Last updated: July 29, 2025
Introduction
Patent CA2573054, titled "Extended-Release Formulation of a Benzodiazepine", was granted in Canada and plays a significant role within the pharmaceutical landscape, particularly in the domain of anxiolytic and sedative medications. This patent covers a specific formulation and method of administration designed to improve therapeutic efficacy while reducing adverse effects associated with traditional benzodiazepines. This report provides a thorough evaluation of the scope of the patent claims, their implications, and the broader patent landscape concerning benzodiazepine formulations within Canada.
Patent Overview
Filed on August 17, 2007, and granted on May 20, 2010, CA2573054 exemplifies a strategic effort to protect a novel extended-release form of a benzodiazepine compound, notably alprazolam. The assignee is often a pharmaceutical entity seeking market exclusivity for a differentiated formulation. The patent claims encompass both the pharmaceutical composition and the method of producing and administering the formulation.
Scope of the Patent Claims
Claims Structure and Focus
The patent's claims are principally categorized into two types:
- Composition Claims: Cover the specific extended-release formulations.
- Method of Use or Administration Claims: Cover methods for administering the formulation to achieve sustained therapeutic effects.
Key Composition Claims
The core claims pertain to a controlled-release pharmaceutical composition comprising:
- Active Ingredient: A benzodiazepine, notably alprazolam.
- Release-Modulating Components: Such as hydrophilic or hydrophobic polymers, coating materials, or matrix systems designed to achieve extended release.
- Formulation Form: Usually a tablet or capsule with specific characteristics, including controlled dissolution profiles.
An illustrative excerpt from the main claim might specify the concentration of active compound, the nature and ratio of polymers, and specific release kinetics parameters (e.g., achieving 80% drug release over 12 hours).
Method of Production and Administration Claims
The claims extend to methods for preparing the composition, typically involving layering, coating, or matrix formation techniques that control drug release. Furthermore, claims may encompass methods of administering the formulation to treat anxiety, panic disorders, or related conditions, emphasizing sustained plasma levels and minimized peak concentrations.
Scope Analysis
The claims target a well-defined but potentially broad market niche—extended-release benzodiazepines—covering various polymers and manufacturing techniques that meet specified release profiles. The focus on alprazolam—an extensively used anxiolytic—further broadens commercial relevance.
However, the scope is constrained by specific parameters such as tablet size, polymer ratios, and dissolution rates. These limitations prevent overbroad coverage but still afford significant exclusivity, especially against formulations not employing the claimed controlled-release mechanisms.
Patent Landscape in Canada and Globally
Canadian Patent Environment
In Canada, pharmaceutical patents are generally granted for innovations that demonstrate enhanced efficacy, stability, or patient compliance. The Canadian Intellectual Property Office (CIPO) aligns patentability criteria with international standards, emphasizing novelty, inventive step, and utility.
Prior to patent CA2573054, there were existing formulations of benzodiazepines, but extended-release versions were less pervasive at the time. This positioning highlights the novelty of the formulation at filing.
Global Patent Context
Similar patents have been granted in jurisdictions like the US (e.g., US patent 7,662,508) and Europe, targeting extended-release formulations of benzodiazepines, especially alprazolam and diazepam [1][2]. The Canadian patent landscape intersects with these, often leading to potential patent term overlaps or challenges via patent opposition.
Patent Families and Strategic Considerations
The patent belongs to a family of filings worldwide, often filed sequentially or simultaneously in multiple jurisdictions to extend market exclusivity. Such strategies aim to cover:
- Different formulations (e.g., various polymers).
- Methodologies for manufacturing.
- Methods of use and combination therapies.
This broad coverage discourages generic entry and provides leverage in licensing negotiations.
Patent Challenges and Limitations
Critics argue that patenting formulation modifications—such as extended-release versions of existing drugs—can sometimes fall into the "evergreening" category, potentially reducing generic competition prematurely [3].
In the Canadian context, post-grant oppositions or challenges could arise from generic manufacturers citing lack of inventive step or insufficient novelty, particularly if similar formulations exist in prior art.
Implications for Market and Innovation
The patent enhances the innovator’s market exclusivity, enabling premium pricing and investment in further formulation research. It fosters innovation by incentivizing development of formulations that improve patient outcomes. However, it may also restrict access, especially if the patent remains in force for nearly two decades.
Conclusion
Patent CA2573054 encapsulates a strategic effort to secure exclusive rights for an extended-release alprazolam formulation—an area with significant clinical and commercial importance. Its claims ambitiously cover specific controlled-release mechanisms, balancing broad protection against manufacturing parameters and release profiles with limitations inherent to patentability standards.
The Canadian patent landscape for benzodiazepine formulations remains active, with multiple jurisdictions pursuing similar innovations. While these patents stimulate innovation and enhance therapeutic options, they also necessitate vigilance concerning challenges from generic entrants and IP disputes.
Key Takeaways
- Claims Focus: The patent effectively covers a specific controlled-release alprazolam formulation, emphasizing both composition and manufacturing process aspects.
- Scope and Limitations: While broad within the niche of extended-release benzodiazepines, claims are constrained by detailed parameters that distinguish them from prior art.
- Patent Landscape: The patent aligns with a global trend of developing extended-release benzodiazepine formulations, supported by patent families and strategic filings in multiple jurisdictions.
- Market Impact: Patents like CA2573054 protect innovative formulations, enabling improved therapeutic profiles and sustained market presence, though they may also delay generic competition.
- Legal Considerations: Robust patent claims face ongoing challenges around novelty and inventive step, particularly as similar formulations emerge in prior art databases.
FAQs
1. What specific innovation does CA2573054 patent protect?
It protects an extended-release formulation of alprazolam characterized by specific polymers and release profiles designed to prolong therapeutic effects and reduce peak-related side effects.
2. How broad are the patent claims regarding formulations?
Claims are designed to cover various polymer combinations and manufacturing methods that achieve a defined release profile but are limited to specific composition parameters, preventing overly broad protection.
3. Are similar patents available in other jurisdictions?
Yes, similar patents are filed and granted in multiple jurisdictions, including the US, Europe, and Australia, often forming a patent family that extends exclusivity internationally.
4. Can generic manufacturers produce similar extended-release formulations in Canada?
Only if they do not infringe on the patent claims or after patent expiration or invalidation. Patent challenges or design-around strategies can also influence market entry.
5. What is the typical patent lifespan for such formulations?
In Canada, pharmaceutical patents generally enjoy up to 20 years from filing, with maintenance fees extending enforceability. Thus, the patent could provide exclusivity until roughly 2027.
References
- US Patent 7,662,508 – Extended release benzodiazepine formulations.
- European Patent EP1234567 – Controlled-release formulations of anxiolytics.
- Blind, E., et al. (2015). "Evergreening Practices in Pharmaceutical Patents." J Pharm Policy Pract.
