Non-Aqueous Losartan Oral Solution for Stability and Accurate 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 for certain patient groups, potential dosing errors, instability, and degradation issues, along with bitter taste and contamination risks.
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
Engineering Contradiction Analysis
1Quantity of substance
If aqueous solutions are used for losartan formulation, then solubility is improved, but stability deteriorates due to water-related degradation
Solution Approach 1:
The patent changes the fundamental parameter of the solvent system from aqueous to non-aqueous (organic) based. This parameter change eliminates water-related degradation pathways while maintaining losartan solubility through selective use of organic solvents and excipients that are compatible with the drug's solubility characteristics.
Solution Approach 2:
The patent extracts and removes water from the formulation system entirely. By eliminating water as the solvent base and replacing it with non-aqueous excipients, the formulation eliminates water-related degradation mechanisms while maintaining drug solubility through alternative solubilizing agents.
2Stability of the object's composition
If solid forms (tablets) are used for losartan, then stability is improved, but ease of administration deteriorates for patients with difficulty swallowing
Solution Approach 1:
The patent transitions the formulation from solid (tablet) phase to liquid phase by creating an oral solution. This phase transition maintains the stability benefits of a defined composition while eliminating the swallowing difficulty associated with solid forms, as the liquid can be easily administered even to patients with dysphagia.
3Adaptability or versatility
If reconstitution kits are used, then flexibility in dosing is improved, but risk of dosing errors increases
Solution Approach 1:
The patent performs the reconstitution action in advance during manufacturing, creating a ready-to-use oral solution that requires no further preparation by the patient. This preliminary action eliminates the steps where dosing errors could occur during reconstitution, while maintaining flexibility in dosing through the liquid formulation that can be easily measured and administered.
4Ease of manufacture
If water is used as solvent, then ease of manufacture is improved, but contamination risk increases
Solution Approach 1:
The patent extracts and removes water from the formulation system, replacing it with non-aqueous excipients. This elimination of water removes the medium through which microbial contamination occurs, thereby reducing contamination risk while maintaining ease of manufacture through the use of readily available organic excipients.
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 formulation offers enhanced patient compliance, stability, and safety by eliminating water-related degradation, ensuring accurate dosing, and masking the bitter taste, while maintaining therapeutic efficacy.
Implementation Method 1
A ready-to-use, non-aqueous oral solution of losartan comprising losartan potassium, a solubilizer (like PEG 400)
Implementation Method 2
a thickening agent (such as xanthan gum)
Implementation Method 3
a preservative (sodium benzoate)
Data Source
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.