Deferiprone Liquid Formulation Taste Masking
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Solution Overview
Problem
Existing liquid pharmaceutical formulations, particularly for pediatric and geriatric patients, face challenges in masking the bitter taste of drugs like deferiprone, leading to poor compliance and underdosing due to the unpleasant taste and viscosity issues, which previous attempts have not adequately addressed.
Innovation Solution
A palatable liquid deferiprone formulation is developed using a taste masking composition comprising sucralose as a sweetener, hydroxyethylcellulose as a thickening agent, glycerin as a humectant, and flavoring agents such as artificial cherry flavor, which effectively masks the bitter taste and improves palatability.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Ease of operation
If deferiprone is formulated in liquid dosage form for pediatric and geriatric patients, then ease of swallowing is improved, but the bitter taste of the drug becomes prominent leading to poor compliance
Solution Approach 1:
The patent uses a complexing agent (such as cyclodextrin, hydroxypropylbeta-cyclodextrin, or sulfobutyletherbeta-cyclodextrin) as an intermediary substance that binds to deferiprone molecules through host-guest complexation. This complexation masks the bitter taste of deferiprone while maintaining its therapeutic efficacy, allowing the liquid formulation to be palatable for pediatric and geriatric patients.
Solution Approach 2:
The patent creates a composite liquid formulation system combining deferiprone with multiple excipients including complexing agents, sweetening agents, and flavoring agents. This composite approach integrates multiple functional components to simultaneously achieve taste masking, palatability enhancement, and maintained drug efficacy in a single liquid dosage form.
2Object-affected harmful factors
If high levels of sweetening agents are used to mask the bitter taste of deferiprone, then taste masking is improved, but the complexity of the formulation increases
Solution Approach 1:
The complexing agent serves as a primary intermediary that effectively masks the bitter taste of deferiprone through molecular complexation. This mechanism is more efficient than relying solely on high concentrations of sweetening agents, thereby reducing the need for excessive sweeteners and simplifying the overall formulation while achieving superior taste masking.
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 achieves a substantially non-bitter, palatable taste, enhancing patient compliance and bioavailability, as demonstrated by bioequivalence studies with tablets and improved tolerability in clinical trials, with a lower incidence of gastrointestinal adverse reactions compared to tablet formulations.
Implementation Method 1
The increase in viscosity is assumed to limit the contact of the drug with the tongue, presumably by slowing down salivary water uptake into the viscous liquid medicament
Implementation Method 2
a taste masking composition comprising an effective amount of a sweetener (such as sucralose) per litre of liquid composition, an effective amount of a thickening and suspension aid, (for example hydroxyethylcellulose), per litre of liquid composition
Data Source
AI summary
An oral pharmaceutical liquid formulation comprising deferiprone and a taste masking composition, said taste masking composition comprising an effective amount of a sweetener (such as sucralose) per litre of liquid composition, an effective amount of a thickening and suspension aid, (for example hydroxyethylcellulose), per litre of liquid composition, an effective amount of a humectant (such as glycerin) per litre of liquid composition, and an effective amount of at least one flavoring agent, wherein a final form of said taste-masked pharmaceutical has a substantially non-bitter and palatable taste.