United States Patent 7,959,945: A Detailed Analysis of Scope and Claims
Introduction
United States Patent 7,959,945, titled "Dispersible bosentan tablet," is a significant patent in the pharmaceutical field, particularly for the treatment of pulmonary arterial hypertension (PAH). This patent, granted to Actelion Pharmaceuticals Ltd., introduces a novel formulation of bosentan, a dual endothelin receptor antagonist.
Background of Bosentan
Bosentan, marketed under the brand name Tracleer®, is an oral treatment for PAH, classified as Class III and IV in the United States and Class III in Europe. It works by blocking the action of endothelin, a potent vasoconstrictor, thereby reducing pulmonary vascular resistance and improving exercise capacity in patients with PAH[1].
Patent Overview
Publication and Legal Status
The patent was published on June 14, 2011, and is currently active, with an expiration date that would be determined by the patent's filing date and any applicable extensions or adjustments.
Prior Art and Related Patents
The patent builds upon prior art related to dispersible tablets and formulations of bosentan. It addresses specific challenges associated with the stability and bioavailability of bosentan in tablet form.
Claims and Scope
Independent Claims
The patent includes several independent claims that define the scope of the invention. These claims focus on the composition and method of preparing a dispersible bosentan tablet. Key aspects include:
- Composition: The tablet comprises bosentan or a pharmaceutically acceptable salt thereof, along with excipients such as croscarmellose sodium, crosslinked sodium carboxy methyl cellulose, and colloidal silicon dioxide[1].
- Method of Preparation: The method involves mixing the active ingredient with the excipients, followed by compression into a tablet form that is dispersible in water.
Dependent Claims
Dependent claims further specify the proportions of the ingredients, the process of manufacturing, and the physical characteristics of the tablet. For example, the claims detail the use of specific fillers, binders, and disintegrants to achieve the desired dispersibility and stability.
Technical Details
Excipients and Formulation
The patent specifies the use of various excipients to enhance the dispersibility and stability of the bosentan tablet. These include:
- Croscarmellose sodium: Acts as a disintegrant to facilitate the rapid breakdown of the tablet in water.
- Crosslinked sodium carboxy methyl cellulose: Helps in controlling the release of the active ingredient.
- Colloidal silicon dioxide: Used as an anti-caking agent to improve the flow properties of the powder during tablet manufacturing[1].
Manufacturing Process
The manufacturing process involves several steps, including:
- Mixing: The active ingredient and excipients are mixed to form a uniform blend.
- Compression: The blend is then compressed into a tablet form using a tablet press.
- Quality Control: The tablets are tested for their dispersibility, stability, and content uniformity.
Patent Landscape
Related Patents and Applications
The patent landscape for bosentan and related formulations is complex, with multiple patents and applications filed by various pharmaceutical companies. For instance, other patents may cover different formulations, delivery systems, or methods of treatment using bosentan or similar compounds.
International Patent Protection
The protection of this patent is not limited to the United States. Actelion Pharmaceuticals Ltd. would likely have filed corresponding patent applications in other jurisdictions to secure global protection for their invention.
Impact and Significance
Clinical Implications
The dispersible bosentan tablet offers significant clinical benefits, particularly for patients who have difficulty swallowing solid tablets. This formulation improves patient compliance and can enhance the therapeutic efficacy of bosentan in treating PAH.
Market and Commercial Impact
The introduction of a dispersible bosentan tablet expands the market for PAH treatments, providing a more convenient and patient-friendly option. This can lead to increased market share and revenue for the patent holder.
Challenges and Future Directions
Patent Scope and Quality
The scope of the patent is defined by its claims, and the quality of these claims is crucial for maintaining the patent's validity. Research on patent scope suggests that narrower claims at publication are associated with a higher probability of grant and a shorter examination process[4].
Regulatory and Legal Considerations
The patent holder must navigate regulatory and legal landscapes to ensure compliance with intellectual property laws and pharmaceutical regulations. This includes monitoring for potential infringements and defending the patent against challenges.
Key Takeaways
- Innovative Formulation: The patent introduces a novel dispersible tablet formulation of bosentan, enhancing patient compliance and therapeutic efficacy.
- Detailed Claims: The patent includes specific claims regarding the composition and method of preparation, defining the scope of the invention.
- Technical Specifications: The use of specific excipients and a detailed manufacturing process ensures the stability and dispersibility of the tablet.
- Clinical and Market Impact: The dispersible bosentan tablet offers significant clinical benefits and market opportunities.
- Regulatory and Legal Considerations: The patent holder must ensure compliance with intellectual property laws and pharmaceutical regulations.
FAQs
What is the primary benefit of the dispersible bosentan tablet?
The primary benefit is improved patient compliance, especially for those who have difficulty swallowing solid tablets, thereby enhancing the therapeutic efficacy of bosentan in treating PAH.
What are the key excipients used in the dispersible bosentan tablet?
The key excipients include croscarmellose sodium, crosslinked sodium carboxy methyl cellulose, and colloidal silicon dioxide.
How does the manufacturing process ensure the quality of the tablets?
The manufacturing process involves mixing the active ingredient and excipients, followed by compression into a tablet form, and includes quality control tests for dispersibility, stability, and content uniformity.
What is the significance of the patent's claims in defining its scope?
The claims define the specific composition and method of preparation, which are crucial for maintaining the patent's validity and protecting the invention from infringement.
How does this patent impact the market for PAH treatments?
The dispersible bosentan tablet expands the market for PAH treatments by providing a more convenient and patient-friendly option, potentially increasing market share and revenue for the patent holder.
Sources
- US7959945B2 - Dispersible bosentan tablet - Google Patents
- Patent Claims Research Dataset - USPTO
- Search for patents - USPTO
- Patent Claims and Patent Scope - SSRN
- LEVOSIMENDAN FOR TREATING PULMONARY HYPERTENSION WITH HEART FAILURE WITH PRESERVED EJECTION FRACTION - Google Patents
