Sugar-Free Paracetamol Liquid Formulation for Stability and Palatability
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Solution Overview
Problem
Existing liquid pharmaceutical formulations of paracetamol often suffer from sedimentation and instability, leading to uneven concentration and unpleasant taste, especially in sugar-based solutions that are not suitable for low-sugar diets or patients with swallowing difficulties.
Innovation Solution
A sugar-free liquid pharmaceutical formulation containing an aqueous solution of paracetamol, polyethylene glycol as a solubilizing agent, xanthan gum as a thickening agent, and a sweetening system comprising sucralose and a mixture of polyols like glycerol, sorbitol, and xylitol, which maintains paracetamol in solution and provides a pleasant taste.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Stability of the object's composition
If paracetamol is suspended in liquid pharmaceutical form, then solubility issues are addressed, but sedimentation and instability occur over time
Solution Approach 1:
The patent changes the physical state of paracetamol from suspended solid particles to dissolved molecular form by optimizing the aqueous solution parameters. This is achieved through specific pH control (using citric acid and sodium citrate buffer system) and temperature management during preparation, allowing complete dissolution of paracetamol without suspension, thereby eliminating sedimentation while maintaining stability.
Solution Approach 2:
The patent introduces buffer systems (citric acid and sodium citrate) as intermediary substances that mediate between paracetamol and water to achieve complete dissolution. These intermediaries control the pH environment to optimize paracetamol solubility and prevent precipitation, ensuring both stability and reliability of the formulation.
2Ease of operation
If sugar-based sweetening agents are used, then palatability is improved, but suitability for low-sugar diets is reduced
Solution Approach 1:
The patent substitutes sugar-based sweetening agents with non-sugar alternatives (such as sucralose or other artificial sweeteners), changing the chemical composition parameters while maintaining the sweetening function. This allows the formulation to provide good palatability without containing sugars, making it suitable for both general use and low-sugar/ diabetic diets.
Solution Approach 2:
The patent extracts and removes sugar components from the sweetening system while retaining the essential sweetening function through alternative substances. This extraction of the harmful element (sugar) while preserving the beneficial function (palatability) resolves the contradiction between taste quality and dietary suitability.
3Quantity of substance
If paracetamol concentration is increased, then therapeutic efficacy is improved, but solubility and stability are compromised
Solution Approach 1:
The patent optimizes multiple solution parameters simultaneously - pH (using buffer system), temperature (controlled during preparation), and ionic strength (through buffer composition) - to maximize paracetamol solubility. This allows achieving high therapeutic concentrations (up to 12.5% or 125 mg/ml) while maintaining complete solubility and stability without precipitation or degradation.
Solution Approach 2:
The buffer system serves multiple functions: it controls pH to optimize solubility, acts as a stabilizer to prevent degradation, and maintains ionic strength for consistent solubility at high concentrations. This multi-functionality allows high paracetamol concentration while maintaining all required stability parameters.
4Ease of operation
If liquid pharmaceutical form is used, then ease of administration is improved, but bitter taste becomes more problematic
Solution Approach 1:
The patent extracts and removes the bitter taste characteristic from the formulation by using complete dissolution of paracetamol in optimized aqueous solution, which prevents the crystalline structure that causes bitterness. Additionally, non-sugar sweetening agents are used to counteract any remaining bitter notes, making the liquid form pleasant-tasting while maintaining ease of administration.
Solution Approach 2:
The patent changes the molecular environment of paracetamol through pH optimization and complete dissolution, which alters the taste profile from bitter to more acceptable. The buffer system and sweetening agents work together to modify the taste parameters, making the liquid formulation palatable while retaining the advantages of liquid administration.
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 maintains paracetamol stability over time, prevents darkening, and offers excellent palatability comparable to conventional syrups, making it suitable for patients with unpleasant taste issues and those on low-sugar diets.
Implementation Method 1
a solubilizing agent containing polyethylene glycol
Implementation Method 2
a thickening agent containing xanthan gum
Data Source
AI summary
The present invention relates to a sugar-free liquid pharmaceutical formulation comprising an aqueous solution of paracetamol, a solubilizing agent containing polyethylene glycol, a thickening agent containing xanthan gum, and a sweetening system containing sucralose and a mixture of polyols containing glycerol, sorbitol and xylitol in a total amount between approx. 15% and 35% w/v relative to the total volume of said pharmaceutical formulation.