Detailed Analysis of the Scope and Claims of United States Patent 6,869,939
Introduction
United States Patent 6,869,939, titled "Formulations containing amiodarone and sulfoalkyl ether cyclodextrin," is a significant patent in the field of pharmaceutical formulations. This patent, granted to Mosher et al., addresses the formulation of amiodarone, an antiarrhythmic agent, using sulfoalkyl ether cyclodextrin (SAE-CD) to enhance its solubility and stability.
Background
Amiodarone is a powerful antiarrhythmic drug used to treat various types of irregular heartbeats. However, its poor water solubility has been a major challenge in formulating it for parenteral administration. The invention described in this patent aims to overcome this issue by using SAE-CD, a derivative of cyclodextrin with improved water solubility.
Scope of the Patent
The patent covers aqueous parenteral formulations that include amiodarone and SAE-CD. Here are the key aspects of the scope:
Components of the Formulation
- Amiodarone: The primary active ingredient, an antiarrhythmic agent.
- Sulfoalkyl Ether Cyclodextrin (SAE-CD): A solubilizing agent that enhances the water solubility of amiodarone[1][2].
Formulation Methods
The patent describes methods for preparing these formulations, including the process of dissolving amiodarone in a solution containing SAE-CD. This method ensures that the amiodarone remains in a stable and soluble form, which is crucial for parenteral administration[1].
Stability and Solubility
The use of SAE-CD significantly improves the water solubility of amiodarone, making it suitable for intravenous or other parenteral administrations. This enhancement in solubility and stability is a critical aspect of the patent[1][4].
Claims of the Patent
The patent includes several claims that define the scope of the invention:
Claim 1: Formulation Composition
The first claim describes the composition of the formulation, which includes amiodarone and SAE-CD in an aqueous solution. This claim sets the foundation for the entire patent by specifying the essential components of the formulation[1].
Claim 2: Method of Preparation
This claim outlines the method of preparing the formulation, including the steps involved in dissolving amiodarone in a solution containing SAE-CD. The method ensures that the final solution is stable and suitable for parenteral administration[1].
Claim 3: Concentration of Components
The patent specifies the concentration ranges for both amiodarone and SAE-CD in the formulation. These concentrations are critical to maintaining the stability and solubility of the drug[1].
Claim 4: Additional Components
The patent also allows for the inclusion of additional components such as acidifiers, stabilizers, and antioxidants to further enhance the stability and shelf life of the formulation[1].
Patent Landscape
Understanding the patent landscape around this invention is crucial for assessing its impact and potential applications.
Prior Art
The patent references several prior art documents, including other patents related to cyclodextrin formulations and methods of preparing them. These references highlight the advancements made by the current patent over existing technologies[1][2].
Related Patents
Other patents, such as WO2011156481A2, also discuss formulations including amiodarone and cyclodextrin derivatives. These patents indicate a broader interest in improving the solubility and stability of amiodarone using various cyclodextrin derivatives[2].
Competitive Advantage
The use of SAE-CD in this patent provides a significant competitive advantage by offering a more stable and soluble formulation of amiodarone compared to other existing formulations. This enhances the drug's efficacy and safety profile for parenteral administration[1][4].
Industrial Applications
The industrial applications of this patent are substantial, particularly in the pharmaceutical industry.
Parenteral Administration
The formulation described in the patent is specifically designed for parenteral administration, which includes intravenous, intramuscular, and subcutaneous injections. This makes it a valuable asset for hospitals and healthcare providers[1][2].
Pharmaceutical Manufacturing
Pharmaceutical companies can use this patent to develop and manufacture amiodarone formulations that are more stable and effective. This can lead to improved patient outcomes and reduced complications associated with the administration of amiodarone[1].
Legal and Regulatory Aspects
The patent's legal status and regulatory compliance are important considerations.
Expiration and Extensions
The patent has expired, but it is essential to note that the technology and methods described can still be used and improved upon. Any new developments or improvements would need to be patented separately[1].
Regulatory Compliance
The formulation must comply with regulatory standards for pharmaceuticals, including those related to stability, solubility, and safety. The patent provides a framework that can be used to ensure compliance with these regulations[1].
Key Takeaways
- Improved Solubility: The use of SAE-CD significantly enhances the water solubility of amiodarone.
- Stability: The formulation ensures the stability of amiodarone, making it suitable for parenteral administration.
- Method of Preparation: The patent outlines a specific method for preparing the formulation.
- Concentration Ranges: The patent specifies concentration ranges for both amiodarone and SAE-CD.
- Additional Components: The formulation can include additional components like acidifiers and stabilizers.
- Industrial Applications: The patent has significant applications in the pharmaceutical industry, particularly for parenteral administration.
Frequently Asked Questions (FAQs)
What is the main purpose of using SAE-CD in the formulation of amiodarone?
The main purpose of using SAE-CD is to enhance the water solubility and stability of amiodarone, making it suitable for parenteral administration.
What are the key components of the formulation described in the patent?
The key components are amiodarone and SAE-CD in an aqueous solution.
How does the patent improve the stability of amiodarone?
The patent improves the stability by using SAE-CD, which helps in maintaining the solubility of amiodarone in an aqueous solution.
What are the potential applications of this patent in the pharmaceutical industry?
The potential applications include the development and manufacture of amiodarone formulations for parenteral administration, enhancing patient outcomes and reducing complications.
Is the patent still in force?
No, the patent has expired, but the technology and methods described can still be used and improved upon.
Cited Sources
- US6869939B2 - Formulations containing amiodarone and sulfoalkyl ether cyclodextrin - Google Patents
- WO2011156481A2 - Formulations including amiodarone and salts thereof and methods of their manufacture and use - Google Patents
- US8410077.pdf - Google Patents
- FORMULATIONS CONTAINING AMIODARONE AND SULFOALKYL ... - PubChem
