United States Patent 5,004,613: A Detailed Analysis
Introduction
The United States Patent 5,004,613, titled "Oral sustained release pharmaceutical formulation and process," is a significant invention in the field of pharmaceuticals, particularly focusing on sustained release formulations. This patent, granted on March 26, 1991, outlines a method and composition for creating oral sustained release pharmaceutical tablets.
Inventors and Assignees
The patent was invented by a team of researchers and assigned to the company that employed them. However, the specific names of the inventors and the assignee are not provided in the sources, but it is common for such patents to be assigned to pharmaceutical companies or research institutions.
Background of the Invention
The invention addresses the need for pharmaceutical formulations that can release the active ingredient over an extended period, improving patient compliance and therapeutic efficacy. Sustained release formulations are designed to maintain a consistent drug concentration in the bloodstream, reducing the frequency of dosing and potential side effects associated with peak drug levels.
Summary of the Invention
The patent describes a method for preparing oral sustained release pharmaceutical tablets. The process involves creating a wet granulation using povidone (PVP) in water or an alcohol-water mixture as the granulating agent. The active pharmaceutical ingredient is mixed with inactive powdered excipients and hydroxyethyl cellulose (HEC), then granulated, dried, milled, and blended with additional excipients before being compressed into tablets[4].
Claims of the Patent
The patent claims are crucial as they define the scope of the invention and what is protected by the patent. Here are the key claims:
Composition Claims
- The patent claims a pharmaceutical composition comprising a matrix formed from granulations of the active ingredient mixed with inactive powdered excipients and HEC, using PVP as the granulating agent[4].
Process Claims
- The process claims include the steps of granulating, drying, milling, blending with additional excipients, and compressing the mixture into tablets to achieve a sustained release profile[4].
Functional Claims
- The claims also cover the functionality of the sustained release formulation, ensuring that the rate of release of the pharmaceutical can be varied or controlled[4].
Patent Landscape
Understanding the patent landscape is essential for positioning this invention within the broader context of pharmaceutical formulations.
Prior Art
The patent references several prior art documents, including earlier patents related to sustained release formulations and granulation processes. For example, it mentions U.S. Pat. No. 4,820,522, which is a continuation-in-part of the current patent application[4].
Competitive Landscape
The patent landscape in the early 1990s included various other sustained release formulations and processes. Patents such as U.S. Pat. No. 5,298,262 and U.S. Pat. No. 5,302,401, which deal with nanoparticulate compositions and methods to reduce particle size growth, indicate a vibrant and innovative field[2].
Technological Advancements
The invention builds upon existing technologies by introducing a specific method using PVP and HEC to achieve sustained release. This advancement was significant in the field of pharmaceutical formulations, offering a new approach to controlling the release rate of active ingredients.
Impact and Applications
The impact of this patent is multifaceted:
Therapeutic Benefits
- The sustained release formulation improves patient compliance by reducing the frequency of dosing.
- It maintains a consistent drug concentration in the bloodstream, enhancing therapeutic efficacy and reducing side effects.
Industrial Applications
- The process described in the patent can be scaled up for industrial production, making it a practical solution for pharmaceutical manufacturers.
- The use of PVP and HEC as granulating agents and excipients, respectively, provides a stable and reliable method for producing sustained release tablets.
Enforceability and Defensibility
A thorough patentability search, as described in other contexts, is crucial for ensuring the enforceability and defensibility of the patent. This involves analyzing the specific claims, understanding prior art, and refining the patent claims to accurately reflect the novel and non-obvious aspects of the invention[3].
Licensing and Enforcement
The patent's value extends to licensing and enforcement. Understanding the patent landscape allows patent holders to identify potential licensees and negotiate favorable terms. In the event of infringement, a well-supported patent application ensures that the patent claims are defensible, strengthening the patent holder’s position in legal actions[3].
Key Takeaways
- Innovation in Formulation: The patent introduces a novel method for creating sustained release pharmaceutical tablets using PVP and HEC.
- Therapeutic Benefits: The formulation improves patient compliance and maintains consistent drug levels, enhancing therapeutic efficacy.
- Industrial Significance: The process is scalable and practical for industrial production.
- Patent Landscape: The invention is part of a broader landscape of sustained release formulations and processes.
- Enforceability: A thorough patentability search is essential for ensuring the patent's enforceability and defensibility.
FAQs
Q: What is the primary innovation of United States Patent 5,004,613?
A: The primary innovation is the method for creating oral sustained release pharmaceutical tablets using povidone (PVP) as the granulating agent and hydroxyethyl cellulose (HEC) as an excipient.
Q: How does the sustained release formulation improve patient compliance?
A: The sustained release formulation reduces the frequency of dosing, making it easier for patients to adhere to their medication regimen.
Q: What are the key components of the sustained release matrix described in the patent?
A: The matrix is formed from granulations of the active ingredient mixed with inactive powdered excipients and HEC, using PVP as the granulating agent.
Q: How does the patent contribute to the broader field of pharmaceutical formulations?
A: The patent introduces a new approach to controlling the release rate of active ingredients, contributing to the advancement of sustained release formulations.
Q: What is the significance of a thorough patentability search in relation to this patent?
A: A thorough patentability search ensures that the patent claims are well-supported, reducing ambiguity and strengthening the enforceability of the patent against potential infringers.
