United States Patent 6,440,458: A Detailed Analysis of Scope and Claims
Introduction
United States Patent 6,440,458, titled "Sustained Release Formulations of Macrolide Compounds," is a significant patent in the pharmaceutical industry, particularly in the field of drug delivery systems. This patent, issued on August 27, 2002, pertains to oral formulations of macrolide compounds, such as tacrolimus, designed for sustained release. Here, we will delve into the scope, claims, and the broader patent landscape surrounding this invention.
Background
Macrolide compounds, including tacrolimus, are crucial in various medical treatments, especially in immunosuppressive therapy. However, their hydrophobic nature often poses challenges in terms of bioavailability and stability. The invention described in US Patent 6,440,458 addresses these issues by providing sustained release formulations that enhance the therapeutic efficacy and patient compliance.
Scope of the Patent
Overview
The patent focuses on the development of sustained release formulations for macrolide compounds. These formulations are designed to release the active ingredient over an extended period, improving the drug's bioavailability and reducing the frequency of dosing.
Key Components
The sustained release formulations described in the patent typically include:
- Macrolide Compound: The active ingredient, such as tacrolimus.
- Matrix Material: A combination of hydrophilic and hydrophobic polymers that control the release rate of the drug.
- Solubilizing Agent: To enhance the solubility of the hydrophobic macrolide compound.
- Other Excipients: Such as fillers, lubricants, and stabilizers to ensure the formulation's stability and performance[5].
Claims
Independent Claims
The patent includes several independent claims that define the scope of the invention:
- Claim 1: Describes the sustained release formulation comprising a macrolide compound, a matrix material, and optionally a solubilizing agent.
- Claim 5: Specifies the method of preparing the sustained release formulation.
- Claim 9: Outlines the use of the sustained release formulation for treating conditions requiring immunosuppression[5].
Dependent Claims
Dependent claims further detail the specific aspects of the invention, such as:
- The type and amount of matrix material used.
- The specific solubilizing agents and their concentrations.
- The release profile characteristics, such as the time required for 63.2% of the maximum amount of the macrolide compound to be dissolved[5].
Patent Landscape
Related Patents
Several other patents are related to or build upon the concepts presented in US Patent 6,440,458:
- United States Patent 6,569,463: Describes a pharmaceutical composition with a solid carrier and encapsulation coat, which enhances the in-vivo performance of hydrophobic drugs[2].
- United States Patent 6,576,259: Relates to modified release compositions of tacrolimus, focusing on different release profiles and formulations[2].
- United States Application Publication 2006/0287352: Details a modified release composition of tacrolimus with specific in-vitro dissolution test criteria[2].
International Patent Landscape
The global patent landscape for sustained release formulations of macrolide compounds is extensive:
- WIPO (PCT) Patents: Such as WO2009022354A2, which describes modified release forms of tacrolimus and is part of the international patent family[2].
- European Patent Office (EPO) and Other International Offices: Provide access to a wide range of patent documents related to pharmaceutical formulations through databases like esp@cenet and PATENTSCOPE[1][4].
Search and Analysis Tools
To navigate the complex patent landscape surrounding US Patent 6,440,458, several tools and resources are available:
- Patent Public Search: A web-based tool provided by the USPTO that offers enhanced access to prior art and patent documents[1].
- Global Dossier: Allows users to view the file histories of related applications from participating IP Offices, including the IP5 Offices[1].
- Patent Analytics: Tools like those offered by Schwegman, which help in categorizing patents by claims and scope concepts, making it easier to analyze large numbers of patent claims[3].
Practical Implications
Commercial and Therapeutic Impact
The sustained release formulations described in US Patent 6,440,458 have significant commercial and therapeutic implications:
- Improved Patient Compliance: By reducing the frequency of dosing, these formulations enhance patient compliance.
- Enhanced Bioavailability: The sustained release profile ensures a more consistent and effective delivery of the active ingredient.
- Competitive Advantage: Companies holding such patents can differentiate their products in a highly competitive pharmaceutical market[5].
Key Takeaways
- Sustained Release Formulations: US Patent 6,440,458 focuses on developing sustained release formulations for macrolide compounds like tacrolimus.
- Scope and Claims: The patent includes detailed claims on the composition, preparation, and use of these formulations.
- Related Patents: Several other patents relate to or build upon the concepts presented in this patent.
- Global Patent Landscape: The patent is part of a broader international landscape of pharmaceutical formulations.
- Search and Analysis Tools: Various tools are available to navigate and analyze the patent landscape.
FAQs
Q: What is the main focus of US Patent 6,440,458?
A: The main focus is on sustained release formulations for macrolide compounds, such as tacrolimus.
Q: What are the key components of the sustained release formulations described in the patent?
A: The key components include the macrolide compound, matrix material, solubilizing agent, and other excipients.
Q: How do the sustained release formulations improve patient compliance?
A: By reducing the frequency of dosing, these formulations enhance patient compliance.
Q: What tools are available for navigating the patent landscape related to this invention?
A: Tools such as Patent Public Search, Global Dossier, and patent analytics software are available.
Q: What is the significance of the patent in the pharmaceutical industry?
A: The patent is significant because it provides a method to improve the bioavailability and stability of hydrophobic macrolide compounds, enhancing their therapeutic efficacy.
Sources
- USPTO - Search for patents: https://www.uspto.gov/patents/search
- Google Patents - WO2009022354A2: https://patents.google.com/patent/WO2009022354A2/fr
- SLWIP - Patent Analytics: https://www.slwip.com/services/patent-analytics/
- Clemson University - Advanced Patent Searching: https://clemson.libguides.com/advanced_patent_searching
- US Patent 6,440,458: https://patentimages.storage.googleapis.com/cb/95/f5/108e0cc32dd42b/US6440458.pdf
