pharmaceutical formulations comprising furosemide, or a pharmaceutically acceptable salt thereof, together with benzyl alcohol and a pharmaceutically acceptable buffer comprising tromethamine or a pharmaceutically acceptable salt thereof. The formulations specify concentration ranges for furosemide and benzyl alcohol, provide corresponding concentration ranges for tromethamine in a pharmaceutically acceptable buffer, and maintain a formulation pH generally between about 6.5 and about 8.5.
The disclosed formulations are presented with pharmaceutically acceptable excipients selected from N-methyl-pyrrolidone, ethanol, glycerin, polyethylene glycol, polysorbate 80, polyvinylpyrrolidone, and cyclodextrin including beta- or O-cyclodextrin. The description also includes optional components and adjustment concepts, including water and pH or osmolarity adjusters, along with disclosed windows for excipient and buffer concentration.
The patent further states that furosemide solubility depends on pH and buffer conditions, and that API-driven pH shifts and appearance changes are observed during solubility screening. Tromethamine is identified as a lead buffer, and excipient solubility studies in GRAS-compatible vehicles describe that excipient combinations can increase furosemide solubility while maintaining pH in a target window.
Claims Coverage
The independent claims collectively cover three inventive features centered on tromethamine-buffered, benzyl alcohol-containing liquid pharmaceutical formulations of furosemide with quantitatively specified component ranges and defined pH ranges.
Concentrated furosemide liquid with benzyl alcohol and tromethamine buffer at pH 6.5–8.5
A liquid pharmaceutical formulation comprising furosemide, or a pharmaceutically acceptable salt thereof, at a furosemide concentration from about 60 mg/mL to about 150 mg/mL, benzyl alcohol from about 0.1% (w/w) to about 10% (w/w), and a pharmaceutically acceptable buffer comprising tromethamine, or a pharmaceutically acceptable salt thereof, at a tromethamine concentration from about 25 mM to about 150 mM, where the formulation has a pH between about 6.5 to about 8.5.
Concentrated furosemide liquid with defined benzyl alcohol and tromethamine buffer at pH 7–8.5
A liquid pharmaceutical formulation comprising furosemide, or a pharmaceutically acceptable salt thereof, at a furosemide concentration from about 70 mg/mL to about 100 mg/mL, benzyl alcohol from about 1% (w/w) to about 3.5% (w/w), and a pharmaceutically acceptable buffer comprising tromethamine, or a pharmaceutically acceptable salt thereof, at a tromethamine concentration from about 50 mM to about 125 mM, where the formulation has a pH between about 7 to about 8.5.
Concentrated furosemide liquid with defined benzyl alcohol and tromethamine buffer at pH 7–8
A liquid pharmaceutical formulation comprising furosemide, or a pharmaceutically acceptable salt thereof, at a furosemide concentration from about 80 mg/mL to about 100 mg/mL, benzyl alcohol from about 1% (w/w) to about 3.5% (w/w), and a pharmaceutically acceptable buffer comprising tromethamine, or a pharmaceutically acceptable salt thereof, at a tromethamine concentration from about 50 mM to about 125 mM, where the formulation has a pH between about 7 to about 8.
The independent claims collectively cover tromethamine-based, benzyl alcohol-containing liquid pharmaceutical formulations of furosemide with pH in defined ranges and with quantitatively specified concentrations of furosemide and tromethamine.
Stated Advantages
Documented Applications
No documented applications found
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