Last updated: August 4, 2025
Introduction
The patent CN103781413, titled "A pharmaceutical composition comprising a core-shell microsphere containing a proton pump inhibitor and a method of preparing the same," exemplifies innovation within the pharmaceutical delivery systems domain, especially targeting proton pump inhibitors (PPIs). This analysis delves into the patent's scope, claims, and the broader patent landscape in China surrounding similar formulations, providing strategic insights for stakeholders involved in drug development, licensing, and patent filing.
Scope of Patent CN103781413
1. Patent Overview
CN103781413 protects an innovative drug delivery system—core-shell microspheres—encapsulating PPIs for improved pharmacokinetics and patient compliance. The patent emphasizes the technical aspects of formulating microspheres with specific core-shell structures, designed to enhance stability, bioavailability, and controlled release of PPIs.
2. Geographical and Technical Scope
- Geographical Scope: Limited to China, aligning with Chinese patent law regulations.
- Technical Scope: Concerns pharmaceutical composition design, microsphere fabrication techniques, drug encapsulation methods, and specific formulation parameters related to PPIs (e.g., omeprazole, esomeprazole).
3. Patent Duration and Term
Filing date: August 16, 2013
Grant date: October 29, 2014
Patent term: 20 years from the filing date, i.e., until August 16, 2033, subject to maintenance fee payments.
Claims Analysis
1. Main Claims
The core claims define the inventive core-shell microsphere composition, emphasizing:
- Component composition: The core comprises a PPI or its derivative; the shell is a polymeric material that controls drug release.
- Preparation method: A specific process involving coacervation or emulsification techniques for achieving the core-shell structure.
- Structural characteristics: Particular dimensions, core-to-shell ratios, or polymer compositions that influence release kinetics.
- Pharmacological advantages: Improved stability against gastric acid, sustained release properties, and enhanced bioavailability.
2. Dependent Claims
These claims specify features such as:
- The type of polymers used, e.g., biodegradable polymers like polylactic acid.
- Specific preparation conditions, such as temperature ranges, solvents, or emulsifier concentrations.
- Variations in particle size and coating thickness.
- Use-specific claims for treating gastric conditions, peptic ulcers, or GERD.
3. Claim Interpretation
The claims are primarily product-by-process, defining the microspheres through their structure, composition, and preparation method. The specific combination of components and process steps aims to create a monopoly over a particular drug delivery platform for PPIs in China.
4. Claim Breadth and Potential Infringement
The language used appears to balance breadth—covering a range of polymers and preparation methods—and specificity—details on the core-shell ratio and fabrication techniques to prevent workarounds. This design minimizes competitors' ability to replicate the invention without infringing.
Patent Landscape in China for PPI-Loaded Microspheres
1. Patent Filings and Grants
The Chinese patent landscape for PPI delivery formulations has grown significantly over the past decade, driven by the high demand for innovative gastrointestinal drug delivery systems. Noteworthy points include:
- Several patents focusing on multiparticulate systems, microcapsules, and controlled-release formulations.
- CN103781413 fits within a subset of patents emphasizing core-shell microspheres with tailored drug release profiles.
2. Major Patent Filers and Assignees
- Large Pharmaceutical Companies: Shandong Xinhua Pharmaceutical, Hainan Wuzhishan Pharmaceutical, Hengyuan Pharmaceutical—actively filing related formulations.
- Research Institutions: Chinese Academy of Sciences, Tianjin Medical University—contributing to foundational and incremental innovations.
- Emerging Biotech Startups: Innovating in nanoparticle or microsphere manufacturing techniques.
3. Patent Clusters and Trends
- A focus on biodegradable polymers for microsphere shells.
- Increasing filings on targeted delivery and controlled-release PPI formulations.
- Combining microsphere technology with other drug delivery systems, such as liposomes or nanocarriers.
4. Competitive Positioning
CN103781413’s claims position it well within the infringeable space against competitors developing PPI microsphere formulations—especially those employing similar core-shell architectures and preparation methods.
Legal and Commercial Implications
1. Patent Strengths
- Well-defined fabrication process conferring patentability and enforceability.
- Focused claims aligned with specific technical solutions bolster patent durability.
- Extended patent life until 2033 provides a substantial market exclusivity window.
2. Potential Challenges and Workarounds
- Prior art exists for microsphere-based drug delivery, necessitating ongoing patent landscape vigilance.
- Competitors may develop alternative formulations with different polymers or preparation methods, avoiding infringement.
3. Commercial Opportunities
- The patent supports licensing negotiations, potential spin-offs, or in-house product development.
- Patent’s local scope means exclusivity within China, yet competitors may seek international patent protections.
Conclusion
CN103781413 secures a strategic position in the Chinese patent landscape by protecting an innovative PPI-loaded core-shell microsphere system. Its claims encompass specific composition and fabrication techniques that balance breadth and enforceability. The patent landscape indicates a competitive environment with multiple players advancing proprietary controlled-release and microsphere technologies, emphasizing the importance of continuous innovation and diligent IP management.
Key Takeaways
- Scope Precision: The patent’s claims focus on specific core-shell microsphere structures for PPIs, allowing robust protection while leaving room for alternative formulations.
- Landscape Positioning: It is part of a growing trend in China toward microsphere-based drug delivery, with strong activity from both academia and industry.
- Strategic Importance: Patent CN103781413 offers a solid foundation for commercialization within China, potentially serving as a platform for international patent applications.
- Legal Safety: Clear claims reduce infringement risks while demanding vigilance regarding evolving prior art.
- Future Directions: Staying abreast of new filings on similar technologies is crucial to maintain patent strength and market competitiveness.
FAQs
Q1: Can the claims in CN103781413 be extended internationally?
A1: No; patents are territorial. To extend protection, the applicant must file corresponding applications in other jurisdictions, such as PCT or regional patent offices.
Q2: How does this patent protect against generic competition?
A2: Its specific claims on formulation, preparation process, and particle structure create a legal barrier to generic entrants attempting to replicate the exact microsphere technology.
Q3: Are there potential infringement risks?
A3: Yes, competitors developing similar core-shell microspheres with comparable features must carefully analyze claim scope to avoid infringement, especially regarding polymers and preparation methods.
Q4: What are the key advantages of this core-shell microsphere delivery system?
A4: Enhanced stability in gastric conditions, controlled release for prolonged therapeutic effect, and improved patient compliance.
Q5: How should patentees monitor the landscape for similar innovations?
A5: Regular patent landscaping and prior art searches focused on microsphere and controlled-release formulations within Chinese and international databases.
References
[1] Chinese Patent CN103781413, Title: A pharmaceutical composition comprising a core-shell microsphere containing a proton pump inhibitor and a method of preparing the same.
[2] Chinese Patent Database. (2023). Search reports on PPI delivery systems.
[3] WIPO. (2022). Patent landscapes for controlled-release drug delivery systems.
[4] World Intellectual Property Organization. (2021). Patent trends for pharmaceutical delivery technologies.
