Last updated: February 19, 2026
What is the Core Invention Claimed in UA126977?
Patent UA126977, granted on October 27, 2023, claims a pharmaceutical composition for treating inflammatory bowel diseases (IBD), specifically Crohn's disease and ulcerative colitis. The invention centers on a novel formulation of mesalazine (5-aminosalicylic acid), an established anti-inflammatory drug. The primary innovation lies in the specific pharmaceutical dosage form and its associated release profile, designed to optimize drug delivery to the colon, the primary site of IBD pathology.
The patent describes a multiparticulate system. This system consists of individual granules or pellets, each coated with a pH-dependent polymer. This coating is designed to remain intact in the acidic environment of the stomach and the alkaline environment of the small intestine. It dissolves only when it reaches the neutral to slightly alkaline pH of the colon, thereby releasing the mesalazine directly into the affected tissues.
The formulation details specified in the patent include:
- Active Pharmaceutical Ingredient: Mesalazine. The patent specifies a dosage range, typically between 1 gram and 4 grams per day for adult patients.
- Core Material: The mesalazine is incorporated into a core, which can be a soluble inert matrix or a matrix that aids in the release of the active ingredient.
- Coating Layer: A pH-dependent enteric coating. The patent identifies specific polymers such as methacrylic acid copolymers (e.g., Eudragit L, S), cellulose derivatives (e.g., hydroxypropyl methylcellulose phthalate), or polyvinyl acetate phthalate. The key characteristic is that the coating has a dissolution pH of approximately 6.0 or higher, ensuring release in the colon.
- Dosage Form: The multiparticulate system is typically formulated into capsules or tablets for oral administration.
The claimed benefit of this formulation is improved therapeutic efficacy due to targeted delivery, reduced systemic absorption, and consequently, a lower incidence of dose-dependent side effects often associated with mesalazine, such as gastrointestinal upset.
What are the Key Claims and Their Specificity?
The patent's claims are structured to protect the novel formulation and its method of use. The core claims define the composition and its functional characteristics.
Claim 1 (Independent Claim for Composition): This is the central claim. It defines the pharmaceutical composition as comprising:
- A plurality of medicament particles, wherein each particle comprises mesalazine.
- A coating applied to each medicament particle, wherein the coating is a pH-dependent release coating that is insoluble at pH values below 6.0 and soluble at pH values of 6.0 or higher.
This claim is broad enough to cover various methods of creating the medicament particles (e.g., extrusion-spheronization, layering) and specific types of pH-dependent polymers, provided they meet the solubility threshold.
Dependent Claims: These claims further refine and narrow the scope of the independent claims by adding specific limitations. Examples include:
- Claim 2: Specifies that the medicament particles are in the form of granules or pellets.
- Claim 3: Details the pH-dependent release coating, listing examples of suitable polymers such as methacrylic acid copolymers.
- Claim 4: Defines the dissolution pH range of the coating more precisely, for example, between 6.0 and 7.0.
- Claim 5: States that the composition is formulated as a capsule or tablet.
- Claim 6: Claims a method of treating inflammatory bowel diseases by administering the claimed composition. This claim focuses on the therapeutic application.
The specificity of the pH-dependent release mechanism is a critical aspect. By setting the dissolution threshold at pH 6.0 or higher, the patent aims to ensure drug release predominantly in the distal ileum and colon, thereby differentiating it from older mesalazine formulations that might release earlier in the small intestine. This targeted release is the primary technological differentiator being protected.
What is the Patent Landscape for Mesalazine Formulations in Ukraine?
The patent landscape for mesalazine formulations is characterized by a history of incremental innovations aimed at improving delivery and patient compliance. UA126977 represents a recent addition to this landscape, focusing on a multiparticulate pH-dependent release system.
Existing mesalazine formulations generally fall into categories based on their release mechanisms:
- Standard Release: Oral formulations with immediate release, often leading to systemic absorption and potential side effects. These are largely out of patent protection.
- Slow-Release (SR) and Sustained-Release (XR) Formulations: These aim to prolong drug release, but may not always achieve precise colonic targeting.
- pH-Dependent Release Formulations:
- Sulfasalazine: An older prodrug that cleaves in the colon to release mesalazine. Its use is associated with specific side effects due to the sulfapyridine moiety.
- Eudragit Coated Formulations: Various patents and marketed products utilize Eudragit polymers (or similar pH-sensitive acrylic copolymers) to achieve targeted release. These formulations vary in their specific coating properties and core technologies (e.g., single-unit tablets, multiparticulate systems).
- Rectal Formulations: Suppositories and enemas for localized treatment, particularly for distal colitis.
Key patent trends for mesalazine globally and likely relevant to Ukraine include:
- Novel Delivery Systems: Focus on improving colon targeting through pH-sensitive coatings, osmotic pumps, or prodrug strategies.
- Combination Therapies: Patents for mesalazine in combination with other IBD drugs.
- Manufacturing Processes: Patents related to specific methods of producing advanced mesalazine formulations.
UA126977 competes within the "pH-dependent release" category. Its novelty, as claimed, lies in the specific design of its multiparticulate system and the precise pH dissolution profile (>= 6.0) that dictates colonic release. Companies operating in Ukraine that develop or market mesalazine products will need to assess their freedom to operate against UA126977, particularly if their formulations employ multiparticulate systems with similar pH-dependent release characteristics.
A review of publicly available Ukrainian patent databases would be necessary for a definitive analysis of all active mesalazine patents. However, the general trend indicates a mature market with ongoing efforts to refine drug delivery for improved efficacy and safety. UA126977 is an example of such refinement within the oral mesalazine space.
What is the Potential Market Impact and Competitive Landscape?
The potential market impact of UA126977 is tied to its ability to offer a demonstrably superior clinical profile compared to existing mesalazine formulations. If the claimed targeted delivery and improved safety/efficacy profile can be substantiated through clinical data, it could command a significant share of the oral mesalazine market for IBD.
Competitive Landscape Considerations:
- Existing Branded Mesalazine Products: Several branded mesalazine products are marketed globally and likely in Ukraine. Many of these, particularly those utilizing pH-dependent coatings, may have patent protection that overlaps or is adjacent to UA126977. Companies holding patents on established Eudragit-coated mesalazine formulations (e.g., those for Crohn's disease and ulcerative colitis) represent direct competitors.
- Generic Mesalazine Products: Once patents expire, generic versions of mesalazine formulations become available. However, the patentability of novel delivery systems like UA126977 allows for extended market exclusivity for the innovating company. Generic manufacturers will need to ensure their products do not infringe UA126977 if they intend to launch similar pH-dependent multiparticulate formulations.
- Alternative IBD Treatments: Mesalazine is a cornerstone for mild to moderate IBD but is often used in conjunction with or transitioned to other drug classes for moderate to severe disease, including immunomodulators (e.g., azathioprine, methotrexate) and biologic therapies (e.g., anti-TNF agents, anti-integrins). UA126977's market position will be influenced by the overall treatment algorithms for IBD.
Key Factors for Market Impact:
- Clinical Differentiation: Robust clinical trial data demonstrating superior efficacy, better tolerability, or improved patient adherence compared to existing treatments.
- Regulatory Approval: Successful navigation of Ukraine's drug regulatory approval processes.
- Pricing and Reimbursement: Strategic pricing and successful negotiation with national health systems and insurers in Ukraine for favorable reimbursement status.
- Patent Exclusivity Duration: The remaining term of patent protection for UA126977 (granted in 2023) provides a significant window for market exclusivity.
- Marketing and Sales Infrastructure: The patent holder's ability to effectively market and distribute the product within Ukraine.
Given that mesalazine remains a first-line therapy for many IBD patients, any formulation that can enhance its benefits while mitigating side effects has the potential for substantial market penetration. However, the competitive landscape is crowded with various delivery systems, necessitating a clear demonstration of superiority for UA126977 to achieve significant market impact.
What are the Implications for R&D and Investment?
For Research and Development (R&D) departments, UA126977 highlights the ongoing value of innovation in drug delivery systems, even for established active pharmaceutical ingredients (APIs). The patent signals that novel formulations can secure patent protection and market exclusivity.
R&D Implications:
- Focus on Colon Targeting: The success of UA126977 reinforces the strategy of developing drug delivery systems specifically designed for colonic release, particularly for inflammatory conditions affecting this region.
- Multiparticulate Systems: The patent's emphasis on multiparticulate systems suggests this approach continues to be a viable platform for achieving controlled and targeted drug release.
- pH-Dependent Polymers: Continued research into novel or optimized pH-dependent polymers that offer precise dissolution profiles at specific colonic pH ranges remains relevant.
- Freedom to Operate (FTO) Analysis: R&D teams must conduct thorough FTO analyses to ensure new mesalazine formulations do not infringe on claims like those in UA126977, especially concerning multiparticulate compositions with pH >= 6.0 dissolution.
For investors, UA126977 represents a case study in how pharmaceutical innovation can extend product lifecycles and create new market opportunities.
Investment Implications:
- Patented Innovation in Mature Markets: The patent indicates potential for high returns in established therapeutic areas when significant product differentiation is achieved through formulation or delivery technology.
- Life Cycle Management: Investment in companies holding patents on advanced drug delivery systems can be a strategy for pharmaceutical companies seeking to defend market share for their existing APIs or launch new, premium-priced versions.
- Due Diligence: Investors should scrutinize the strength and breadth of patent claims, the competitive landscape, and the underlying clinical data supporting the claimed benefits of such innovations. The novelty of the delivery system, as protected by UA126977, is a key asset.
- Ukrainian Pharmaceutical Market: This patent highlights the potential for innovation within the Ukrainian pharmaceutical sector, suggesting that localized R&D efforts can yield valuable intellectual property.
Investment decisions should be informed by a thorough understanding of the patent's scope, the commercial viability of the claimed technology, and the overall market dynamics for IBD treatments in Ukraine and potentially broader markets.
Key Takeaways
- Patent UA126977 protects a multiparticulate mesalazine formulation for treating inflammatory bowel diseases, characterized by a pH-dependent release coating dissolving at pH 6.0 or higher for targeted colonic delivery.
- The core claims define the composition, emphasizing the mesalazine particles and the specific properties of the enteric coating. Dependent claims further detail particle form, polymer types, and therapeutic use.
- The patent landscape for mesalazine includes various release mechanisms; UA126977 contributes to the segment of pH-dependent oral formulations, differentiating itself through its multiparticulate design and specific release pH threshold.
- Market impact depends on clinical differentiation, regulatory approval, pricing, reimbursement, and the patent holder's market execution. Competition exists from other branded and generic mesalazine products and alternative IBD therapies.
- R&D implications include continued focus on colon targeting and multiparticulate systems, necessitating rigorous FTO analyses. Investment implications involve assessing opportunities in mature markets through patented delivery system innovation and scrutinizing patent strength and clinical validation.
Frequently Asked Questions
1. What is the specific therapeutic indication of the drug protected by UA126977?
The patent UA126977 protects a pharmaceutical composition for the treatment of inflammatory bowel diseases, specifically Crohn's disease and ulcerative colitis.
2. What is the key technological innovation claimed in UA126977?
The key innovation is a multiparticulate pharmaceutical composition of mesalazine featuring a pH-dependent release coating designed to dissolve at a pH of 6.0 or higher, thereby targeting drug release to the colon.
3. How does the drug formulation claimed in UA126977 differ from older mesalazine formulations?
Unlike older formulations that may have broader release profiles, UA126977's multiparticulate system with a specific pH dissolution threshold (>= 6.0) aims for more precise delivery to the colon, potentially reducing systemic absorption and associated side effects.
4. What are the primary types of polymers mentioned in the patent for the pH-dependent coating?
The patent mentions methacrylic acid copolymers (e.g., Eudragit L, S), cellulose derivatives (e.g., hydroxypropyl methylcellulose phthalate), or polyvinyl acetate phthalate as suitable pH-dependent release coating materials.
5. What is the expected duration of market exclusivity for the product patented by UA126977 in Ukraine?
Patent UA126977 was granted on October 27, 2023. The duration of patent protection in Ukraine is typically 20 years from the filing date, though specific factors can influence this. An analysis of the filing date is necessary to determine the precise expiry.
Citations
[1] The State Enterprise "Ukrainian Intellectual Property Institute". (2023). Patent UA126977. (Proprietary data accessed through patent databases).
