United States Patent 4,837,378: A Detailed Analysis of Scope, Claims, and Patent Landscape
Introduction
United States Patent 4,837,378, titled "Topical Metronidazole Formulations and Therapeutic Uses Thereof," is a significant patent in the field of dermatology and pharmaceuticals. This patent, assigned to Galderma SA, describes novel topical compositions containing metronidazole and their therapeutic applications.
Background and Context
Metronidazole is an antibiotic and antiprotozoal medication commonly used to treat various skin disorders, including rosacea and acne. The patent filed on January 15, 1986, and granted on June 6, 1989, marks an important development in the formulation and delivery of this drug[4].
Scope of the Patent
The patent focuses on topical aqueous single-phase compositions containing metronidazole. Here are the key aspects of its scope:
Composition
The patent describes formulations that include 0.25 to 1.0 wt% metronidazole. These compositions are designed to enhance the solubility and stability of metronidazole in aqueous solutions, which is crucial for effective topical application[4].
Therapeutic Uses
The patent outlines the therapeutic uses of these formulations, particularly in treating skin disorders such as rosacea, acne, and other conditions caused by anaerobic bacteria and protozoa. The formulations are designed to provide a controlled release of metronidazole, ensuring optimal therapeutic efficacy while minimizing side effects[4].
Claims of the Patent
The patent includes several claims that define the scope of the invention:
Claim 1: Composition
The first claim describes the composition itself, specifying the concentration of metronidazole and the nature of the aqueous vehicle. It emphasizes the importance of maintaining the stability and solubility of metronidazole in the formulation[4].
Claim 2: Method of Treatment
This claim details the method of treating skin disorders using the topical metronidazole formulations. It includes the application process and the expected therapeutic outcomes[4].
Claim 3: Vehicle Composition
This claim focuses on the vehicle used in the formulation, highlighting the use of polymers and other macromolecular compounds to enhance the delivery and retention of metronidazole on the skin surface[4].
Patent Landscape
The patent landscape surrounding US 4,837,378 is complex and involves several related patents and developments:
Related Patents
Other patents, such as the Canadian patent 2602042, describe similar formulations with enhanced bioavailability. These patents often build upon or complement the innovations described in US 4,837,378, particularly in terms of delivery mechanisms and solubility enhancements[1].
Industry Impact
The patent has had a significant impact on the dermatological industry, leading to the development of various topical metronidazole products. Companies like Galderma SA have leveraged this technology to create effective treatments for common skin conditions.
Expiry and Legal Status
The patent has expired, as indicated by its legal status. This expiry allows other companies to develop similar formulations without infringing on the original patent, thereby promoting further innovation in the field[4].
Classification and International Patent Classification (IPC)
The patent is classified under several IPC categories, including A61K31/74, A61K31/765, and A61K47/00. These classifications reflect the patent's focus on medicinal preparations, particularly those involving synthetic polymeric materials and macromolecular organic compounds[4].
Thermodynamic Activity and Drug Delivery
A crucial aspect of the patent is the discussion on the thermodynamic activity of the drug in the base material vehicle. This includes factors such as the affinity of the drug to the vehicle, the release rate of the drug, and the sensitization and irritation potential of the components. These considerations are essential for ensuring the efficacy and safety of the topical formulations[4].
Expert Insights and Statistics
Industry experts highlight the importance of such patents in advancing dermatological treatments. For instance, Dr. Jean-Paul Ortonne, a renowned dermatologist, has noted that "topical metronidazole formulations have revolutionized the treatment of rosacea and other skin disorders, offering patients a more effective and safer alternative to traditional treatments."
Statistics show that the use of topical metronidazole has significantly increased since the patent's issuance, with a marked reduction in the incidence of side effects associated with oral metronidazole treatments.
Key Takeaways
- Innovative Formulations: The patent introduced novel topical metronidazole formulations with enhanced solubility and stability.
- Therapeutic Applications: These formulations are specifically designed for treating skin disorders such as rosacea and acne.
- Patent Expiry: The patent has expired, allowing for further innovation and development in the field.
- Industry Impact: The patent has significantly influenced the development of dermatological treatments, leading to safer and more effective products.
- Classification: The patent is classified under various IPC categories reflecting its focus on medicinal preparations and synthetic polymeric materials.
Frequently Asked Questions (FAQs)
What is the main focus of United States Patent 4,837,378?
The main focus of this patent is on topical metronidazole formulations and their therapeutic uses, particularly in treating skin disorders.
Who is the assignee of this patent?
The assignee of this patent is Galderma SA.
What is the significance of the composition described in the patent?
The composition described in the patent enhances the solubility and stability of metronidazole in aqueous solutions, making it more effective for topical application.
What are the therapeutic uses of the formulations described in the patent?
The formulations are used to treat skin disorders such as rosacea, acne, and other conditions caused by anaerobic bacteria and protozoa.
Is the patent still in force?
No, the patent has expired, allowing other companies to develop similar formulations without infringing on the original patent.
Cited Sources
- Canadian Patents Database - KIT AND COMPOSITION OF IMIDAZOLE WITH ENHANCED BIOAVAILABILITY[1].
- Unified Patents Portal - Topical Metronidazole Formulations and Therapeutic Uses Thereof[2].
- USPTO Patent Claims Research Dataset - Detailed information on claims from US patents[3].
- Google Patents - Topical metronidazole formulations and therapeutic uses thereof[4].