Reduced Preservative Liquid Pharmaceutical Composition
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Solution Overview
Problem
Pharmaceutical compositions containing substituted benzhydryl piperazines, such as cetirizine and levocetirizine, are prone to microbial contamination due to the lack of effective preservatives, especially when the seal is broken, exposing them to environmental and bodily microorganisms.
Innovation Solution
A liquid pharmaceutical composition with reduced amounts of preservatives, specifically parahydroxybenzoate esters, is developed, using concentrations between 0 and 1.5 mg/ml, which provides stability against microbial contamination while maintaining antimicrobial efficacy.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Object-affected harmful factors
If traditional preservative concentrations are used, then microbial contamination is prevented, but patient safety is compromised due to allergic reactions and if preservatives are reduced or eliminated, then patient safety is improved, but microbial contamination risk increases
Solution Approach 1:
The patent removes traditional preservatives (parabens, benzalkonium chloride, phenoxethanol) from the pharmaceutical composition and replaces them with the active substance itself (cetirizine, levocetirizine, or efletirizine) which exhibits intrinsic preservative activity, thereby eliminating allergic reactions while maintaining microbial protection
Solution Approach 2:
The active substance (cetirizine, levocetirizine, or efletirizine) serves dual functions: (1) therapeutic antihistaminic activity and (2) preservative activity against bacteria, yeasts, and molds, eliminating the need for separate preservative agents and their associated allergenicity risks
2Object-affected harmful factors
If preservatives are reduced to less than 3 mg/ml, then patient safety is improved by reducing allergic reactions, but the composition becomes more susceptible to microbial contamination
Solution Approach 1:
The active substance (cetirizine, levocetirizine, or efletirizine) provides self-preservative activity, meaning the therapeutic agent itself protects the composition from microbial contamination without requiring additional preservative agents, enabling preservative reduction below 3 mg/ml while maintaining stability
3Reliability
If multiple preservatives are used to ensure stability, then microbial contamination is prevented, but the manufacturing process becomes more complex and costly
Solution Approach 1:
The patent extracts and eliminates multiple preservative agents (parabens, benzalkonium chloride, phenoxethanol) from the formulation, simplifying the manufacturing process by reducing the number of ingredients to be sourced, handled, and controlled, while maintaining microbial protection through the active substance's intrinsic preservative activity
Solution Approach 2:
The active substance serves multiple functions including therapy and preservation, eliminating the need for multiple separate preservative agents and their associated manufacturing complexities, thereby simplifying the overall manufacturing process
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 composition effectively prevents microbial growth, reducing the risk of allergic reactions in sensitive patients and simplifying the manufacturing process by minimizing the use of poorly soluble preservatives, while ensuring the stability and safety of the pharmaceutical solution over time.
Implementation Method 1
the active substances belonging to the family of substituted benzhydryl piperazines possess a preservative effect in aqueous solutions
Data Source
AI summary
The present invention relates to a liquid composition containing an active substance belonging to the family of substituted benzhydryl piperazines with reduced amounts of preservatives.