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Publication Number
US-10596119-B1
Publication Date
2020-03-24
Expiration Date
Abstract
Disclosed herein are treatments for diseases such as sleep apnea, hyperuricemia, autistic spectrum disorder (ASD) and other brain disorders using controlled-release (CR, e.g., extended-release (ER) or prolonged-release (PR)) oral dosage formulations comprising an effective amount of Torsemide.
Core Innovation
The invention relates to controlled-release oral torsemide formulations, including extended-release or prolonged-release torsemide, that use an erosion-controlled polymer matrix and specified excipients. The formulation includes hydroxypropyl methyl cellulose and hydroxy propyl cellulose, and lipid/fatty-acid matrix components including glyceryl behenate and polyethylene glycol glyceride. It is defined by weight ranges for torsemide and matrix components, together with binder, filler/lactose, lubricant/talc, and magnesium stearate components.
The invention further describes defined particulate and bulk excipient characteristics, including microcrystalline cellulose used as a binder with nominal particle size parameters. In-vitro dissolution and release profile targets and modeling are described to support controlled-release behavior of torsemide. The approach is positioned as a way to manage torsemide exposure over time by reducing plasma level fluctuations compared with immediate-release torsemide.
The disclosure includes clinical rationale and comparative evaluation of immediate-release versus extended-release torsemide, including effects on urine flow, natriuresis/diuresis, creatinine clearance, blood pressure, and pharmacokinetic parameters. A novel mechanism is also discussed in which torsemide extended-release is linked to renal NKCC2 effects and modulation of membrane guanylate cyclase/cGMP pathways with natriuretic peptides, relating to diuretic efficiency and renal/heart-brain interaction. The invention also frames combined therapy use cases with other drug classes, including SGLT inhibitors and aldosterone receptor antagonists.
Claims Coverage
The partial content contains five independent claim themes, each centered on a daily torsemide dose range of 5-200 mg or a pharmaceutically acceptable salt thereof, combined with at least one other drug product from specified drug classes. The independent claims cover treating sleep apnea, hyperuricemia, Autism Spectrum Disorder (ASD), brain disorders, and heart failure patients with diabetes.
Treating sleep apnea with daily torsemide and specified adjunct drug classes
A method of treating sleep apnea comprising administration of daily dose of 5-200 mg torsemide or a pharmaceutically acceptable salt thereof, and at least one other drug product comprising an aldosterone receptor antagonist, a sodium glucose linked transporter (SGLT) inhibitor, a sympatholytic agent, or an anxiolytic agent.
Treating hyperuricemia with daily torsemide and specified adjunct drug classes
A method of treating hyperuricemia comprising administration of a daily dose of 5-200 mg torsemide or a pharmaceutically acceptable salt thereof, and at least one other drug product comprising an aldosterone receptor antagonist, a sodium glucose linked transporter (SGLT) inhibitor, a sympatholytic agent, or an anxiolytic agent.
Treating Autism Spectrum Disorder (ASD) with daily torsemide and specified adjunct drug classes
A method of treating Autism Spectrum Disorder (ASD) comprising administration of daily dose of 5-200 mg torsemide or a pharmaceutically acceptable salt thereof, and at least one other drug product comprising an aldosterone receptor antagonist, a sodium glucose linked transporter (SGLT) inhibitor, a sympatholytic agent, or an anxiolytic agent.
Treating brain disorders with daily torsemide and expanded specified adjunct drug classes
A method of treating brain disorders comprising the administration of daily dose of 5-200 mg torsemide or a pharmaceutically acceptable salt thereof, and at least one other drug product comprising an aldosterone receptor antagonist, a sodium glucose linked transporter (SGLT) inhibitor, a sympatholytic agent, an anxiolytic agent, NKCC inhibitor, or N-Methyl-D-Aspartate (NMDA) receptor antagonist.
Treating heart failure patients with diabetes with daily torsemide and specified adjunct drug classes
A method of treating heart failure patients with diabetes comprising administration of daily dose of 5-200 mg torsemide or a pharmaceutically acceptable salt thereof, and at least one other drug product comprising an aldosterone receptor antagonist, a sodium glucose linked transporter (SGLT) inhibitor, a sympatholytic agent, or an anxiolytic agent.
Overall, the claim coverage emphasizes combining a daily torsemide dose of 5-200 mg or a pharmaceutically acceptable salt with at least one other drug product selected from aldosterone receptor antagonists, SGLT inhibitors, sympatholytic agents, anxiolytic agents, and, for brain disorders, NKCC inhibitor and/or an NMDA receptor antagonist. Dependent claims further refine the torsemide formulation composition and narrow the release form of the co-administered drug products to immediate release or extended release.
Stated Advantages
Not explicitly described in patent.
Documented Applications
Not explicitly described in patent.
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