Mirabegron Modified-Release Tablet Composition for Stable Dissolution
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Solution Overview
Problem
Existing mirabegron compositions face issues with dissolution profile, stability, and pharmacotechnical properties such as flowability and homogeneity, despite the need for an improved modified release tablet formulation.
Innovation Solution
A modified release tablet composition comprising mirabegron with particle sizes less than 50 µm and polyethylene oxide of molecular weights between 4,000,000 and 7,000,000, along with additional excipients, is formulated using dry granulation or direct compression to ensure uniformity and stability, employing polyethylene oxide as a release controlling agent.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Speed
If mirabegron composition is formulated with conventional particle sizes and excipients, then manufacturing is simpler, but dissolution rate and bioavailability are insufficient
Solution Approach 1:
The patent applies parameter changes by specifying precise particle size ranges for mirabegron (d10: 5-20 μm, d50: 15-30 μm, d90: 20-40 μm) and polyethylene oxide (molecular weight 4,000,000-7,000,000), along with specific concentration ranges (mirabegron 10-40%, polyethylene oxide 5-20%). These parameter optimizations resolve the contradiction by enhancing dissolution rate through controlled particle size reduction while maintaining formulation simplicity through defined concentration ranges and a limited excipient palette.
Solution Approach 2:
The patent employs composite materials by combining mirabegron with specific ratios of polyethylene oxide (molecular weight 4,000,000-7,000,000) and other excipients in defined proportions. This composite formulation approach improves dissolution rate and bioavailability while maintaining manufacturing feasibility through established direct compression or wet granulation processes, thus resolving the technical contradiction between performance enhancement and formulation complexity.
2Duration of action of moving object
If polyethylene oxide with molecular weight 4,000,000-7,000,000 is used as release controlling agent, then modified release profile is achieved, but manufacturing complexity increases
Solution Approach 1:
The patent resolves this contradiction by optimizing the molecular weight parameter of polyethylene oxide to 4,000,000-7,000,000 and specifying its concentration range (5-20%). This parameter optimization enables sustained release over 12-24 hours while maintaining compatibility with standard manufacturing processes like direct compression and wet granulation, thus achieving extended release duration without proportionally increasing manufacturing complexity.
3Speed
If mirabegron particle size is reduced to d(0.9) less than 50 μm, then dissolution profile improves, but flowability and compressibility deteriorate
Solution Approach 1:
The patent resolves this contradiction by precisely controlling the particle size distribution parameters: d10: 5-20 μm, d50: 15-30 μm, d90: 20-40 μm. This controlled reduction in particle size improves dissolution rate while the specific distribution range maintains adequate flowability and compressibility for manufacturing, thus resolving the technical contradiction between dissolution enhancement and manufacturing ease.
Solution Approach 2:
The patent employs composite materials by combining finely divided mirabegron with polyethylene oxide and other excipients in specific ratios. This composite approach allows the use of reduced particle size mirabegron (improving dissolution) while the excipient matrix compensates for potential flowability and compressibility issues, thus resolving the technical contradiction.
4Reliability
If modified release formulation is used to prevent food effect, then bioavailability stability improves, but formulation complexity increases
Solution Approach 1:
The patent resolves this contradiction by formulating a composite material system comprising mirabegron, polyethylene oxide (molecular weight 4,000,000-7,000,000), and specific excipients in defined proportions. This composite formulation achieves reliable bioavailability by preventing food effect through controlled release mechanisms, while maintaining relatively simple manufacturing processes (direct compression or wet granulation), thus balancing bioavailability stability with formulation complexity.
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 desired dissolution rates, improved homogeneity, and enhanced stability with a simple, cost-effective manufacturing process, maintaining consistent drug levels in the bloodstream over an extended period.
Implementation Method 1
polyethylene oxide as a sustained release agent
Implementation Method 2
polyethylene oxide having a molecular weight of between 4,000,000 and 7,000,000
Data Source
AI summary
The present invention relates to a modified release tablet composition comprising mirabegron and polyethylene oxide wherein; mirabegron having a d (0.9) particle size less than 50 µm and polyethylene oxide having a molecular weight of between 4,000,000 and 7,000,000.