Modified-Release Fesoterodine Formulation for Stability and Dissolution
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Solution Overview
Problem
Fesoterodine is prone to degradation due to hydrolyzation and oxidation, necessitating the development of a stable formulation that maintains chemical and physical integrity over an extended period.
Innovation Solution
A modified release formulation comprising fesoterodine with a fructose-sucrose mixture as stabilizers, along with excipients like hydroxypropylmethyl cellulose and glyceryl dibehenate, provides enhanced stability and controlled release properties.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Stability of the object's composition
If fesoterodine is formulated with conventional stabilizers, then chemical stability is improved, but physical stability and dissolution profile are compromised
Solution Approach 1:
The patent uses a composite stabilizer system combining sucrose (reducing sugar) and fructose (monosaccharide) in specific weight ratios (1:4 to 4:1). This composite approach provides both chemical stability through Maillard reaction prevention and physical stability through glass transition temperature enhancement, resolving the contradiction between chemical and physical stability requirements.
Solution Approach 2:
The patent optimizes the weight ratio parameters of sucrose to fructose (1:4 to 4:1) and controls the water content (0.5-5% w/w) to achieve the desired glass transition temperature and physical stability. By changing these compositional parameters, the formulation maintains both chemical integrity and physical properties simultaneously.
2Stability of the object's composition
If fesoterodine is stabilized against hydrolyzation and oxidation, then chemical stability is improved, but dissolution rate and pharmacotechnical properties deteriorate
Solution Approach 1:
The sucrose-fructose mixture acts as an intermediary substance that protects fesoterodine from hydrolyzation and oxidation while maintaining dissolution properties. The reducing sugars in this mixture form protective complexes with the drug molecule, preventing degradation pathways while allowing controlled release and maintaining pharmacotechnical properties like flowability and compressibility.
3Stability of the object's composition
If complex microencapsuled structures are used, then stability is improved, but device complexity and manufacturing cost increase
Solution Approach 1:
The patent extracts the essential stabilizing function from complex microencapsuled structures and implements it through a simpler sucrose-fructose mixture system. This eliminates the need for complex shell formulations and multi-component matrices, reducing device complexity while maintaining stability through the glass transition mechanism and chemical protection provided by the sugar mixture.
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 improved chemical stability, physical stability, and desired dissolution profile, along with excellent pharmacotechnical properties such as flowability and homogeneity, while maintaining effective drug release over 12-24 hours.
Implementation Method 1
stabilizers with binding properties was used, so while the stable formulation is provided without using extra load of excipients
Data Source
AI summary
The present invention relates to modified release formulations comprising fesoterodine or a pharmaceutically acceptable salt thereof with at least two sugars or its derivatives as stabilizers.