United States Patent 6,884,433: A Detailed Analysis of Scope, Claims, and Patent Landscape
Introduction
United States Patent 6,884,433, titled "Sustained Release Formulations of Macrolide Immunomodulators," is a significant patent in the pharmaceutical field, particularly in the area of immunosuppressive drugs. This patent, granted to a pharmaceutical company, outlines innovative formulations for the sustained release of macrolide compounds, such as tacrolimus.
Background of the Invention
The patent addresses the need for improved formulations of macrolide immunomodulators, which are crucial for preventing organ rejection in transplant patients. Traditional formulations often suffer from issues such as variable bioavailability and the need for frequent dosing, which can lead to patient non-compliance and reduced efficacy[1].
Scope of the Patent
The patent covers sustained release formulations comprising a macrolide compound, specifically tacrolimus. The scope includes:
Formulation Composition
The formulations described in the patent consist of a macrolide compound, such as tacrolimus, combined with various excipients to achieve a sustained release profile. The composition may include hydrophilic and lipophilic components to enhance the solubility and stability of the drug[1].
Release Profile
A key aspect of the patent is the defined release profile. The formulations are designed to release the active ingredient over a prolonged period, ensuring that 63.2% (T63.2%) of the maximum amount of tacrolimus or its hydrate is dissolved within 0.7 to 15 hours. This is measured using the Japanese Pharmacopoeia 13th edition Dissolution Test no. 2 (Paddle method, 50 rpm) in a test solution adjusted to pH 4.5[1].
Claims of the Patent
The claims of the patent are critical as they define the scope of protection. Here are some key claims:
Formulation Claims
- The patent claims formulations that release less than 20% w/w of the active ingredient within 0.5 hours when subjected to an in-vitro dissolution test using the USP paddle method and 0.1N HCl as the dissolution medium[1].
Process Claims
- The patent also claims a process for preparing these sustained release formulations, which involves dissolving a portion of the macrolide compound in a solvent, mixing with carriers, drying to form a solid dispersion, and then processing the solid dispersion with additional components such as fillers and disintegrants[4].
Patent Landscape
The patent landscape surrounding US Patent 6,884,433 is complex and involves several related patents and applications.
Related Patents
- Other patents, such as United States Patent 6,440,458 and United States Patent 6,576,259, also relate to sustained release formulations of macrolide compounds. These patents describe similar formulations and release profiles, indicating a robust body of work in this area[1].
Patent Applications
- United States Application Publication 2006/0287352 describes a modified release composition of tacrolimus, which aligns with the scope of US Patent 6,884,433. This application further underscores the ongoing innovation in this field[1].
Advantages and Innovations
The patent offers several advantages over traditional formulations:
Enhanced Bioavailability
- The sustained release profile ensures a more consistent and prolonged exposure to the active ingredient, enhancing bioavailability and reducing the need for frequent dosing[1].
Improved Patient Compliance
- By providing a formulation that releases the drug over a longer period, patient compliance is improved, as the dosing regimen is simplified[1].
Stability and Solubility
- The use of hydrophilic and lipophilic components in the formulation enhances the stability and solubility of the drug, which is particularly important for hydrophobic compounds like tacrolimus[1].
Industrial and Clinical Impact
The impact of this patent is significant both industrially and clinically.
Industrial Impact
- The patent protects a valuable intellectual property asset for the pharmaceutical company, allowing them to market and sell the formulation without competition from generic versions for a specified period. This can lead to significant revenue and market dominance[5].
Clinical Impact
- Clinically, the sustained release formulation of tacrolimus can improve the management of organ transplantation by providing a more reliable and consistent immunosuppressive effect. This can lead to better patient outcomes and reduced rates of organ rejection[1].
Legal and Regulatory Aspects
The patent application and granting process for US Patent 6,884,433 would have followed the standard procedures outlined by the U.S. Patent and Trademark Office (USPTO).
Patent Application Process
- The application would have included a specification, drawings, oath or declaration, application data sheet, transmittal letter, and fees. The claims would have been carefully drafted to define the scope of protection[5].
Prior Art Search
- Before filing, a thorough prior art search would have been conducted to ensure the novelty and non-obviousness of the invention. This search would have included reviewing existing patents and publications related to macrolide formulations[5].
Conclusion
United States Patent 6,884,433 represents a significant advancement in the field of pharmaceutical formulations, particularly for macrolide immunomodulators like tacrolimus. The patent's scope and claims are carefully defined to protect the innovative sustained release formulations, which offer improved bioavailability, patient compliance, and stability.
Key Takeaways
- Sustained Release Profile: The patent describes formulations that release the active ingredient over a prolonged period, enhancing bioavailability and patient compliance.
- Formulation Composition: The formulations include hydrophilic and lipophilic components to enhance solubility and stability.
- Industrial and Clinical Impact: The patent has significant industrial and clinical implications, protecting intellectual property and improving patient outcomes.
- Legal and Regulatory Aspects: The patent application and granting process followed standard USPTO procedures, including a thorough prior art search.
Frequently Asked Questions
What is the main innovation of US Patent 6,884,433?
The main innovation is the development of sustained release formulations of macrolide compounds, such as tacrolimus, which improve bioavailability and patient compliance.
How does the release profile of the formulation described in the patent differ from traditional formulations?
The formulation releases 63.2% of the maximum amount of tacrolimus within 0.7 to 15 hours, ensuring a prolonged and consistent exposure to the active ingredient.
What are the advantages of the sustained release formulation over traditional formulations?
The advantages include enhanced bioavailability, improved patient compliance, and better stability and solubility of the drug.
How does the patent protect the intellectual property of the pharmaceutical company?
The patent protects the formulation by defining specific claims that prevent others from making, using, or selling similar formulations for a specified period.
What is the clinical impact of this patent on organ transplantation?
The sustained release formulation of tacrolimus can improve the management of organ transplantation by providing a more reliable and consistent immunosuppressive effect, leading to better patient outcomes and reduced rates of organ rejection.
Cited Sources
- WO2009022354A2 - Formes pharmaceutiques ... - Google Patents
- U.S. Patent and Trademark Office (USPTO) | USAGov
- Patent Claims Research Dataset - USPTO
- United States Patent (10) Patent No.: US 8,501,764 B2
- Patents | The Maryland People's Law Library
