United States Patent 8,263,600: A Detailed Analysis of Scope and Claims
Overview of the Patent
The United States Patent 8,263,600, titled "Antifungal composition with enhanced bioavailability," pertains to the development of stable, liquid suspensions containing an antifungally effective amount of the micronized compound posaconazole. This patent is crucial in the field of pharmaceuticals, particularly for treating fungal infections in patients with compromised immune systems.
Patent Scope
Background and Purpose
The patent aims to address the issue of poor bioavailability associated with traditional antifungal formulations. Posaconazole, a triazole antifungal drug, is effective against invasive infections by Candida and Aspergillus species but faces challenges in absorption when administered orally[4].
Key Components
- Posaconazole: The primary active ingredient, a triazole antifungal drug.
- Micronization: The process of reducing the particle size of posaconazole to enhance bioavailability.
- Liquid Suspension: The formulation type that improves the stability and efficacy of the antifungal compound.
Claims of the Patent
Independent Claims
The patent includes several independent claims that define the scope of the invention:
- Claim 1: Describes the antifungal composition as a liquid suspension containing a micronized posaconazole and specific excipients such as thickening agents, surfactants, and solvents.
- Claim 2: Specifies the particle size of the micronized posaconazole, typically less than 10 microns.
- Claim 3: Details the composition of the liquid suspension, including the presence of purified water, glycerine, and xanthan gum as thickening agents[1].
Dependent Claims
Dependent claims further elaborate on the independent claims by specifying additional components and their proportions:
- Claim 4: Includes the use of citric acid as a pH adjuster.
- Claim 5: Describes the addition of preservatives such as sodium benzoate.
- Claim 6: Specifies the concentration of posaconazole in the suspension[1].
Formulation and Composition
Excipients and Additives
The patent outlines various excipients and additives that enhance the stability and bioavailability of the posaconazole suspension:
- Thickening Agents: Xanthan gum is used to maintain the suspension's viscosity.
- Surfactants: Polysorbate 80 is included to improve the solubility of posaconazole.
- Solvents: Glycerine and purified water are used as solvents to create a stable liquid suspension[1].
Stability and Bioavailability
The formulation ensures that the micronized posaconazole remains suspended and stable, thereby enhancing its bioavailability. This is critical for effective treatment of fungal infections, especially in patients with compromised immune systems.
Patent Landscape
Related Patents
Several patents are related to the formulation and use of posaconazole:
- US5703079: An earlier patent that also deals with antifungal compositions but does not specify the micronization process.
- US6958337: Another patent that describes different formulations of posaconazole but lacks the specific enhancements of US8263600[4].
Litigation and Settlements
Patent litigation and settlements in the pharmaceutical industry often involve disputes over the validity and infringement of patents. While US8263600 has not been specifically mentioned in recent litigation settlements, the broader context of patent disputes in the industry highlights the importance of clear and enforceable patent claims[2].
Examination Process and Scope
Narrowing of Claims
The examination process for this patent likely involved narrowing the scope of the claims to ensure clarity and validity. Research indicates that narrower claims at publication are associated with a higher probability of grant and a shorter examination process[3].
Impact on Pharmaceutical Industry
Treatment of Fungal Infections
The invention described in US8263600 significantly impacts the treatment of fungal infections by providing a more bioavailable form of posaconazole. This is particularly beneficial for patients with severe immune deficiencies.
Market and Competition
The enhanced bioavailability of posaconazole in this formulation can give the patent holder a competitive edge in the market. However, the expiration of the patent in 2022 opens up the market for generic versions, potentially increasing competition[4].
Key Takeaways
- Enhanced Bioavailability: The patent describes a formulation that significantly improves the bioavailability of posaconazole.
- Stable Liquid Suspension: The use of specific excipients ensures the stability of the micronized posaconazole in a liquid suspension.
- Patent Scope: The claims are narrowly defined to ensure clarity and validity, focusing on the unique aspects of the formulation.
- Impact on Treatment: The invention is crucial for treating fungal infections in patients with compromised immune systems.
- Market Implications: The patent’s expiration has opened the market to generic versions, increasing competition.
FAQs
What is the primary active ingredient in the patent US8263600?
The primary active ingredient is posaconazole, a triazole antifungal drug.
What is the significance of micronization in this patent?
Micronization reduces the particle size of posaconazole, enhancing its bioavailability.
What are the key excipients used in the liquid suspension?
Key excipients include xanthan gum, glycerine, purified water, and polysorbate 80.
How does the patent impact the treatment of fungal infections?
The patent provides a more bioavailable form of posaconazole, which is crucial for treating fungal infections in patients with compromised immune systems.
When did the patent US8263600 expire?
The patent expired in April 2022.
Sources
- US8263600B2 - Antifungal composition with enhanced bioavailability - Google Patents
- ANDA Litigation Settlements Fall 2020 | Hatch-Waxman - Robins Kaplan LLP
- Patent Claims and Patent Scope - SSRN
- Posaconazole: Uses, Interactions, Mechanism of Action - DrugBank
