Fampridine Prolonged-Release Tablet for Stability and Dissolution
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Solution Overview
Problem
Existing fampridine compositions suffer from substantial degradation during storage, leading to increased impurities and instability, and lack a simultaneous solution for stability and dissolution profile improvement.
Innovation Solution
A prolonged-release tablet formulation using fampridine with a particle size smaller than 120 µm and a cellulosic polymer, such as HPMC K100LV, ensures stability and desired dissolution profile by utilizing cellulose-derived polymers as prolonged-release agents.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Duration of action of stationary object
If fampridine is formulated in prolonged-release matrix tablets with conventional excipients, then prolonged-release profile is achieved, but substantial degradation occurs during storage leading to increased impurities
Solution Approach 1:
The patent changes the particle size parameter of fampridine to d(0.9) smaller than 120 μm, which fundamentally alters the drug's behavior in the matrix tablet. This parameter change enables both prolonged-release profile and improved stability by reducing the drug's reactivity with excipients while maintaining dissolution characteristics
Solution Approach 2:
The patent uses a composite matrix system combining cellulosic polymers (such as HPMC) with specific excipients in defined ratios. This composite material approach creates a formulation where the cellulosic polymer matrix provides both the prolonged-release mechanism and a stable environment that prevents drug degradation
2Productivity
If fampridine particle size is reduced to improve dissolution profile, then dissolution rate increases, but stability during storage deteriorates due to increased reactivity
Solution Approach 1:
The patent optimizes the particle size parameter to a specific range (d(0.9) smaller than 120 μm) that simultaneously achieves both goals. This precise parameter control ensures sufficient surface area for dissolution while minimizing the reactive surface area that causes degradation during storage
3Duration of action of stationary object
If conventional prolonged-release formulations are used, then release profile is achieved, but content uniformity varies significantly
Solution Approach 1:
By controlling the fampridine particle size to d(0.9) smaller than 120 μm, the patent ensures more uniform distribution of the drug throughout the matrix during compression. This particle size control prevents segregation and ensures consistent drug content in each tablet while maintaining the prolonged-release mechanism
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 provides high stability and content uniformity, maintaining a prolonged-release profile while preventing degradation, thus enhancing the effectiveness of fampridine in treating multiple sclerosis symptoms.
Implementation Method 1
cellulose derived polymers as prolonged-release polymers... act as binders that swell when hydrated by gastric media and delay absorption
Implementation Method 2
The tablet also has the desired dissolution profile... in a tablet in which the degradation of the active pharmaceutical ingredient is prevented or at least significantly reduced even under harsh conditions
Data Source
AI summary
The present invention relates to a prolonged-release tablet comprising fampridine and at least one pharmaceutically acceptable excipient wherein a d (0.9) particle size of fampridine is smaller than 120 µm and at least one cellulosic polymer for prolonged-release.