United States Patent 5,422,123: A Comprehensive Analysis
Introduction
United States Patent 5,422,123, titled "Tablet for Pharmaceutical Use Able to Release Active Substances at Successive Times," is a significant innovation in the field of controlled drug delivery systems. This patent, assigned to Pharmidea SRL, outlines a novel approach to designing tablets that can release active pharmaceutical ingredients (APIs) in a controlled and successive manner.
Background and Motivation
The development of this patent was driven by the need for more sophisticated drug delivery systems that can provide both immediate and sustained release of therapeutic agents. Traditional tablets often suffer from limitations such as rapid release, which can lead to peak and trough effects, or delayed onset of action. The inventors aimed to address these issues by designing a tablet that could release APIs at successive times, enhancing the therapeutic efficacy and patient compliance.
Patent Claims
The patent includes several key claims that define the scope and novelty of the invention:
Claim 1: Tablet Composition
The patent claims a tablet comprising a deposit core containing a therapeutically active substance, a support-platform partially covering the deposit core, and a layer of swellable and/or gellable polymeric material[2].
Claim 2: Support-Platform
The support-platform is described as being made of swellable and/or gellable polymeric materials. This platform plays a crucial role in controlling the release of the active substance from the deposit core[2].
Claim 3: Layer of Polymeric Material
The layer of polymeric material is designed to swell or gel upon contact with a dissolution medium, thereby modulating the release of the active substance. This layer can be applied in various configurations to achieve the desired release profile[2].
Claim 4: Successive Release
The patent claims that the tablet is capable of releasing the active substance at successive times, which is achieved through the combination of the deposit core, support-platform, and polymeric layer. This successive release profile is critical for maintaining therapeutic levels of the drug over an extended period[2].
Detailed Description of the Invention
Deposit Core
The deposit core contains the therapeutically active substance. This core is the primary reservoir of the drug and is designed to release the API in a controlled manner[2].
Support-Platform
The support-platform partially covers the deposit core and is made of swellable and/or gellable polymeric materials. This platform helps in controlling the initial release of the drug and ensures that the API is released in a sustained manner[2].
Polymeric Layer
The polymeric layer is applied over the support-platform and is designed to swell or gel upon contact with a dissolution medium. This swelling or gelling action modulates the release of the active substance, allowing for a prolonged and controlled release profile[2].
Advantages and Benefits
Controlled Release
The tablet design ensures a controlled release of the active substance, which helps in maintaining therapeutic levels of the drug over an extended period. This reduces the need for frequent dosing and improves patient compliance[2].
Successive Release Profile
The successive release profile allows for both immediate and sustained release of the API, addressing the peak and trough effects associated with traditional tablets. This enhances the therapeutic efficacy of the drug[2].
Improved Bioavailability
The controlled release mechanism can improve the bioavailability of the drug by ensuring that the API is released in a manner that optimizes absorption in the body[2].
Patent Landscape
Related Patents
Several other patents in the field of controlled drug delivery systems share similarities with US Patent 5,422,123. For example:
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US Patent 5,882,682: This patent discloses a device for controlled delivery of therapeutically active pharmaceutical ingredients in dispersion, using a compressed core, a polymer forming gelatinous microscopic particles upon hydration, and a water-insoluble coating with formed apertures[1].
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US Patent 5,972,389: This patent describes gastric-retained controlled-release oral drug dosage forms comprising particles of a solid-state drug dispersed in a swellable/erodible polymer[1].
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US Patent 6,372,255: This patent outlines a multi-layer tablet with immediate and prolonged release layers, similar to the successive release profile of US Patent 5,422,123[1].
Competitive Analysis
The patent landscape in controlled drug delivery systems is highly competitive, with numerous patents and patent applications focusing on various mechanisms for controlled release. US Patent 5,422,123 stands out due to its unique combination of a deposit core, support-platform, and polymeric layer, which provides a flexible and effective way to achieve successive release of APIs.
Impact on the Pharmaceutical Industry
Innovation in Drug Delivery
US Patent 5,422,123 has contributed significantly to the innovation in drug delivery systems. The concept of successive release has been adopted and modified in various subsequent patents, reflecting its impact on the field[2].
Clinical Applications
The controlled release mechanism described in this patent has been applied in various clinical settings to improve the efficacy and safety of drug therapies. This includes applications in chronic diseases where sustained drug levels are crucial for effective management[2].
Regulatory Considerations
The patent's claims and descriptions have also influenced regulatory guidelines for controlled release formulations. Regulatory bodies often refer to such patents when evaluating the safety and efficacy of new drug delivery systems[4].
Key Takeaways
- Controlled Release Mechanism: The patent describes a novel controlled release mechanism using a deposit core, support-platform, and polymeric layer.
- Successive Release Profile: The tablet is designed to release active substances at successive times, enhancing therapeutic efficacy and patient compliance.
- Bioavailability and Efficacy: The controlled release profile improves bioavailability and reduces peak and trough effects.
- Impact on Industry: The patent has influenced innovation in drug delivery systems and has clinical applications in various diseases.
- Regulatory Influence: The patent's claims have shaped regulatory guidelines for controlled release formulations.
FAQs
Q: What is the primary innovation of US Patent 5,422,123?
A: The primary innovation is the design of a tablet that can release active substances at successive times using a deposit core, support-platform, and polymeric layer.
Q: How does the support-platform contribute to the controlled release mechanism?
A: The support-platform, made of swellable and/or gellable polymeric materials, partially covers the deposit core and helps in controlling the initial release of the drug.
Q: What are the advantages of the successive release profile described in the patent?
A: The successive release profile ensures both immediate and sustained release of the API, improving therapeutic efficacy and patient compliance.
Q: How has this patent influenced the pharmaceutical industry?
A: The patent has contributed to innovation in drug delivery systems, influenced clinical applications, and shaped regulatory guidelines for controlled release formulations.
Q: Are there similar patents in the field of controlled drug delivery?
A: Yes, several other patents, such as US Patents 5,882,682 and 5,972,389, share similarities with US Patent 5,422,123 but offer different mechanisms for controlled release.
Sources Cited
- EP2521537A2 - Pharmazeutische ... - Google Patents
- US-5422123-A - Unified Patents Portal
- Patent Claims Research Dataset - USPTO
- Search for patents - USPTO
