Analyzing the Scope and Claims of United States Patent 9,468,598
Introduction
United States Patent 9,468,598, granted in 2016, is a significant patent that involves the development of a specific formulation and method for the determination of certain pharmaceutical compounds. Here, we will delve into the details of this patent, including its scope, claims, and the broader patent landscape it operates within.
Background of the Patent
The patent in question, US 9,468,598B2, focuses on the identification and quantification of Roflumilast, a drug used in the treatment of chronic obstructive pulmonary disease (COPD), and its related impurities. The patent also addresses the formulation and stability of pharmaceutical products containing Roflumilast[1].
Scope of the Patent
Pharmaceutical Formulation
The patent describes a method for formulating Roflumilast using lactose monohydrate as an excipient. However, it also highlights the potential formation of a lactose adduct, specifically a Maillard-based lactose adduct, which can be detrimental to the stability and efficacy of the drug. The patent suggests alternatives to lactose monohydrate to avoid this issue[1].
Analytical Method
A key aspect of the patent is the development of a robust and precise reversed-phase high-performance liquid chromatography (RP-HPLC) method for the determination of Roflumilast and its impurities. This method involves using a Phenomenex Luna C18 column with a specific mobile phase composition and gradient mode to achieve accurate quantification[1].
Claims of the Patent
Main Claims
The patent includes several claims that define the scope of the invention:
- Claim 1: A method for determining Roflumilast and its impurities using RP-HPLC.
- Claim 2: A pharmaceutical formulation comprising Roflumilast and an excipient other than lactose monohydrate to prevent the formation of a Maillard-based lactose adduct.
- Claim 3: Stability studies to ensure the formulation remains stable under various conditions[1].
Dependent Claims
Dependent claims further specify the conditions and parameters of the main claims, such as the specific column and mobile phase used in the RP-HPLC method, and the acceptable concentration ranges for Roflumilast and its impurities.
Patent Landscape
Relevant Technologies
The patent operates within the broader landscape of pharmaceutical formulation and analytical chemistry. It intersects with technologies related to drug stability, excipient selection, and advanced chromatographic techniques.
Industry Trends
The pharmaceutical industry is increasingly focused on developing robust and stable formulations that minimize the risk of impurity formation. This patent aligns with these trends by providing a method to avoid the formation of a specific impurity (Maillard-based lactose adduct) and ensuring the stability of Roflumilast formulations[1].
Regulatory Compliance
The patent adheres to international guidelines such as the ICH Q2(R1) for method validation and ICH M7 for genotoxic impurities. This ensures that the methods and formulations described are compliant with regulatory standards, which is crucial for pharmaceutical products[1].
Impact on Pharmaceutical Development
Formulation Development
The patent's emphasis on avoiding lactose monohydrate as an excipient due to the potential for Maillard-based lactose adduct formation is significant. This guidance can help formulation scientists select alternative excipients to ensure the stability and efficacy of their products.
Analytical Methodology
The RP-HPLC method described in the patent provides a precise and robust analytical tool for the quantification of Roflumilast and its impurities. This can be adopted by pharmaceutical companies to ensure the quality and consistency of their products.
Stability Studies
The patent includes detailed stability studies conducted at different temperatures and humidity levels to ensure that the formulation remains stable over time. This is critical for pharmaceutical products, as stability directly impacts the drug's efficacy and safety.
Conclusion
United States Patent 9,468,598B2 is a comprehensive patent that addresses critical aspects of pharmaceutical formulation and analytical methodology. Its scope includes the development of stable formulations and precise analytical methods, which are essential for ensuring the quality and efficacy of pharmaceutical products.
Key Takeaways
- Formulation Alternatives: The patent suggests avoiding lactose monohydrate to prevent the formation of Maillard-based lactose adducts.
- Analytical Method: A robust RP-HPLC method is described for the determination of Roflumilast and its impurities.
- Regulatory Compliance: The methods and formulations are compliant with international guidelines such as ICH Q2(R1) and ICH M7.
- Stability Studies: Detailed stability studies ensure the formulation remains stable under various conditions.
FAQs
What is the main focus of United States Patent 9,468,598?
The main focus of this patent is the development of a stable pharmaceutical formulation for Roflumilast and a precise analytical method for its determination.
Why is lactose monohydrate avoided in the patent?
Lactose monohydrate is avoided due to the potential formation of a Maillard-based lactose adduct, which can affect the stability and efficacy of the drug.
What analytical method is described in the patent?
The patent describes a reversed-phase high-performance liquid chromatography (RP-HPLC) method using a Phenomenex Luna C18 column and a specific mobile phase composition.
What are the regulatory guidelines followed in this patent?
The patent adheres to international guidelines such as ICH Q2(R1) for method validation and ICH M7 for genotoxic impurities.
What are the implications of the stability studies in the patent?
The stability studies ensure that the formulation of Roflumilast remains stable over time under various temperature and humidity conditions, which is crucial for maintaining the drug's efficacy and safety.
Sources
- Identification of Maillard Based Lactose Adduct in Pharmaceutical Formulation - SSRN.
- Determining Inventorship for US Patent Applications - Oregon State University.
- Patent Claims Research Dataset - USPTO.
- HFTO 2021 Patent Analysis - Department of Energy.
- U.S. Patent Small Claims Court - ACUS.
