United States Patent 6,455,533: A Detailed Analysis of Scope, Claims, and Patent Landscape
Introduction
United States Patent 6,455,533, titled "Pharmaceutical compositions for oral administration, comprising an active substance and a cyclodextrin," is a significant patent in the pharmaceutical industry. This patent, granted to a pharmaceutical company, outlines specific formulations and methods for enhancing the bioavailability and stability of certain active substances when administered orally.
Background
The patent was filed on July 2, 1998, and it pertains to the use of cyclodextrins in pharmaceutical compositions. Cyclodextrins are cyclic oligosaccharides known for their ability to form inclusion complexes with various molecules, thereby improving the solubility, stability, and bioavailability of active pharmaceutical ingredients (APIs)[5].
Scope of the Patent
Active Substances
The patent focuses on active substances belonging to the family of substituted benzhydrylpiperazines. These compounds are commonly used in antihistamine medications, such as cetirizine and hydroxyzine. The general formula for these substances includes specific substitutions and configurations that are detailed in the patent[1].
Cyclodextrins
Cyclodextrins, particularly β-cyclodextrin, are integral components of the pharmaceutical compositions described. These molecules form complexes with the active substances, enhancing their solubility and stability in aqueous environments. The patent specifies the proportions and preparation methods for these cyclodextrin complexes[1].
Pharmaceutical Compositions
The patent describes various formulations for oral administration, including tablets, chewable tablets, and oral syrups. Each formulation includes the active substance, cyclodextrin, and other excipients such as flavoring agents and fillers like mannitol or impalpable sucrose[1].
Claims of the Patent
The patent includes 18 claims that define the scope of the invention. Here are some key claims:
Claim 1
This claim describes the pharmaceutical composition comprising an active substance belonging to the substituted benzhydrylpiperazine family and a cyclodextrin. It specifies the proportions of the active substance and cyclodextrin and the presence of other excipients[1].
Claim 2-5
These claims detail the specific substitutions on the benzhydrylpiperazine ring, including the positions and types of substituents (e.g., hydrogen, halogen, alkyl, or alkoxy groups)[1].
Claim 6-10
These claims cover the different forms of the pharmaceutical compositions, such as tablets, chewable tablets, and oral syrups, and the methods of preparing these formulations[1].
Claim 11-18
These claims address the use of the pharmaceutical compositions for treating conditions such as allergies and the inclusion of pharmaceutically acceptable salts of the active substances[1].
Patent Landscape
Related Patents and Applications
The patent landscape surrounding US 6,455,533 includes other patents related to the use of cyclodextrins in pharmaceutical formulations. For instance, European Patent EP 58146, mentioned in the patent, describes similar substituted benzhydrylpiperazines and their use in pharmaceuticals[1].
International Patent Offices
The global patent landscape for similar inventions can be explored through databases such as the European Patent Office (EPO), Japan Patent Office (JPO), and the World Intellectual Property Organization (WIPO). These databases provide access to international patent applications and granted patents, helping to identify similar or overlapping inventions[2].
Patent Analytics
To fully understand the patent landscape, patent analytics tools can be used. These tools help in categorizing patents by claims and scope concepts, identifying gaps or opportunities in intellectual property protection, and generating claim charts to review patent coverage with technical experts[3].
Impact on Pharmaceutical Industry
Enhanced Bioavailability
The use of cyclodextrins as described in the patent significantly enhances the bioavailability of the active substances, making the medications more effective. This is particularly important for drugs like cetirizine, which are commonly used for treating allergies[1].
Regulatory Approvals
The patent has been referenced in regulatory approvals, such as the FDA's approval of Zyrtec chewable tablets (NDA 21621), which relied on the safety and efficacy findings of the listed drug cetirizine. The patent number 6,455,533 is listed in the FDA documentation for this approval[4].
Key Takeaways
- Cyclodextrin Complexes: The patent highlights the use of cyclodextrins to improve the solubility and stability of active pharmaceutical ingredients.
- Specific Formulations: Detailed formulations for tablets, chewable tablets, and oral syrups are provided.
- Regulatory Impact: The patent has been crucial in the regulatory approval of certain pharmaceutical products.
- Global Patent Landscape: The patent is part of a broader landscape of international patents related to pharmaceutical formulations.
- Patent Analytics: Tools like claim charts and scope concepts are essential for understanding and managing the patent landscape.
FAQs
Q: What is the main focus of United States Patent 6,455,533?
A: The main focus is on pharmaceutical compositions for oral administration, comprising an active substance from the substituted benzhydrylpiperazine family and a cyclodextrin.
Q: How do cyclodextrins enhance the active substances in these compositions?
A: Cyclodextrins form inclusion complexes with the active substances, improving their solubility, stability, and bioavailability.
Q: What types of formulations are described in the patent?
A: The patent describes formulations for tablets, chewable tablets, and oral syrups.
Q: How has this patent impacted regulatory approvals?
A: The patent has been referenced in FDA approvals, such as for Zyrtec chewable tablets, relying on the safety and efficacy findings of the listed drug cetirizine.
Q: What tools can be used to analyze the patent landscape related to this invention?
A: Tools such as claim charts, scope concepts, and international patent databases can be used to analyze the patent landscape.
Sources
- US6455533B1 - Pharmaceutical compositions for oral administration, comprising an active substance and a cyclodextrin - Google Patents
- Search for patents - USPTO
- Patent Analytics | Intellectual Property Law - SLWIP
- 209089Orig1s000 209090Orig1s000 - FDA
- United States Patent (10) Patent No.: US 6,455,533 B1 - Patent Images Storage
