United States Patent 6,977,257: A Detailed Analysis of Scope, Claims, and Patent Landscape
Introduction
The United States Patent 6,977,257, titled "Aripiprazole oral solution," is a significant patent in the pharmaceutical industry, particularly in the field of psychiatric medications. This patent, granted on December 20, 2005, pertains to the formulation and composition of an oral solution of aripiprazole, a medication used to treat schizophrenia, bipolar disorder, and other psychiatric conditions.
Background of the Invention
Aripiprazole, a partial agonist at the dopamine D2 and serotonin 5-HT1A receptors, is commonly administered in tablet or oral solution forms. The patent addresses the need for a stable and effective oral solution formulation of aripiprazole, which is crucial for patient compliance and therapeutic efficacy[4].
Scope of the Patent
The scope of the patent is broad and encompasses various embodiments of the pharmaceutical solution.
Concentrations of Aripiprazole
The patent specifies different concentrations of aripiprazole in the oral solution, ranging from 0.75 mg/ml to 1.5 mg/ml, with a specific embodiment at 1 mg/ml. This variability allows for tailored dosing regimens to suit different patient needs[1][4].
Pharmaceutically Suitable Solvent Systems
The patent describes several solvent systems that can be used:
- Water alone
- Water with one or more surfactants
- Water with one or more solubilizing agents
- Water with one or more water-miscible solvents (such as ethanol, glycerin, propylene glycol, sorbitol, polyethylene glycols, and polyvinylpyrrolidone)
- Combinations of these components[1][4].
Sweeteners and Flavoring Agents
The patent also includes embodiments with various sweeteners and flavoring agents to enhance palatability. These include natural sweeteners (e.g., sucrose, fructose, dextrose), semi-synthetic sweeteners, and synthetic sweeteners[1].
Claims of the Patent
The patent contains multiple claims that define the scope of the invention.
Independent Claims
The independent claims focus on the composition of the pharmaceutical solution, including the concentration of aripiprazole and the types of solvent systems used. For example, Claim 1 describes a pharmaceutical solution comprising aripiprazole in a concentration of 1 mg/ml in a solvent system that includes water and one or more surfactants or solubilizing agents[4].
Dependent Claims
Dependent claims further specify the components and their combinations, such as the use of specific sweeteners, flavoring agents, and preservatives. These claims build upon the independent claims to provide a detailed description of the various embodiments of the invention[4].
Patent Landscape
Related Patents and Applications
The patent landscape for aripiprazole oral solutions includes other patents and applications related to formulations, delivery systems, and methods of use. For instance, provisional application U.S. Ser. No. 60/286,718, filed on April 25, 2001, is cited as a priority application, indicating a continuum of research and development in this area[5].
Patent Scope Metrics
Research on patent scope, such as the work by Marco, Sarnoff, and deGrazia, highlights the importance of metrics like independent claim length and independent claim count in assessing patent breadth. These metrics can indicate the complexity and specificity of the patent claims, which in turn affect the patent's validity and enforcement[3].
Impact on the Pharmaceutical Industry
The patent has significant implications for the pharmaceutical industry:
Patient Compliance
The availability of an oral solution formulation of aripiprazole enhances patient compliance, especially for those who have difficulty swallowing tablets. This formulation can be particularly beneficial for pediatric and geriatric patients[1].
Therapeutic Efficacy
The stable and effective formulation ensures consistent therapeutic efficacy, which is crucial for managing psychiatric conditions. The variability in concentrations and solvent systems allows for personalized treatment plans[1].
Competitive Landscape
The patent protects the specific formulations and compositions described, providing a competitive advantage to the patent holder. This can influence market dynamics and innovation in the field of psychiatric medications[4].
Legal and Regulatory Considerations
Patent Expiration
The patent has expired, which means that the protected formulations and compositions are now in the public domain. This expiration can lead to the development of generic versions of the oral solution, potentially increasing accessibility and reducing costs for patients[4].
Litigation and Licensing
The expiration of the patent also reduces the likelihood of litigation related to patent infringement. However, during its active period, the patent would have been a significant factor in licensing agreements and litigation strategies within the pharmaceutical industry[3].
Key Takeaways
- Formulation Variability: The patent covers a range of concentrations and solvent systems for aripiprazole oral solutions.
- Patient Compliance: The oral solution formulation enhances patient compliance, especially for those with difficulty swallowing tablets.
- Therapeutic Efficacy: The stable and effective formulation ensures consistent therapeutic efficacy.
- Competitive Advantage: The patent provided a competitive advantage during its active period.
- Public Domain: The patent has expired, allowing for the development of generic versions.
FAQs
What is the primary focus of United States Patent 6,977,257?
The primary focus is on the formulation and composition of an oral solution of aripiprazole for psychiatric medications.
What are the different concentrations of aripiprazole covered by the patent?
The concentrations range from 0.75 mg/ml to 1.5 mg/ml, with a specific embodiment at 1 mg/ml.
What types of solvent systems are described in the patent?
The solvent systems include water alone, water with surfactants, solubilizing agents, water-miscible solvents, and combinations thereof.
Why is the oral solution formulation important?
It enhances patient compliance, especially for those who have difficulty swallowing tablets, and ensures consistent therapeutic efficacy.
Has the patent expired?
Yes, the patent has expired, allowing the formulations and compositions to enter the public domain.
Sources
- United States Patent and Trademark Office, "United States Patent 6,977,257 B2," April 24, 2002.
- USPTO, "Patent Claims Research Dataset," August 28, 2017.
- SSRN, "Patent Claims and Patent Scope," September 29, 2016.
- Google Patents, "US6977257B2 - Aripiprazole oral solution," December 20, 2005.
- Justia Patents, "US Patent for Aripiprazole oral solution," December 20, 2005.
