PEG-PVP-Propylene Glycol Liquid Formulation Stability
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Solution Overview
Problem
Existing pharmaceutical compositions, particularly concentrated liquid formulations, face challenges in solubility and stability due to the poor solubility of agents like guaifenesin and the susceptibility of phenylephrine to degradation, leading to precipitation issues and bitter taste, which complicates the formulation of effective and palatable oral liquid medications for cold, cough, flu, and allergy relief.
Innovation Solution
A composition comprising polyethylene glycol, polyvinylpyrrolidone, and propylene glycol, with specific weight percentages of guaifenesin and phenylephrine, that inhibits precipitation and enhances stability, allowing for a palatable and effective oral liquid formulation that can be administered in low volumes, either as a solution or suspension, or filled into capsules.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Ease of operation
If concentrated liquid compositions are used to reduce dosing volume, then ease of dosing and volume are improved, but solubility of pharmaceutical agents deteriorates leading to precipitation
Solution Approach 1:
The patent uses cosolvents (polyethylene glycol and propylene glycol) as intermediary substances to mediate between the pharmaceutical agents and water, enabling high concentration formulations while maintaining solubility. These cosolvents create a compatible solvent environment that prevents precipitation of agents like guaifenesin and phenylephrine in concentrated liquid compositions.
Solution Approach 2:
The patent changes the physical-chemical parameters of the solvent system by incorporating specific ratios of polyethylene glycol (10-40% w/v) and propylene glycol (5-20% w/v) to modify solubility characteristics. This parameter change enables the formulation to maintain stability at higher pharmaceutical agent concentrations without precipitation.
2Reliability
If multiple pharmaceutical agents are combined in liquid formulations, then therapeutic efficacy is improved, but compatibility and stability deteriorate due to interactions between agents
Solution Approach 1:
The cosolvent system acts as an intermediary medium that facilitates compatibility between multiple pharmaceutical agents with different solubility characteristics. The polyethylene glycol and propylene glycol create a unified solvent environment that prevents adverse interactions and precipitation between agents like guaifenesin and phenylephrine.
Solution Approach 2:
The patent creates a composite solvent system combining polyethylene glycol, propylene glycol, and water in specific ratios. This composite material provides enhanced compatibility and stability for multi-agent formulations, allowing therapeutic combinations to remain stable in liquid form without precipitation or degradation.
3Ease of operation
If water-soluble pharmaceutical agents are used to improve dissolution, then ease of administration is improved, but bitter taste is generated that reduces consumer acceptance
Solution Approach 1:
The cosolvent system serves as an intermediary that modifies the taste profile of water-soluble pharmaceutical agents. By replacing part of the aqueous solvent with polyethylene glycol and propylene glycol, the bitter taste associated with high water content formulations is reduced while maintaining solubility and ease of 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 composition provides a stable and palatable solution that maintains the solubility of guaifenesin and phenylephrine, preventing precipitation and degradation, thus ensuring effective relief for symptoms like cold, cough, flu, fever, headache, pain, body ache, and allergy, with improved stability and taste.
Implementation Method 1
a mixture of polyethylene glycol, polyvinylpyrrolidone (PVP) and propylene glycol
Implementation Method 2
Enhanced stability of novel liquid compositions
Data Source
AI summary
The present invention relates to compositions of pharmaceutical agents in combination with additional pharmaceutical agents in a mixture of polyethylene glycol, polyvinylpyrrolidone, and propylene glycol and a process of making the compositions.