Taste-Masked Cationic Resin Composition
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Solution Overview
Problem
Existing taste-masking technologies for pharmaceutical compounds, particularly those using ion exchange resins, face challenges in achieving high loading concentrations and effective taste-masking, with issues of unbound active compounds affecting the taste and release profiles.
Innovation Solution
A taste-masked composition is created by loading a physiologically active compound onto a polymeric matrix with ionic functional groups and washing it with a nonpolar solvent to remove unbound compounds without dissociating the bound ones, using a cation exchange resin with anionic functional groups and a basic active compound, ensuring at least 60% functional group binding and minimal unbound active compound presence.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Quantity of substance
If an ion exchange resin is used to adsorb an active compound for taste-masking, then the active compound becomes available after passing the oral cavity, but the concentration of active compound that can be loaded and the effectiveness of taste-masking remain unsatisfactory
Solution Approach 1:
The patent changes the chemical parameters of the ion exchange resin by selecting specific functional groups (carboxylic acid, sulfonic acid, phosphonic acid) and controlling the ratio of bound active compound to functional groups (at least 0.5:1). This optimization of chemical parameters enables both high loading concentration and effective taste-masking by ensuring sufficient binding capacity while maintaining high active compound concentration on the resin.
2Manufacturing precision
If a polar solvent is used to wash the loaded matrix to remove unbound active compounds, then unbound compounds are removed, but dissociation of bound active molecules from the loaded matrix occurs
Solution Approach 1:
The patent changes the physical parameter of the washing solvent by selecting nonpolar solvents (polarity index less than 5, preferably less than 3) instead of polar solvents. This parameter change allows effective removal of unbound active compounds while preventing dissociation of bound active molecules, as the nonpolar solvent does not interfere with the ionic interactions between the active compound and the ion exchange resin functional groups.
3Productivity
If the concentration of active compound on the ion exchange resin is increased, then loading efficiency improves, but unbound active compound remains affecting taste
Solution Approach 1:
The patent optimizes the chemical parameter of binding by ensuring that at least 0.5 moles of active compound are bound per mole of functional groups, creating strong ionic interactions that prevent dissociation. Combined with nonpolar solvent washing, this ensures high loading efficiency while eliminating unbound active compound that would cause disagreeable taste.
Solution Approach 2:
The patent applies extraction by using nonpolar solvents to selectively remove unbound active compounds from the loaded matrix. The nonpolar solvent extracts only the unbound active compound while leaving the bound active compound intact on the ion exchange resin, thereby eliminating the harmful taste effect while maintaining high loading concentration.
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 solution results in a high-loading, effective taste-masked composition that prevents undesirable taste in the mouth and ensures rapid release in the stomach, maintaining a high concentration of bound active compounds while minimizing unbound ones, thereby enhancing the organoleptic properties and bioavailability.
Implementation Method 1
a taste-masked composition containing an ion exchange resin having carboxylic acid functional groups and dextromethorphan
Implementation Method 2
washing the loaded matrix to remove unbound active compounds without causing competing dissociation of the bound active from the matrix
Data Source
AI summary
The present invention provides a taste-masked composition containing an active compound. The composition is taste-masked by employing a loaded polymeric matrix which is produced by incorporating or complexing the active compound on a polymeric matrix having ionic functional groups and removing unbound active compounds from the polymeric matrix.