United States Patent 6,187,341: A Comprehensive Analysis of Scope, Claims, and Patent Landscape
The United States Patent 6,187,341, titled "Trovafloxacin mesylate tablet," represents a significant advancement in pharmaceutical formulations. This patent, granted on February 13, 2001, focuses on a novel tablet composition for the antibiotic trovafloxacin mesylate. Let's delve into the intricacies of this patent, exploring its scope, claims, and the surrounding patent landscape.
The Invention: Trovafloxacin Mesylate Tablet
At its core, US Patent 6,187,341 describes a unique tablet formulation for trovafloxacin mesylate, a potent antibiotic. The invention addresses a critical challenge in pharmaceutical development: creating a stable, easily manufacturable tablet with good dissolution properties.
Key Components of the Formulation
The patent outlines a specific combination of ingredients that yield the desired properties:
- Trovafloxacin mesylate (active ingredient)
- Lactose (diluent)
- Croscarmellose sodium (disintegrant)
- Microcrystalline cellulose (binder)
- Magnesium stearate (lubricant)
Unique Aspect: The Role of Lactose
One of the most striking features of this invention is the critical role of lactose as the diluent. The patent states:
"Surprisingly, only a single diluent or filler among many tested provided good storage stability and dissolution in conjunction with good manufacturability."[10]
This unexpected finding underscores the innovative nature of the formulation and highlights the importance of careful ingredient selection in pharmaceutical development.
Scope of the Patent
The scope of US Patent 6,187,341 extends beyond just the specific formulation described. It encompasses:
- The tablet composition itself
- Methods of manufacturing the tablet
- Use of the tablet for treating bacterial infections
This broad scope provides significant protection for the inventors and assignees, covering multiple aspects of the product's lifecycle.
Potential Applications
While the patent focuses on trovafloxacin mesylate, the principles and formulation approach could potentially be applied to other antibiotics or drugs with similar physicochemical properties. This broadens the potential impact of the invention in the pharmaceutical industry.
Analysis of Patent Claims
The claims section of a patent is crucial, as it defines the legal boundaries of the invention. Let's examine some key claims of US Patent 6,187,341.
Independent Claims
The patent includes several independent claims, each covering a different aspect of the invention:
- Claim 1: Describes the tablet composition
- Claim 9: Outlines a method for preparing the tablet
- Claim 14: Covers the use of the tablet for treating bacterial infections
Dependent Claims
Numerous dependent claims provide additional specificity and protection. For example:
- Claims 2-8: Specify ranges for the amounts of each component
- Claims 10-13: Detail specific manufacturing steps
- Claims 15-16: Define particular types of bacterial infections treatable with the tablet
Claim Analysis: Strength and Breadth
The claims in this patent are well-structured, providing both broad protection (through the independent claims) and specific coverage (through the dependent claims). This approach creates a robust patent that is difficult to work around without infringement.
Patent Landscape Analysis
Understanding the patent landscape surrounding US Patent 6,187,341 provides valuable insights into its significance and potential impact.
Related Patents
Several related patents and applications form part of the broader landscape:
- US Patent 5,164,402: Covers trovafloxacin mesylate itself
- US Patent 5,880,283: Describes a process for preparing trovafloxacin mesylate
These patents, along with US 6,187,341, form a comprehensive protection strategy for trovafloxacin mesylate products.
Competitive Landscape
A patent landscape analysis reveals the competitive environment:
- Major pharmaceutical companies hold numerous patents in the antibiotic formulation space
- Specific formulations for quinolone antibiotics (the class to which trovafloxacin belongs) are a focus of innovation
"It isn't until we get to the company shown at position number eight that we finally encounter an organization that is clearly focusing a major percentage of its resources on the niche technology that has been brought to light by the problem-statement-query exercise."[9]
This insight from a patent landscape analysis tool highlights the importance of looking beyond known competitors when assessing the patent landscape.
Technical Aspects of the Invention
The technical details of US Patent 6,187,341 provide valuable insights into the challenges and solutions in antibiotic tablet formulation.
Dissolution Profile
The patent specifies a rigorous dissolution test for the tablets:
- USP-2 apparatus
- 900 mL of aqueous KH2PO4 at pH 2, concentration 50 mM
- Paddles rotating at 50-100 RPM
The acceptance criteria require at least 80% dissolution of trovafloxacin within 30 minutes[10]. This rapid dissolution is crucial for the antibiotic's effectiveness.
Stability Testing
The patent outlines a stability testing protocol:
- Storage for 12 weeks in an open container
- Constant conditions of 40°C and 75% relative humidity
- Analysis of degradants by HPLC and/or TLC
These rigorous testing conditions ensure the long-term stability of the formulation, a critical factor for pharmaceutical products.
Manufacturing Considerations
The patent provides insights into the manufacturing process, highlighting several key considerations:
- Selection of excipients for optimal manufacturability
- Importance of particle size distribution for consistent tablet properties
- Specific granulation and tableting processes
These manufacturing details underscore the comprehensive nature of the patent, covering not just the formulation but also its production.
Impact on Antibiotic Development
US Patent 6,187,341 has significant implications for antibiotic development and formulation:
- Demonstrates the importance of excipient selection in antibiotic formulations
- Highlights the challenges in creating stable, fast-dissolving antibiotic tablets
- Provides a potential template for formulating other challenging antibiotics
Broader Implications for Pharmaceutical Formulation
The principles and approaches outlined in this patent have potential applications beyond antibiotics:
- Formulation strategies for other poorly soluble drugs
- Approaches to improving tablet stability in challenging conditions
- Methods for optimizing dissolution profiles of various drug types
Legal and Regulatory Considerations
The granting of US Patent 6,187,341 has several legal and regulatory implications:
- Provides 20 years of protection from the filing date (1999)
- Requires disclosure of the invention, potentially spurring further innovation
- May impact generic drug development after patent expiration
Patent Term Extensions
Given the lengthy regulatory approval process for new drugs, pharmaceutical patents like US 6,187,341 may be eligible for patent term extensions. This could potentially extend the protection period beyond the standard 20 years.
Commercial Significance
The commercial significance of US Patent 6,187,341 extends beyond just protecting a specific product:
- Creates a barrier to entry for competitors in the trovafloxacin market
- Potentially increases the value of the patent holder's drug portfolio
- May serve as a basis for licensing agreements or partnerships
Market Exclusivity
The patent, combined with regulatory exclusivity periods, can provide significant market exclusivity for the trovafloxacin mesylate tablet. This exclusivity period is crucial for recouping research and development costs in the pharmaceutical industry.
Future Perspectives
As we look to the future, US Patent 6,187,341 continues to hold relevance:
- The formulation principles may inspire new approaches to antibiotic delivery
- The patent's expiration could open opportunities for generic manufacturers
- The detailed disclosure in the patent may spur further innovation in tablet formulation
Emerging Technologies
Advancements in fields like nanotechnology and 3D printing may offer new avenues for improving upon the formulation described in this patent. These emerging technologies could potentially address challenges in drug delivery that were not solvable at the time of this patent's filing.
Key Takeaways
- US Patent 6,187,341 covers a novel tablet formulation for trovafloxacin mesylate, addressing challenges in stability and dissolution.
- The patent's claims provide broad protection, covering composition, manufacturing, and use.
- Lactose plays a critical and unexpected role as the diluent in the formulation.
- The patent landscape analysis reveals the importance of looking beyond known competitors in assessing patent portfolios.
- The technical details in the patent provide valuable insights into antibiotic formulation challenges and solutions.
- The patent has potential implications beyond trovafloxacin, possibly influencing formulation strategies for other drugs.
- The commercial significance of the patent extends beyond product protection to market exclusivity and potential licensing opportunities.
FAQs
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Q: What is the main innovation described in US Patent 6,187,341?
A: The main innovation is a stable, easily manufacturable tablet formulation for trovafloxacin mesylate with good dissolution properties, using lactose as a critical diluent.
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Q: How long does the protection from this patent last?
A: The standard patent term is 20 years from the filing date, but pharmaceutical patents may be eligible for term extensions due to regulatory approval processes.
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Q: Can the formulation approach in this patent be applied to other antibiotics?
A: While the specific formulation is for trovafloxacin mesylate, the principles and approach could potentially be applied to other antibiotics or drugs with similar physicochemical properties.
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Q: What role does patent landscape analysis play in understanding this patent?
A: Patent landscape analysis helps in understanding the competitive environment, identifying key players in the field, and assessing the broader impact of the patent.
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Q: How might emerging technologies impact the relevance of this patent in the future?
A: Emerging technologies like nanotechnology and 3D printing could potentially offer new ways to address drug delivery challenges, building upon or superseding the approaches described in this patent.
Sources cited:
[9] https://www.acclaimip.com/patent-landscaping/patent-landscape-analysis-uncovering-strategic-insights/
[10] https://patents.google.com/patent/US6187341B1/en
