Last updated: February 19, 2026
This report analyzes Australian patent application AU2017251691, titled "PHARMACEUTICAL COMPOSITIONS AND METHODS." The patent claims relate to specific formulations of apixaban, a direct factor Xa inhibitor used as an anticoagulant. The analysis focuses on the scope of the claims, the technological landscape, and potential competitive implications for pharmaceutical R&D and investment.
What are the core claims of AU2017251691?
The primary claims of AU2017251691 cover pharmaceutical compositions containing apixaban and specific excipients.
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Claim 1 defines a pharmaceutical composition comprising:
- Apixaban.
- An alkali metal salt of a carboxylic acid selected from the group consisting of potassium acetate, sodium acetate, potassium citrate, sodium citrate, potassium succinate, and sodium succinate.
- A disintegrant.
- A lubricant.
The claim specifies a weight percentage range for the alkali metal salt, typically between 1% and 10% by weight of the composition. The disintegrant is described as being present in an amount of 5% to 20% by weight, and the lubricant in an amount of 0.5% to 5% by weight.
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Claim 2 depends on Claim 1 and further specifies the disintegrant as crospovidone.
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Claim 3 depends on Claim 1 and further specifies the disintegrant as sodium starch glycolate.
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Claim 4 depends on Claim 1 and further specifies the lubricant as magnesium stearate.
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Claim 5 defines a method of treating or preventing thromboembolic disorders comprising administering a pharmaceutical composition defined in Claim 1.
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Claim 6 depends on Claim 5 and specifies the thromboembolic disorder as atrial fibrillation.
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Claim 7 depends on Claim 5 and specifies the thromboembolic disorder as deep vein thrombosis or pulmonary embolism.
The claims aim to protect specific formulations that may improve the dissolution or bioavailability of apixaban, particularly for oral administration.
What is the technological context of apixaban formulations?
Apixaban, marketed as Eliquis, is a widely prescribed anticoagulant. Its efficacy and safety profile have led to significant market penetration. However, like many active pharmaceutical ingredients (APIs), apixaban's physical and chemical properties can influence its formulation characteristics, including dissolution rate, stability, and overall bioavailability.
Previous research and patent applications in this area have focused on various strategies to optimize apixaban delivery. These include:
- Particle Size Reduction: Micronization or nano-milling of apixaban to increase surface area and improve dissolution.
- Amorphous Solid Dispersions: Formulating apixaban in an amorphous state to enhance solubility.
- Use of Solubilizers: Incorporating excipients that can improve the apparent solubility of poorly soluble drugs.
- Controlled Release Formulations: Developing dosage forms that release apixaban over a specific period.
The inclusion of alkali metal salts of carboxylic acids in AU2017251691 suggests an approach to enhance the dissolution rate of apixaban, potentially by influencing the microenvironment pH or promoting disintegration. Potassium acetate and sodium succinate are examples of excipients that have been explored for their effects on drug dissolution and stability.
What is the patent landscape surrounding apixaban formulations?
The patent landscape for apixaban is robust, with numerous patents covering the compound itself, its therapeutic uses, manufacturing processes, and various formulations. Key patents for apixaban include those covering the molecule's synthesis and initial therapeutic applications.
For formulations, the landscape is characterized by continuous innovation aimed at:
- Improving Efficacy and Safety: Developing formulations with more predictable pharmacokinetics.
- Enhancing Patient Compliance: Creating user-friendly dosage forms, such as orally disintegrating tablets or fixed-dose combinations.
- Circumventing Existing Patents: Developing novel formulations that offer a distinct inventive step and patentability.
- Extending Market Exclusivity: Obtaining new patents on improved formulations that can provide market protection beyond the expiry of primary compound patents.
Companies holding key apixaban patents include Bristol-Myers Squibb and Pfizer. The competitive environment necessitates constant monitoring of patent filings and granted patents for potential infringements or opportunities for licensing.
How does AU2017251691 fit into the existing patent landscape?
AU2017251691 targets a specific formulation approach for apixaban. Its novelty and inventiveness will be assessed against prior art, which includes existing apixaban formulations and patents disclosing the use of similar excipients in pharmaceutical compositions.
The use of alkali metal salts of carboxylic acids, in combination with specific disintegrants and lubricants, represents a particular technical teaching. The patentability hinges on whether this specific combination of excipients provides an unexpected technical advantage or solves a problem not previously addressed by the prior art. For example, if these formulations demonstrate superior dissolution profiles, improved stability under specific conditions, or enhanced manufacturing characteristics compared to existing formulations, this could support a finding of inventiveness.
The claims are relatively broad within their defined scope, covering a class of alkali metal salts and standard pharmaceutical excipients. However, the patent landscape is crowded, and the scope of protection offered by AU2017251691 may be limited by earlier patents disclosing similar formulation strategies or combinations of excipients for apixaban or other poorly soluble drugs.
A thorough prior art search would be required to determine the exact novelty and inventiveness of the claimed compositions relative to existing patents. This would involve examining patents and scientific literature describing apixaban formulations, as well as patents claiming the use of potassium acetate, sodium succinate, crospovidone, sodium starch glycolate, and magnesium stearate in oral solid dosage forms for other APIs.
What are the implications for R&D and investment?
The filing of AU2017251691 signals ongoing efforts to innovate in the apixaban space. For R&D departments, this patent application highlights potential areas for formulation development:
- Investigating Novel Excipient Combinations: The patent suggests that alkali metal salts of carboxylic acids, coupled with specific disintegrants, can be a fruitful area for improving apixaban's performance.
- Developing Bioequivalent Generic Formulations: If this patent matures into a granted patent, it could present challenges for generic manufacturers seeking to market their apixaban products, requiring them to develop non-infringing formulations.
- Exploring New Therapeutic Applications: While the claims focus on thromboembolic disorders, optimizing apixaban's dissolution could potentially benefit other therapeutic indications if they were developed.
For investors, the existence of such patent applications is crucial for understanding the competitive dynamics and potential future market exclusivity of apixaban products.
- Risk Assessment for Generic Entry: Patents on novel formulations can act as a barrier to generic competition, potentially extending the market exclusivity for the innovator product or a licensee. Investors in generic pharmaceutical companies need to assess the risk posed by such formulation patents.
- Opportunity for Licensing and Acquisition: Companies holding patents on improved formulations can leverage these assets through licensing agreements or by being acquisition targets.
- Strategic Portfolio Management: For companies involved in apixaban research or development, understanding this patent's scope is essential for strategic portfolio management and avoiding infringement.
The financial performance of apixaban-based products is significant. The market for anticoagulants is substantial and competitive. Therefore, any patent that strengthens exclusivity or offers a tangible improvement in product performance can have a material impact on market share and profitability. The precise financial implications will depend on the granted claims' breadth and strength, the enforceability of the patent, and the competitive response from other market players.
Key Takeaways
- AU2017251691 claims specific pharmaceutical compositions of apixaban utilizing alkali metal salts of carboxylic acids, disintegrants, and lubricants.
- The patent aims to protect formulations that may enhance apixaban's dissolution and bioavailability.
- The patent landscape for apixaban is dense, with continuous innovation in formulation strategies.
- This patent application indicates ongoing efforts to refine apixaban delivery and potentially extend market exclusivity.
- R&D implications include exploring novel excipient combinations and developing non-infringing formulations for generic competition.
- Investment considerations involve assessing risks related to generic entry, potential licensing opportunities, and strategic portfolio management in the anticoagulant market.
Frequently Asked Questions
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What is the primary technical innovation claimed in AU2017251691?
The primary innovation claimed is a pharmaceutical composition of apixaban that includes an alkali metal salt of a carboxylic acid, specifically to enhance its dissolution characteristics.
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Which specific alkali metal salts of carboxylic acids are covered by the claims?
The claims cover potassium acetate, sodium acetate, potassium citrate, sodium citrate, potassium succinate, and sodium succinate.
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What are the potential advantages of the claimed formulations?
The claimed formulations are intended to improve the dissolution rate of apixaban, which can lead to enhanced bioavailability and potentially more predictable therapeutic outcomes.
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How might AU2017251691 impact generic apixaban manufacturers?
If granted, this patent could present a barrier to entry for generic manufacturers if their proposed formulations fall within the scope of the granted claims, necessitating the development of alternative, non-infringing formulations.
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Does this patent application cover new therapeutic uses of apixaban?
No, this patent application focuses on pharmaceutical compositions and methods of treatment for thromboembolic disorders using these specific compositions, not on novel therapeutic indications for apixaban.
Citations
[1] Australian Patent Application AU2017251691. (2017). PHARMACEUTICAL COMPOSITIONS AND METHODS. IP Australia.
