United States Patent 4,968,509: A Detailed Analysis of Scope, Claims, and Patent Landscape
Introduction
United States Patent 4,968,509, titled "Oral sustained release acetaminophen formulation and process," is a significant innovation in the field of pharmaceuticals, particularly in the development of sustained-release formulations. This patent, issued on November 6, 1990, addresses the formulation and manufacturing process of a sustained-release acetaminophen product.
Background and Context
The patent is a continuation of application Ser. No. 78,138, filed on July 27, 1987, which later issued as U.S. Pat. No. 4,820,522 on April 11, 1989. This background indicates a series of developments aimed at improving the delivery mechanism of acetaminophen, a widely used analgesic and antipyretic medication[1].
Scope of the Patent
Therapeutic Composition
The patent is directed to a sustained release therapeutic composition comprising acetaminophen as the therapeutically active medicament. This composition includes a matrix formed from granulations of acetaminophen mixed with inactive powdered excipients and hydroxyethyl cellulose (HEC) using an aqueous solution of Povidone U.S.P. (polyvinylpyrrolidone--PVP) as the granulating agent[1].
Key Components
- Active Ingredient: Acetaminophen, which constitutes 68% to 94% of the total composition by weight.
- Inactive Ingredients: These include granulating agents and excipients, which make up 6% to 32% of the total composition by weight. In preferred embodiments, these inactive ingredients are less than 15% of the total weight[1].
Formulation Process
The process involves granulating acetaminophen with PVP, drying, milling, blending with additional excipients, and then compressing the mixture into a tablet. This process allows for the controlled release of acetaminophen over a sustained period[1].
Claims of the Patent
Main Claims
The patent claims cover the following:
- A sustained release therapeutic composition comprising acetaminophen and a matrix formed from granulations mixed with HEC and PVP.
- The process of making this composition, including the steps of granulating, drying, milling, blending, and compressing.
- The specific ratios of active to inactive ingredients, ensuring a controlled release profile[1].
Dependent Claims
Dependent claims further specify the composition and process, including:
- The use of a bi-layer tablet with both immediate and sustained release layers.
- The precise weight percentages of acetaminophen and inactive ingredients.
- The method of using two polymers (HEC and PVP) to achieve the desired release profile[1].
Patent Landscape
Related Patents
The patent landscape surrounding US 4,968,509 includes other innovations in sustained-release formulations and pharmaceutical technologies. For example:
- Patents like US 7,858,609B2 focus on different active ingredients and formulations, such as ganaxolone, but share similarities in the use of advanced delivery systems[2].
Competitive Analysis
The competitive landscape in pharmaceuticals, especially in pain management and analgesics, is highly competitive. Companies like McNeil (the manufacturer of Tylenol) have multiple patents covering various aspects of their products. The '509 patent provides a unique position in the market by offering a sustained-release formulation of acetaminophen, which can differentiate it from immediate-release products[5].
Intellectual Property Strategy
Claim Coverage Matrix
To fully leverage the '509 patent, a Claim Coverage Matrix can be used to analyze which patents and claims are actively protecting the intellectual property. This tool helps in identifying gaps or opportunities in the patent portfolio and ensures that the claims cover the intended technology[3].
Scope Concepts
Categorizing patents by scope concepts, such as the use of specific polymers or the process of granulation, can provide a powerful tool for filtering and analyzing large numbers of patent claims. This approach helps in determining the value of the patent claims and identifying future design opportunities[3].
Impact on the Pharmaceutical Industry
Market Domination
The sustained-release formulation of acetaminophen has significant market implications. It offers patients a more convenient dosing regimen, reducing the need for frequent dosing and potentially improving compliance. This can lead to market dominance for products utilizing this technology.
Regulatory Considerations
Regulatory bodies closely monitor pharmaceutical formulations to ensure safety and efficacy. The '509 patent's detailed process and composition ensure compliance with regulatory standards, making it easier to bring the product to market.
Key Takeaways
- Sustained Release Technology: The patent introduces a novel sustained-release formulation of acetaminophen, enhancing patient compliance and convenience.
- Unique Composition: The use of HEC and PVP as granulating agents and excipients allows for a controlled release profile.
- Process Innovation: The detailed process of granulating, drying, milling, blending, and compressing ensures consistent product quality.
- Intellectual Property: The patent provides strong intellectual property protection, allowing for differentiation in a competitive market.
- Regulatory Compliance: The formulation and process comply with regulatory standards, facilitating market approval.
FAQs
What is the main innovation of US 4,968,509?
The main innovation is the development of a sustained-release formulation of acetaminophen using a matrix formed from granulations mixed with hydroxyethyl cellulose (HEC) and Povidone U.S.P. (PVP).
What are the key components of the sustained-release matrix?
The key components include acetaminophen (68% to 94% by weight) and inactive ingredients such as granulating agents and excipients (6% to 32% by weight).
How does the process of making the sustained-release composition differ from other formulations?
The process involves granulating acetaminophen with PVP, drying, milling, blending with additional excipients, and then compressing the mixture into a tablet, allowing for a controlled release profile.
What is the significance of using HEC and PVP in the formulation?
The use of HEC and PVP as granulating agents and excipients enables the controlled release of acetaminophen over a sustained period.
How does this patent impact the pharmaceutical industry?
The patent introduces a more convenient dosing regimen, potentially improving patient compliance and giving products using this technology a competitive edge in the market.
Sources
- US4968509A - Oral sustained release acetaminophen formulation and process - Google Patents
- US7858609B2 - Solid ganaxolone formulations and methods for the making and use thereof - Google Patents
- Patent Analytics | Intellectual Property Law - SLWIP
- US9439866.pdf - Google Patents
- CV 5471 - Patently-O - Patently-O
