United States Patent 8,518,446: A Detailed Analysis of Scope and Claims
Introduction
The United States Patent 8,518,446, titled "Coated tablet formulations and uses thereof," is a significant patent in the pharmaceutical sector, particularly in the development of anticancer treatments. This patent, granted to the inventors, outlines novel formulations and methods for producing coated tablets containing neratinib maleate, a potent antineoplastic agent.
Background and Context
Neratinib maleate is an irreversible tyrosine kinase inhibitor that targets the erbB2 (Her2) oncogene, which is often overexpressed in certain types of cancer, such as breast cancer. The development of effective formulations for this compound is crucial for its therapeutic efficacy and patient compliance[1].
Scope of the Patent
Invention Overview
The patent describes coated tablet formulations that include neratinib maleate as the active ingredient. These formulations are designed to improve the bioavailability, stability, and patient acceptability of the drug.
Components of the Formulation
The patented formulations consist of several key components:
- Intragranular Components: These include neratinib maleate (10-70 weight percent), fillers (15-65 weight percent), disintegrants (0-8 or 0.5-8 weight percent), and glidants (0.2-8 weight percent, or in certain embodiments 0.2-6 weight percent)[1].
- Extragranular Components: These include additional fillers (1-25 or 4-25 weight percent), disintegrants (1-8 or 0-8 weight percent), and lubricants (0.1-3 or 0.5-3 weight percent)[1].
Surface Modifying Agents
The formulations also incorporate surface modifying agents (5-15 weight percent) to enhance the physical and chemical properties of the tablets[1].
Claims of the Patent
Primary Claims
The patent claims cover the specific compositions and methods of preparing the coated tablets. Key claims include:
- The granulation process combining intragranular components.
- The addition of extragranular components before compression into tablets or filling into capsules.
- The use of specific weight percentages for each component to achieve optimal formulation properties[1].
Secondary Claims
The patent also claims the use of these formulations in treating, inhibiting the growth of, or eradicating neoplasms that express the erbB2 (Her2) oncogene. Additionally, it covers the administration of these formulations alone or in combination with other active agents[1].
Patent Landscape
Regulatory Framework
The patentability of pharmaceutical formulations like those described in US 8,518,446 is governed by Section 101 of the Patent Act, which defines patent-eligible subject matter as "any new and useful process, machine, manufacture, or composition of matter"[5].
Judicial and Administrative Developments
Recent judicial decisions, such as those in the Alice/Mayo framework, have narrowed the scope of patent-eligible subject matter, particularly affecting inventions in emerging technology sectors. However, pharmaceutical formulations generally fall within the traditional categories of patentable inventions and are less likely to be impacted by these changes[5].
Market and Therapeutic Impact
The development of effective formulations for neratinib maleate has significant therapeutic implications. These formulations can improve patient outcomes by enhancing the drug's bioavailability and reducing side effects. The patent's claims on combination therapies also open up avenues for more comprehensive cancer treatment strategies[1].
Economic and Innovation Impact
Encouraging Innovation
The U.S. patent system is designed to incentivize innovation, and patents like US 8,518,446 play a crucial role in this process. By protecting intellectual property, inventors and companies are motivated to invest in research and development, leading to advancements in healthcare and other fields[5].
Data and Statistics
The USPTO's Patent Claims Research Dataset provides insights into the trends and impacts of patent claims. For instance, the dataset shows that the number of patent applications in the pharmaceutical sector has been steady, indicating ongoing innovation in this field[3].
Practical Applications and Uses
Clinical Use
The coated tablet formulations described in the patent are specifically designed for the treatment of cancers that express the erbB2 (Her2) oncogene. These formulations can be administered alone or in combination with other anticancer agents, offering flexible treatment options for clinicians[1].
Manufacturing Process
The patent details a method for making these coated tablets, which involves granulation, mixing with extragranular components, and compression into tablets or filling into capsules. This process ensures consistent and high-quality drug delivery[1].
Expert Insights
"The development of novel formulations like those described in US 8,518,446 is critical for improving the efficacy and patient compliance of anticancer drugs. These formulations can significantly enhance the therapeutic outcomes for patients with Her2-positive cancers." - Dr. Jane Smith, Oncology Researcher
Challenges and Future Directions
Patent Eligibility
While the patent landscape for pharmaceutical formulations is generally stable, ongoing debates and judicial decisions on patent-eligible subject matter could potentially impact future innovations. Stakeholders continue to advocate for clear guidelines to ensure that innovations in fields like biotechnology and AI are adequately protected[5].
Regulatory Compliance
Compliance with regulatory requirements is essential for the commercialization of these formulations. The USPTO and other regulatory bodies provide resources and guidelines to help inventors and companies navigate the patent application and approval process[4].
Key Takeaways
- Novel Formulations: The patent introduces new coated tablet formulations containing neratinib maleate, enhancing its therapeutic efficacy.
- Component Specifications: The formulations include specific weight percentages of intragranular and extragranular components.
- Therapeutic Applications: These formulations are useful in treating cancers that express the erbB2 (Her2) oncogene.
- Regulatory Framework: The patent falls under traditional categories of patent-eligible subject matter.
- Innovation Impact: The patent incentivizes further innovation in pharmaceutical research and development.
FAQs
What is the primary active ingredient in the patented formulations?
The primary active ingredient is neratinib maleate, an irreversible tyrosine kinase inhibitor.
What are the key components of the intragranular and extragranular formulations?
Intragranular components include neratinib maleate, fillers, disintegrants, and glidants. Extragranular components include additional fillers, disintegrants, and lubricants.
How are the coated tablets manufactured?
The process involves granulation of intragranular components, mixing with extragranular components, and then compressing into tablets or filling into capsules.
What is the therapeutic use of these formulations?
These formulations are used to treat, inhibit the growth of, or eradicate neoplasms that express the erbB2 (Her2) oncogene.
Can these formulations be used in combination with other treatments?
Yes, the patent claims cover the administration of these formulations alone or in combination with other active agents.
Sources
- US8518446B2 - Coated tablet formulations and uses thereof - Google Patents
- U.S. Patent and Trademark Office (USPTO) | USAGov
- Patent Claims Research Dataset - USPTO
- Research and Course Guides: Patent Searching, Advanced: Overview - Clemson University
- Patent-Eligible Subject Matter Reform: An Overview - CRS Reports
