Pharmaceutical Composition with HPMC Release Modifier
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Solution Overview
Problem
Current pharmaceutical compositions face challenges in achieving a controlled release profile for active pharmaceutical ingredients, particularly in maintaining a mean drug release of at least 80% between 6 and 10 hours, which is crucial for effective therapeutic delivery.
Innovation Solution
A pharmaceutical composition comprising granules with an active pharmaceutical ingredient and intragranular excipients, along with an extragranular portion of hydroxypropyl methylcellulose or its mixture as a release modifier, designed for oral administration using a specific dissolution profile with the paddle method in phosphate buffer.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Duration of action of moving object
If conventional release modifiers are used, then drug release can be achieved, but the dissolution profile cannot maintain at least 80% mean drug release between 6 and 10 hours
Solution Approach 1:
The patent changes the chemical parameter of the release modifier by specifically selecting hydroxypropyl methylcellulose (HPMC) with defined viscosity ranges (4,000-15,000 cP or 15,000-25,000 cP). This parameter change in the excipient's physical properties enables the dissolution profile to achieve at least 80% mean drug release between 6-10 hours, resolving the contradiction between release duration and dissolution control.
Solution Approach 2:
The patent creates a composite tablet structure with distinct granule and non-granule portions, where each portion contains specific excipients with complementary functions. The granule portion provides drug delivery while the non-granule HPMC portion controls release, creating a composite system that achieves both sustained duration and precise dissolution profile control.
2Productivity
If drug release is accelerated, then therapeutic effect is improved, but release occurs outside the desired 6-10 hour window
Solution Approach 1:
The patent applies local quality by creating spatially distinct regions within the tablet: granule portions that facilitate drug release and non-granule HPMC portions that control release timing. This local differentiation allows the drug release rate to be optimized while maintaining precise timing control within the 6-10 hour window, resolving the contradiction between release rate and timing control.
3Ease of manufacture
If tablet composition is simplified, then manufacturing is easier, but dissolution profile cannot be precisely controlled
Solution Approach 1:
The patent segments the tablet into distinct functional portions: granule material containing the drug and intragranular excipients, and non-granule material containing HPMC as release modifier. This segmentation allows each portion to be optimized for its specific function while maintaining overall manufacturing simplicity, achieving both ease of manufacture and precise dissolution profile control.
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 composition achieves a controlled drug release of at least 80% between 6 and 10 hours, ensuring effective therapeutic delivery and stability, addressing the challenge of maintaining a consistent release profile.
Implementation Method 1
an extragranular portion comprising at least one release modifier; wherein the release modifier is a hydroxypropyl methylcellulose or a mixture thereof
Implementation Method 2
the composition has a dissolution profile of at least about 80% mean drug release between about 6 hours and about 10 hours
Data Source
AI summary
Provided is a pharmaceutical composition comprising: (a) granules comprising an active pharmaceutical ingredient, and one or more intragranular excipients; and an extragranular portion comprising at least one release modifier. Also provided are process for the preparation and methods for the use of the pharmaceutical composition.