Detailed Analysis of the Scope and Claims of United States Patent 8,097,651
Introduction
United States Patent 8,097,651, titled "Diclofenac formulations and methods of use," is a significant patent in the pharmaceutical industry, particularly for the treatment of migraine and other acute pain episodes. This patent, assigned to APR Applied Pharma Research s.a., outlines innovative formulations and methods for using diclofenac, a nonsteroidal anti-inflammatory drug (NSAID).
Patent Overview
The patent was issued on January 17, 2012, and is set to expire on June 16, 2026[2][4].
Claims and Scope
Formulations
The patent describes various formulations of diclofenac designed to provide both rapid and sustained relief from acute pain. These formulations include:
- Oral Formulations: The patent specifies oral formulations containing about 50 mg of diclofenac or its pharmaceutically acceptable salt. These formulations are designed to achieve a maximum plasma concentration (C max) of 1400 to 2500 ng/ml and a time to reach maximum plasma concentration (t max) of 10 to 35 minutes[4].
- Liquid and Powder Forms: The formulations can be administered as a liquid for oral ingestion or as a powder sachet that is mixed with water before administration. They can also be provided in unit dose vials or as a drop formulation[4].
Methods of Use
The patent details methods for treating acute pain, including migraine, using these diclofenac formulations. Key aspects include:
- Administration Frequency: The formulation is administered no more than three times in a 24-hour period, with dosing intervals of 2, 4, 6, or 8 hours as needed for pain[4].
- Symptom Relief: The methods also address symptoms that often accompany migraine and acute pain, such as photophobia, phonophobia, nausea, and vomiting[2][4].
Pharmacokinetics
The patent emphasizes the importance of achieving specific pharmacokinetic parameters to ensure effective pain relief. This includes:
- C max and t max: The formulations are designed to achieve a C max of 1400 to 2500 ng/ml and a t max of 10 to 35 minutes. This rapid onset and sustained release profile is crucial for providing immediate and prolonged pain relief[4].
Advantages
The formulations and methods described in the patent offer several advantages:
- Reduced Medication Requirements: The sustained relief provided by these compositions decreases the need for additional pain medications, making it more convenient and potentially reducing side effects[4].
- Convenience: The oral formulations, especially the liquid and powder forms, offer ease of administration, which is particularly beneficial for patients experiencing acute pain[4].
Patent Landscape
Related Patents
The patent is part of a series of patents related to diclofenac formulations and methods of use. Other relevant patents include:
- Patent 7,759,394: Also related to diclofenac formulations and methods, with similar expiration dates[2].
- Patent 8,927,604: Issued in 2015, this patent further elaborates on the methods and formulations for treating migraine and acute pain using diclofenac[2].
- Patent 9,827,197: Issued in 2017, this patent continues the development of diclofenac formulations with a focus on specific pharmacokinetic profiles[2].
Generic Availability
As of 2024, a generic version of Cambia, a product covered by this patent, has been approved by the FDA. However, commercial availability is not guaranteed until the patent expires or other market conditions are met[2].
Patent Expiration and Generic Entry
The patent is set to expire on June 16, 2026. After this date, generic versions of the diclofenac formulations described in the patent can enter the market, provided they meet the necessary bioequivalence requirements[2].
Impact on Innovation and Competition
The patent's scope and claims have significant implications for innovation and competition in the pharmaceutical industry:
- Innovation: The patent encourages the development of new formulations and methods that improve upon existing treatments for acute pain and migraine.
- Competition: The expiration of the patent will open the market to generic competitors, potentially reducing costs and increasing accessibility of these treatments[3].
Conclusion
United States Patent 8,097,651 is a critical patent in the field of pain management, particularly for migraine and acute pain. Its claims and scope define specific formulations and methods of using diclofenac that offer rapid and sustained relief. As the patent landscape evolves, the expiration of this patent will likely lead to increased competition and potentially more affordable treatments.
Key Takeaways
- The patent covers diclofenac formulations for treating migraine and acute pain.
- Formulations are designed for rapid and sustained pain relief.
- Specific pharmacokinetic parameters are crucial for effectiveness.
- The patent expires on June 16, 2026, allowing for generic entry thereafter.
- The patent encourages innovation and will impact competition in the pharmaceutical market.
FAQs
What is the primary focus of United States Patent 8,097,651?
The primary focus is on diclofenac formulations and methods for treating migraine and other acute pain episodes.
What are the key pharmacokinetic parameters for the diclofenac formulations described in the patent?
The formulations aim to achieve a C max of 1400 to 2500 ng/ml and a t max of 10 to 35 minutes.
How often can the diclofenac formulation be administered according to the patent?
The formulation can be administered no more than three times in a 24-hour period, with dosing intervals of 2, 4, 6, or 8 hours as needed for pain.
What are the advantages of the diclofenac formulations described in the patent?
The formulations provide rapid and sustained pain relief, reducing the need for additional pain medications and offering convenience in administration.
When is the patent set to expire?
The patent is set to expire on June 16, 2026.
Cited Sources
- US8097651B2 - Diclofenac formulations and methods of use - Google Patents.
- Generic Cambia Availability - Drugs.com.
- Patent Claims and Patent Scope - Hoover Institution.
- US8097651B2 - Diclofenac formulations and methods of use - Google Patents.
- Pharmaceutical drugs covered by patent 8,097,651 - Drug Patent Watch.
