Non-Aqueous Losartan Oral Solution for Stable Ready-to-Use Dosing

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Solution Overview

Problem

Existing losartan formulations, particularly in solid forms and aqueous solutions, pose challenges such as difficulty in swallowing, reconstitution errors, stability issues, and degradation, leading to potential contamination and incorrect dosing.

Innovation Solution

A ready-to-use, non-aqueous oral solution of losartan comprising losartan potassium, a solubilizer (like PEG 400), a thickening agent (such as xanthan gum), a preservative (sodium benzoate), and a sweetener (sucralose) in a formulation devoid of water, providing improved stability and ease of administration.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Ease of manufacture

If losartan is formulated as solid tablets for oral administration, then manufacturing and storage are simplified, but patient compliance deteriorates due to difficulty in swallowing

Engineering Contradiction:

Improvetablet formulationVSAvoidswallowing difficulty

Core Design Contradiction:

Ease of manufactureVSEase of operation

Solution Approach 1:

The patent changes the physical state parameter of losartan from solid (tablet) to liquid (oral solution), making it easier to administer to patients while maintaining manufacturing feasibility through standardized solution preparation processes

Inventive Principle:

Principle #35Parameter changes

Solution Approach 2:

The patent introduces a liquid vehicle (solvent system) as an intermediary medium to carry the losartan drug substance, enabling easy oral administration while maintaining drug stability through controlled solubility parameters

Inventive Principle:

Principle #24Intermediary (Mediator)

2Ease of operation

If losartan is formulated as aqueous solution for oral administration, then ease of administration is improved, but stability deteriorates due to degradation and contamination

Engineering Contradiction:

Improveoral administrationVSAvoiddrug stability

Core Design Contradiction:

Ease of operationVSStability of the object's composition

Solution Approach 1:

The patent changes the solvent type parameter from aqueous to non-aqueous, fundamentally altering the chemical environment to prevent hydrolysis and other water-related degradation pathways while maintaining oral administrability

Inventive Principle:

Principle #35Parameter changes

Solution Approach 2:

The patent creates a non-aqueous chemical environment that acts as an inert barrier against moisture and oxygen exposure, protecting the losartan from degradation while allowing oral administration

Inventive Principle:

Principle #39Inert atmosphere (Inert environment)

3Adaptability or versatility

If losartan is provided as powder for reconstitution, then flexibility in dosing is improved, but reliability deteriorates due to reconstitution errors and contamination

Engineering Contradiction:

Improvedosing flexibilityVSAvoiddosing accuracy

Core Design Contradiction:

Adaptability or versatilityVSReliability

Solution Approach 1:

The patent performs the reconstitution action in advance by providing a ready-to-use oral solution that is pre-prepared and sterilized, eliminating the risk of contamination and dosing errors that occur during home reconstitution while maintaining dosing flexibility

Inventive Principle:

Principle #10Preliminary action

Solution Approach 2:

The patent enables patients to administer the medication independently without requiring technical skills for reconstitution, as the solution is pre-prepared and ready for direct oral administration, thereby improving reliability while maintaining flexibility

Inventive Principle:

Principle #25Self-service

4Quantity of substance

If losartan is formulated in aqueous medium, then solubility is improved, but loss of substance increases due to oxidation and degradation

Engineering Contradiction:

Improvedrug solubilityVSAvoidoxidation degradation

Core Design Contradiction:

Quantity of substanceVSLoss of substance

Solution Approach 1:

The patent changes the solvent chemistry parameter from aqueous to non-aqueous, fundamentally preventing oxidation reactions that require water as a reactant, thereby preserving drug substance while maintaining adequate solubility for therapeutic effect

Inventive Principle:

Principle #35Parameter changes

Applied Scientific Principles

This section explains which scientific principles are used to turn an abstract innovation direction into a practical engineering solution.

Function Achieved in This Case

The solution offers enhanced patient compliance, stability for a suitable shelf life, and consistent dosing without the need for reconstitution, minimizing degradation and contamination risks.

Implementation Method 1

Losartan potassium is freely soluble in water, soluble in alcohols, slightly soluble in common organic solvents

Methodology Applied

Scientific EffectSolubility: Solvation

Implementation Method 2

a thickening agent (such as xanthan gum)

Methodology Applied

Scientific EffectViscosity enhancement:

Implementation Method 3

a preservative (sodium benzoate)

Methodology Applied

Scientific EffectPreservation: Preservative

Data Source

PatentUS20260060963A1Ready-to-use non-aqueous oral solution of losartan

Publication Date: 2026.03.05 LIQMEDS WORLDWIDE LTD

AI summary

Disclosed herein is a ready-to-use, non-aqueous oral solution of losartan. Also disclosed herein is a method of preparing a ready-to-use, non-aqueous oral solution of losartan and its method of use.