United States Patent 6,514,520 B2: A Detailed Analysis
Introduction
United States Patent 6,514,520 B2, titled "Stabilized antihistamine syrup," addresses a critical issue in the formulation of antihistamine syrups by providing a stable and effective solution. This patent is crucial for pharmaceutical companies and researchers working on antihistamine formulations.
Background
Antihistamines are widely used to treat allergic reactions, but their stability in liquid formulations has been a challenge. The degradation of active ingredients in syrups can lead to reduced efficacy and shelf life. This patent aims to overcome these issues.
Inventors and Assignees
The patent was filed by inventors who recognized the need for a stable antihistamine syrup. The assignee of the patent is not explicitly mentioned in the provided sources, but it is typically a pharmaceutical company or research institution.
Publication and Priority Dates
- Publication Date: July 5, 2001
- Priority Date: This is derived from the original patent application, which in this case is September 30, 1999[4].
Claims and Scope
The patent includes several key claims that define its scope:
Active Ingredients and Stabilizers
- The patent claims a stabilized antihistamine syrup that includes an active ingredient such as loratadine or desloratadine, along with specific stabilizers to prevent degradation[1][4].
Concentration of Stabilizers
- The stabilizers, such as citric acid and aminopolycarboxylic acids, are added in concentrations ranging from about 0.05 to about 5 mg/mL. This range ensures the stability of the antihistamine without compromising its efficacy[1][4].
Formulation Components
- The syrup formulation may also include other components such as propylene glycol, sucrose, and flavorings to enhance palatability and stability[1][4].
Detailed Description of the Invention
The patent provides a detailed description of how the stabilized antihistamine syrup is formulated:
Degradation Prevention
- The addition of citric acid and aminopolycarboxylic acids prevents the degradation of the antihistamine active ingredient through oxidation and other chemical reactions[1][4].
pH Control
- The pH of the syrup is controlled to ensure that it remains within a range that does not facilitate the degradation of the active ingredient. This is typically achieved by adjusting the concentration of citric acid and other acidic components[1][4].
Sweeteners and Flavorings
- The syrup can include sweeteners like sucrose and flavorings such as mint to make it more palatable for patients, especially children[1][4].
Advantages of the Invention
The stabilized antihistamine syrup offers several advantages:
Extended Shelf Life
- The formulation ensures that the antihistamine remains effective over a longer period, reducing the need for frequent reformulation or replacement[1][4].
Improved Efficacy
- By preventing the degradation of the active ingredient, the syrup maintains its therapeutic efficacy, providing consistent relief to patients[1][4].
Enhanced Patient Compliance
- The palatable nature of the syrup, thanks to the addition of sweeteners and flavorings, improves patient compliance, especially in pediatric patients[1][4].
Patent Landscape
The patent landscape for antihistamine syrups is competitive, with several patents addressing similar issues:
Related Patents
- Other patents, such as the Canadian patent 2656087, also focus on sugar-free and storage-stable antihistaminic syrups, highlighting the ongoing research in this area[2].
Industry Trends
- The trend in pharmaceutical formulations is towards creating stable, effective, and patient-friendly products. This patent aligns with these trends by providing a solution that enhances the stability and efficacy of antihistamine syrups[1][2].
Examination and Legal Status
- The patent was granted on July 5, 2001, and its legal status indicates that it has expired, as patents typically have a lifespan of 20 years from the filing date[1][5].
Impact on Pharmaceutical Industry
This patent has had a significant impact on the pharmaceutical industry:
Formulation Standards
- It has set a standard for the formulation of stable antihistamine syrups, influencing subsequent research and development in this area[1][4].
Patient Care
- By ensuring the stability and efficacy of antihistamine syrups, this patent has contributed to better patient care and outcomes in the treatment of allergic reactions[1][4].
Key Takeaways
- Stability and Efficacy: The patent ensures the stability and efficacy of antihistamine syrups through the use of specific stabilizers.
- Formulation Components: The syrup includes citric acid, aminopolycarboxylic acids, propylene glycol, and sucrose.
- Patient Compliance: The palatable nature of the syrup enhances patient compliance.
- Patent Landscape: The patent is part of a broader landscape of research on stable and effective antihistamine formulations.
- Industry Impact: The patent has set standards for antihistamine syrup formulations and improved patient care.
Frequently Asked Questions (FAQs)
1. What is the main issue addressed by United States Patent 6,514,520 B2?
The main issue addressed is the degradation of antihistamine active ingredients in liquid formulations, which reduces their efficacy and shelf life.
2. What are the key stabilizers used in the patented syrup formulation?
The key stabilizers are citric acid and aminopolycarboxylic acids, added in concentrations ranging from about 0.05 to about 5 mg/mL.
3. How does the patent ensure the stability of the antihistamine?
The patent ensures stability by controlling the pH of the syrup and preventing oxidation and other chemical reactions that degrade the active ingredient.
4. What other components can be included in the syrup formulation?
Other components include propylene glycol, sucrose, and flavorings like mint to enhance palatability.
5. What is the current legal status of the patent?
The patent has expired, as it was granted on July 5, 2001, and patents typically have a lifespan of 20 years from the filing date.
Cited Sources:
- US6514520B2 - Stabilized antihistamine syrup - Google Patents
- Patent 2656087 Summary - Canadian Patents Database
- The IoT : A Look at the IP Landscape of Fitness Wearables - IPWatchdog
- (12) United States Patent (10) Patent No.: US 6,514,520 B2 - Patent Images
- Pharmaceutical drugs covered by patent 6,514,520 - Drug Patent Watch
