United States Patent 8,486,456: A Detailed Analysis of Scope, Claims, and Patent Landscape
Introduction
United States Patent 8,486,456, titled "Itraconazole compositions with improved bioavailability," is a significant patent in the pharmaceutical industry, particularly in the field of antifungal medications. This patent, assigned to Sebela Ireland Ltd, addresses the formulation and delivery of itraconazole, a widely used antifungal drug.
Background of Itraconazole
Itraconazole is an antifungal medication used to treat various fungal infections, including candidiasis, tinea pedis, and tinea unguium. However, its poor solubility in water has been a challenge, affecting its bioavailability and efficacy[2].
Patent Overview
Patent Title and Number
- Title: Itraconazole compositions with improved bioavailability
- Patent Number: US8486456B2
Patent Owner
The patent is owned by Sebela Ireland Ltd, a company involved in the development and marketing of pharmaceutical products[2].
Scope of the Patent
Invention Description
The patent describes a solid dispersion product comprising itraconazole and hydroxypropyl methylcellulose (HPMC). This formulation aims to enhance the bioavailability of itraconazole by improving its solubility and dissolution rate. The solid dispersion is prepared using methods such as melt extrusion, kneading, or other processes that ensure the uniform distribution of itraconazole within the HPMC matrix[1].
Key Components
- Itraconazole: The active antifungal ingredient.
- Hydroxypropyl Methylcellulose (HPMC): A polymer used to improve the solubility and bioavailability of itraconazole.
- Other Excipients: The patent also mentions the use of additional excipients such as propylene glycol, poly(ethylene oxide), and lubricants to enhance the formulation's stability and manufacturability[1].
Claims of the Patent
The patent includes several claims that define the scope of the invention:
Independent Claims
- Claim 1 describes the solid dispersion product comprising itraconazole and HPMC.
- Claim 2 specifies the method of preparing the solid dispersion.
- Claim 3 outlines the dosage form of the composition, including tablets and capsules[1].
Dependent Claims
These claims further detail the specific ratios of itraconazole to HPMC, the methods of preparation, and the physical characteristics of the solid dispersion, such as particle size and melting point[1].
Patent Landscape
Related Patents
The patent landscape for itraconazole is complex, with multiple patents covering various aspects of its formulation and use. Here are some notable patents:
- US10463740, US10806792, US8921374, US9272046, US9713642: These patents, owned by Mayne Pharma, also relate to itraconazole compositions and dosage forms, with an expiration date of June 21, 2033[2].
- US6509038, US7081255, US8591948: These patents, owned by Sebela Ireland Ltd, are related to antifungal compositions with improved bioavailability and have expired as of May 12, 2017[2].
Generic Applications
Several generic versions of itraconazole have been approved, with the first generic version approved by Sandoz Inc on May 28, 2004. Recent approvals include those by Annora Pharma Private Ltd on September 1, 2020[2].
Patent Expiration
The patent US8486456B2 is set to expire on October 3, 2028. This expiration date can be subject to change based on legal activities such as patent term extensions or amendments to the claims[2].
Impact on the Pharmaceutical Industry
Bioavailability Enhancement
The improved bioavailability of itraconazole achieved through this patent has significant implications for patient treatment outcomes. Enhanced bioavailability ensures that the drug is more effectively absorbed by the body, leading to better therapeutic results[1].
Competitive Landscape
The presence of multiple patents and generic applications creates a competitive landscape for itraconazole formulations. Companies like Mayne Pharma, Sebela Ireland Ltd, and various generic manufacturers are actively involved in developing and marketing these formulations[2][4].
Legal and Regulatory Considerations
Patent Litigation and Challenges
The patent landscape for itraconazole includes several legal activities such as patent litigation and Paragraph IV challenges. These activities can affect the patent's expiration date and the availability of generic versions[2][4].
Regulatory Approvals
The approval of generic versions of itraconazole is regulated by bodies such as the FDA. The approval process involves ensuring that the generic formulations meet the bioequivalence and safety standards of the branded drug[2].
Conclusion
United States Patent 8,486,456 is a crucial patent in the field of antifungal medications, particularly for itraconazole. The patent's focus on improving bioavailability through solid dispersion formulations has enhanced the efficacy of itraconazole treatments. Understanding the scope, claims, and patent landscape of this invention is essential for pharmaceutical companies involved in the development and marketing of itraconazole products.
Key Takeaways
- Improved Bioavailability: The patent describes a method to enhance the bioavailability of itraconazole using solid dispersion with HPMC.
- Patent Ownership: The patent is owned by Sebela Ireland Ltd.
- Patent Expiration: The patent is set to expire on October 3, 2028.
- Competitive Landscape: Multiple patents and generic applications exist for itraconazole formulations.
- Legal and Regulatory Considerations: Patent litigation, challenges, and regulatory approvals are critical factors in the patent landscape.
Frequently Asked Questions (FAQs)
What is the main focus of United States Patent 8,486,456?
The main focus of this patent is to improve the bioavailability of itraconazole through a solid dispersion formulation using hydroxypropyl methylcellulose (HPMC).
Who owns the patent US8486456B2?
The patent US8486456B2 is owned by Sebela Ireland Ltd.
When is the patent set to expire?
The patent is set to expire on October 3, 2028, subject to any changes due to legal activities.
What are the key components of the solid dispersion described in the patent?
The key components include itraconazole, hydroxypropyl methylcellulose (HPMC), and other excipients such as propylene glycol and poly(ethylene oxide).
How does the improved bioavailability of itraconazole impact patient treatment?
Improved bioavailability ensures that the drug is more effectively absorbed by the body, leading to better therapeutic results and enhanced patient treatment outcomes.
Sources:
- US8486456B2 - Itraconazole compositions with improved bioavailability - Google Patents
- Drug Patents containing Itraconazole - Pharsight
- Patent Analytics | Intellectual Property Law - Schwegman
- Generic ITRACONAZOLE INN equivalents, pharmaceutical patent ... - Drug Patent Watch
