Softgel Capsule Fill Composition Preventing Acetaminophen Recrystallization
Find Innovative SolutionsGenerate Solutions
Solution Overview
Problem
Existing combination medications for colds and respiratory infections often face challenges in maintaining a clear, highly concentrated solution suitable for encapsulation in softgel capsules, as some active ingredients like acetaminophen tend to recrystallize, and the use of ionizing agents can accelerate degradation.
Innovation Solution
A bioavailable liquid softgel fill composition is formulated using a solubilizing matrix comprising pharmaceutically acceptable poly(alkylene glycols and polymeric solubilizing agents, such as polyethylene glycol and polyvinylpyrrolidone, which dissolves active ingredients like acetaminophen without ionizing agents, maintaining a clear solution for extended periods.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Quantity of substance
If a highly concentrated solution of medications is prepared for encapsulation in softgel capsules, then the bioavailability of medications is enhanced and the capsule size is reduced, but some medications such as acetaminophen tend to recrystallize
Solution Approach 1:
The patent introduces ionizing agents (alkali metal ions such as lithium, sodium, potassium, rubidium, and cesium cations) as intermediaries to prevent recrystallization of acetaminophen in highly concentrated solutions. These ionizing agents interact with the medication molecules to maintain solubility and prevent crystal formation, enabling stable highly concentrated formulations suitable for softgel encapsulation.
Solution Approach 2:
The patent changes the chemical parameters of the solution by adding ionizing agents that alter the ionic composition and electrical conductivity of the medium. This parameter change affects the solubility characteristics of acetaminophen, preventing recrystallization while maintaining high concentration. The formulation achieves this by carefully controlling the type and amount of ionizing agents present in the solution.
2Stability of the object's composition
If ionizing agents are used to prevent recrystallization of medications, then the stability of the solution is improved, but degradation of active ingredients may be accelerated
Solution Approach 1:
The patent applies local quality by selecting specific types of ionizing agents (certain alkali metal ions) and controlling their distribution and concentration in specific regions of the formulation. Different ionizing agents are used for different medications based on their compatibility and effectiveness, creating locally optimized conditions that prevent recrystallization while minimizing degradation for each specific active ingredient.
Solution Approach 2:
The patent creates composite formulations by combining multiple components including ionizing agents, solvents, and active ingredients in specific ratios. This composite approach allows the formulation to benefit from the recrystallization-preventing properties of ionizing agents while using complementary components to protect against degradation, achieving a balanced stable formulation.
3Ease of operation
If combination medications are formulated in a unitary formulation for convenience, then patient compliance is improved, but the formulation complexity increases
Solution Approach 1:
The patent merges multiple medications (acetaminophen and other active ingredients) into a single unitary formulation that can be encapsulated in one softgel capsule. This combining approach consolidates multiple dosing requirements into a single convenient dosage form, improving patient compliance while the patent simultaneously manages the formulation complexity through systematic use of ionizing agents and optimized solvent systems.
Solution Approach 2:
The patent creates a universal formulation system using ionizing agents that can accommodate multiple different active ingredients with varying solubility characteristics. This multi-functional approach allows the same basic formulation strategy (using ionizing agents to prevent recrystallization) to be applied across different medication combinations, simplifying the development process despite the complexity of creating combination products.
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 allows for a stable, clear, and bioavailable combination of analgesics, decongestants, expectorants, and antihistamines in softgel capsules, enhancing bioavailability and compliance, while avoiding recrystallization and degradation issues.
Implementation Method 1
solubilizing the AIs in a suitable matrix comprising a polymeric solubilizing agent and water in an alkylene glycol and poly(alkylene glycol) vehicle
Data Source
AI summary
Clear bioavailable liquid softgel fill compositions comprising a) at least one analgesic and one or more of decongestants, expectorants, antitussives and/or antihistamines; b) a matrix comprising a pharmaceutically acceptable poly(alkylene glycol) and a pharmaceutically acceptable alkylene glycol; c) a solubilizing agent comprising a pharmaceutically acceptable polymeric solubilizing agent and water are disclosed. Also disclosed are methods for the preparation of such clear fill compositions, and softgel capsules containing the clear bioavailable liquid fill composition.