Levetiracetam Extended Release Tablet Core and Coating
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Solution Overview
Problem
Development of extended release drug formulations for water-soluble active ingredients like levetiracetam is challenging due to their ready dissolution, leading to bulky products and limited control over drug release, which affects patient compliance and the effectiveness of release controlling mechanisms.
Innovation Solution
A pharmaceutical composition comprising a tablet core with a water-insoluble polymer as the primary component, surrounded by an extended release coating that includes a mixture of water-insoluble and water-soluble polymers, allowing for controlled release of levetiracetam with varying polymer ratios to optimize dissolution characteristics.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If water-soluble polymers are used in the tablet core to control drug release, then drug release control is achieved, but the product becomes bulky and patient compliance deteriorates
Solution Approach 1:
The patent changes the solubility parameter of the polymer from water-soluble to water-insoluble, fundamentally altering how the polymer controls drug release. Instead of relying on polymer swelling and dissolution, the water-insoluble polymer provides structural framework that controls release through diffusion and erosion mechanisms, achieving release control without the bulkiness associated with high polymer loads of water-soluble polymers
Solution Approach 2:
The patent creates a composite tablet core formulation combining water-insoluble polymer with water-soluble excipients and drug. This composite approach allows the water-insoluble polymer to provide structural integrity and release control while the water-soluble components facilitate drug dissolution and release, achieving effective drug delivery without excessive bulk
2Duration of action of moving object
If hydrophilic matrix agents are used in the tablet core, then extended release is achieved, but the release controlling mechanism becomes limited in flexibility
Solution Approach 1:
The patent changes the hydrophilicity parameter of the matrix agent from hydrophilic to hydrophobic (water-insoluble), which fundamentally alters the release mechanism. The water-insoluble polymer provides a stable structural framework that can be combined with various water-soluble excipients and coatings, enabling flexible adjustment of release profiles through formulation variables rather than being constrained to a single hydrophilic matrix mechanism
Solution Approach 2:
The water-insoluble polymer serves multiple functions: providing structural framework, controlling release through diffusion barriers, and enabling compatibility with various water-soluble excipients and coatings. This multi-functionality provides greater formulation flexibility and adaptability compared to single-mechanism hydrophilic matrix systems
3Duration of action of moving object
If highly swellable hydrophilic polymer matrix is used, then extended release structure is provided, but release controlling coatings become ineffective
Solution Approach 1:
The patent changes the swelling behavior parameter of the polymer matrix from highly swellable to non-swellable (water-insoluble). This prevents the matrix from expanding and compromising coating integrity, allowing release-controlling coatings to remain effective while still providing extended release through the polymer's structural framework and controlled erosion/diffusion mechanisms
4Reliability
If water-soluble polymers are used in high amounts for extended release, then drug release control is improved, but patient compliance deteriorates due to bulky product
Solution Approach 1:
The patent changes the solubility parameter of the polymer from water-soluble to water-insoluble, enabling effective release control at lower polymer loadings. The water-insoluble polymer provides structural framework and diffusion barriers that control release without requiring the high polymer concentrations needed for water-soluble polymer systems, thereby reducing product bulkiness and improving patient compliance
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 use of a water-insoluble polymer core and a combination of polymers in the coating enables controlled release of levetiracetam, reducing the bulkiness of high-dose drugs and enhancing patient compliance by achieving extended release profiles with improved flexibility and effectiveness.
Implementation Method 1
the ready dissolution of these drugs, thus making it far more difficult to control the release of these substances
Implementation Method 2
controlled release of levetiracetam, reducing the bulkiness of high-dose drugs
Implementation Method 3
an extended release coating that includes a mixture of water-insoluble and water-soluble polymers, allowing for controlled release
Data Source
AI summary
Pharmaceutical compositions in the form of tablets are disclosed including water-soluble active ingredients such as levetiracetam and a polymer component which primarily includes water-insoluble polymers comprising between 60% and 100% of the polymer component in the tablet core, preferably the entire polymer component in the tablet core. The pharmaceutical compositions can also include an extended-release coating including both water-soluble and water-insoluble polymers.