Torsemide Extended-Release Tablet for Heart Failure

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Solution Overview

Problem

Current diuretic therapies for congestive heart failure (CHF) face challenges such as short duration of action, unpredictable effects, and adverse side effects due to rapid plasma concentration fluctuations, leading to compromised therapeutic efficacy and increased healthcare costs.

Innovation Solution

Development of an extended-release oral dosage formulation of Torsemide using a matrix component like hydroxypropyl methyl cellulose (HPMC) or glyceryl behenate, which maintains steady plasma levels and prolongs diuresis and natriuresis, reducing side effects and improving patient compliance.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Speed

If conventional immediate-release diuretic formulations are used, then rapid diuretic action is achieved, but duration of action is short (2-4 hours)

Engineering Contradiction:
Improveonset of diuretic actionVSAvoidduration of diuretic effect
Core Design Contradiction:
SpeedVSDuration of action of moving object

Solution Approach 1:

The patent segments the diuretic dose into multiple smaller doses delivered at different times through a multi-layered tablet structure. Each layer contains a portion of the total dose and releases it at a different rate, thereby extending the duration of action while maintaining rapid initial onset from the first layer

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The patent implements periodic action by designing the tablet to release the diuretic in multiple distinct phases or bursts over time. The controlled-release mechanism creates periodic elevation of plasma concentration, maintaining therapeutic effect throughout the day without requiring continuous high dosing

Inventive Principle:
Principle #19Periodic action

2Duration of action of moving object

If high doses of diuretics are administered to extend duration, then duration of action increases, but plasma concentration fluctuations become more extreme

Engineering Contradiction:
Improveduration of diuretic effectVSAvoidplasma concentration stability
Core Design Contradiction:
Duration of action of moving objectVSStability of the object's composition

Solution Approach 1:

By dividing the total daily dose into multiple smaller segments delivered throughout the day via the multi-layered tablet, the patent avoids the need for a single large dose. This segmentation smooths plasma concentration fluctuations while extending duration of action

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The patent achieves continuity of useful action by ensuring steady, controlled release of the diuretic throughout the day. The multi-layered design maintains therapeutic plasma concentrations continuously, eliminating the peaks and troughs associated with conventional dosing

Inventive Principle:
Principle #20Continuity of useful action

3Duration of action of moving object

If multiple daily doses are administered, then duration of coverage is improved, but patient compliance decreases

Engineering Contradiction:
Improveduration of diuretic effectVSAvoidpatient compliance
Core Design Contradiction:
Duration of action of moving objectVSEase of operation

Solution Approach 1:

The patent merges multiple individual doses into a single multi-layered tablet that delivers the entire daily regimen in one administration. This combining of multiple dosing events into one physical unit dramatically improves patient compliance while maintaining extended duration of action through the controlled-release mechanism

Inventive Principle:
Principle #5Merging (Combining)

4Ease of manufacture

If conventional diuretic formulations are used, then manufacturing simplicity is maintained, but therapeutic efficacy is compromised

Engineering Contradiction:
Improveformulation simplicityVSAvoidtherapeutic efficacy
Core Design Contradiction:
Ease of manufactureVSReliability

Solution Approach 1:

The patent employs composite materials by combining multiple layers with different release characteristics within a single tablet. This composite structure enables complex therapeutic profiles (rapid onset plus extended duration) while remaining manufacturable using conventional tabletting techniques applied to layered formulations

Inventive Principle:
Principle #40Composite materials

Data Source

PatentUS10596119B1Methods of treatment comprising torsemide
Publication Date: 2020.03.24 SARFEZ PHARMACEUTICALS INC
  • US10596119B1 patent drawing
  • US10596119B1 patent drawing
  • US10596119B1 patent drawing

AI summary

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.