Micronized Tolcapone Sustained Release Tablet
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Solution Overview
Problem
Current tolcapone formulations are immediate release, leading to peak plasma concentrations and short therapeutic levels, necessitating the development of an extended release tablet to maintain effective plasma levels for a longer duration.
Innovation Solution
The development of sustained release tablets using micronized tolcapone in combination with a release retardant and a binder, manufactured through a direct compression process, which slows the release of tolcapone and maintains therapeutic levels for a prolonged period.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Duration of action of moving object
If non-micronized tolcapone is used in immediate release formulations, then the manufacturing process is simple, but the plasma concentration peaks quickly and therapeutic levels are not maintained for a prolonged period
Solution Approach 1:
The patent changes the particle size parameter of tolcapone by micronization, reducing it to achieve a slower dissolution rate. This parameter change transforms the immediate release characteristic into sustained release, extending the duration of therapeutic plasma levels while controlling the peak concentration speed
Solution Approach 2:
The patent creates a composite formulation by combining micronized tolcapone with specific excipients including release retardants (such as hydroxypropyl methyl cellulose, ethyl cellulose, or starch) and binders. This composite material structure controls the release kinetics, achieving sustained release profile that maintains therapeutic levels for prolonged periods
2Duration of action of moving object
If micronized tolcapone is used in sustained release formulations, then the release of tolcapone is slower and more controlled, but the manufacturing process complexity increases due to direct compression requirements
Solution Approach 1:
The patent extracts the granulation step from the traditional tablet manufacturing process. By using micronized tolcapone directly in compression without requiring granulation and blending with extragranular excipients, the process is simplified despite the micronization requirement. The direct compression approach eliminates complex multi-step processing
Solution Approach 2:
The patent changes the physical state parameter of tolcapone to micronized form, which enables direct compression manufacturing. This parameter change allows the material to be compressed directly into sustained release tablets without requiring complex granulation equipment and processes, thus controlling manufacturing complexity while achieving the desired release profile
Data Source
AI summary
The present invention relates to sustained release tablet comprising micronized tolcapone, a release retardant and a binder, to said tablet for use in the prevention and/or treatment of a transthyretin-associated amyloidosis, to a method for the prevention and/or treatment of a transthyretin-associated amyloidosis comprising administering to a subject in need thereof an effective amount of said tablet, to pharmaceutical composition in the form of said tablet which is used in the prevention and/or treatment of a transthyretin-associated amyloidosis and to a process for the manufacture of said tablet.