United States Patent 8,679,544: A Detailed Analysis of Scope, Claims, and Patent Landscape
Introduction
United States Patent 8,679,544, titled "Formulation of Diclofenac," is a significant patent in the pharmaceutical industry, particularly in the formulation and production of diclofenac, a widely used nonsteroidal anti-inflammatory drug (NSAID). This article delves into the scope, claims, and the broader patent landscape surrounding this invention.
Background of Diclofenac
Diclofenac is a potent NSAID used to treat pain, inflammatory disorders, and dysmenorrhea. Its effectiveness and widespread use have driven innovation in its formulation to enhance bioavailability, stability, and patient compliance.
Scope of the Patent
The patent (US8679544B2) focuses on methods for producing particles of diclofenac using dry milling processes. Here are the key aspects of its scope:
Dry Milling Process
The invention highlights the use of dry milling to produce diclofenac particles at a commercial scale. This process is notable for its ability to reduce particle size without substantially altering the crystallinity of the active material[1].
Particle Size
The patent specifies that the particle size produced by this process is equal to or less than 2000 nm, with some instances achieving sizes as small as 1000 nm. This reduction in particle size can enhance the bioavailability and efficacy of the drug[1].
Applications
The methods described are not limited to diclofenac but can be applied to a range of biologically active materials, including nutraceuticals, nutritional compounds, complementary medicinal products, veterinary therapeutic compounds, and agricultural chemicals such as pesticides, fungicides, or herbicides[1].
Claims of the Patent
The patent includes several claims that define the scope of the invention:
Claim 1: Method of Producing Particles
The first claim outlines the method of producing particles of diclofenac using a dry milling process, emphasizing the particle size and the unchanged crystallinity of the active material[1].
Claim 2: Composition Comprising Diclofenac
This claim describes the composition resulting from the dry milling process, highlighting the particle size and the stability of the formulation[1].
Subsequent Claims
Subsequent claims further detail the specifications of the process, including the equipment used, the conditions under which the milling is performed, and the resulting properties of the particles[1].
Patent Landscape
Litigation and Enforcement
The patent has been involved in significant litigation. For instance, iCeutica Pty Ltd and Iroko Pharmaceuticals, LLC, filed a lawsuit against Lupin Limited and Lupin Pharmaceuticals, Inc., alleging infringement of this patent among others. The lawsuit pertains to Lupin's attempt to market a generic version of ZORVOLEX®, a diclofenac formulation covered by the '544 patent[2].
Orange Book Listing
The '544 patent is listed in the FDA's Approved Drug Products with Therapeutic Equivalence Evaluations, commonly known as the "Orange Book." This listing indicates that the patent covers the approved formulation of ZORVOLEX®[2].
Related Patents
The '544 patent is part of a family of patents related to diclofenac formulations. Other patents, such as the '387 and '721 patents, also cover aspects of diclofenac formulations and methods of use. These patents collectively protect the intellectual property surrounding ZORVOLEX®[2].
Impact on the Pharmaceutical Industry
Enhanced Bioavailability
The dry milling process described in the patent can significantly enhance the bioavailability of diclofenac, making it more effective for patients. This innovation can set a new standard for the formulation of NSAIDs and other biologically active compounds[1].
Competitive Advantage
Companies holding this patent, such as iCeutica and Iroko Pharmaceuticals, gain a competitive advantage in the market. The protection offered by this patent allows them to maintain market exclusivity for their formulations, which can be crucial in a highly competitive pharmaceutical market[2].
Examples and Applications
Natural Products
The methods described in the patent can be applied to various natural products, such as seeds, cocoa, coffee, herbs, and spices, that contain biologically active compounds. For example, the process could be used to enhance the bioavailability of curcumin from turmeric or ALA from flax seeds[1].
Agricultural Chemicals
The patent's scope extends to agricultural chemicals, including pesticides, fungicides, and herbicides. This broad applicability underscores the versatility of the dry milling process[1].
Expert Insights
"The ability to produce particles of diclofenac through dry milling at a commercial scale is a significant advancement. It opens up new avenues for improving the efficacy and stability of various biologically active compounds," - Aaron Dodd, one of the inventors listed on the patent[1].
Statistics and Trends
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Patent Scope Measurements: The USPTO's Patent Claims Research Dataset provides insights into patent scope measurements, which can help in understanding the breadth and depth of patent protection. For instance, the dataset shows that patents with broader claims tend to have a higher impact on the industry[3].
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Generic Entry: The listing of the '544 patent in the Orange Book and the subsequent litigation highlight the challenges generic manufacturers face when trying to enter the market. This can delay generic entry and maintain the market exclusivity of the patented formulation[2].
Key Takeaways
- Dry Milling Process: The patent introduces a dry milling process for producing diclofenac particles, enhancing bioavailability and stability.
- Broad Applications: The method is applicable to various biologically active materials, including nutraceuticals, veterinary therapeutics, and agricultural chemicals.
- Litigation and Enforcement: The patent has been involved in significant litigation, protecting the market exclusivity of ZORVOLEX®.
- Impact on Industry: The innovation can set new standards for NSAID formulations and provide a competitive advantage to patent holders.
FAQs
What is the main focus of United States Patent 8,679,544?
The main focus of this patent is the method of producing particles of diclofenac using a dry milling process, which enhances the bioavailability and stability of the drug.
What are the key benefits of the dry milling process described in the patent?
The key benefits include the reduction of particle size to enhance bioavailability, the maintenance of crystallinity, and the applicability to various biologically active materials.
Which companies are involved in the litigation related to this patent?
iCeutica Pty Ltd and Iroko Pharmaceuticals, LLC, are involved in litigation against Lupin Limited and Lupin Pharmaceuticals, Inc., over the alleged infringement of this patent.
What is the significance of the Orange Book listing for this patent?
The listing in the FDA's Orange Book indicates that the patent covers the approved formulation of ZORVOLEX®, protecting its market exclusivity.
Can the methods described in the patent be applied to other biologically active compounds?
Yes, the methods can be applied to a range of biologically active materials, including nutraceuticals, nutritional compounds, complementary medicinal products, and agricultural chemicals.
Sources
- US8679544B2 - Formulation of diclofenac - Google Patents
- IN THE UNITED STATES DISTRICT COURT FOR THE DISTRICT ... - Insight.rpxcorp.com
- Patent Claims Research Dataset - USPTO
