Detailed Analysis of the Scope and Claims of United States Patent 8,598,152
Introduction
United States Patent 8,598,152, titled "Co-crystals of tramadol and coxibs," was issued on December 3, 2013, to inventors Carlos Ramon Plata Salaman and Nicolas Tesson, and assigned to Laboratorios Del Dr. Esteve, S.A. This patent is part of a series of inventions related to the development of co-crystals involving tramadol and nonsteroidal anti-inflammatory drugs (NSAIDs)/coxibs, which are crucial for pain management.
Background
Tramadol is a widely used opioid analgesic for treating moderate to severe pain, while coxibs, such as celecoxib, are selective inhibitors of cyclooxygenase-2 (COX-2) and are used to treat pain and inflammation. The combination of these two classes of drugs can offer synergistic benefits in pain management by targeting different pain pathways.
Scope of the Patent
The patent 8,598,152 focuses on the creation, preparation, and use of co-crystals formed by tramadol and co-crystal formers selected from NSAIDs/coxibs. Here are the key aspects of the patent's scope:
Co-crystal Formation
The patent describes the process of forming co-crystals between tramadol and various coxibs, such as celecoxib. These co-crystals are created through specific crystallization techniques that involve mixing the components in a solvent and then crystallizing them under controlled conditions[1][2][4].
Pharmaceutical Uses
The co-crystals are intended for use in pharmaceutical formulations, particularly for the treatment of pain. This includes acute pain, chronic pain, neuropathic pain, and other pain-related conditions such as fibromyalgia and diabetic neuropathies[1].
Methods of Preparation
The patent outlines several methods for preparing these co-crystals, including solvent-based crystallization, grinding, and other mechanical methods. These methods ensure the formation of stable and consistent co-crystals that can be used in various pharmaceutical formulations[1][2].
Claims of the Patent
The claims of the patent are detailed and specific, covering various aspects of the co-crystals and their preparation:
Composition Claims
The patent claims cover the co-crystals themselves, including their composition and the specific ratios of tramadol to coxibs. For example, the co-crystals can be formed with celecoxib in specific stoichiometric ratios[1].
Method Claims
The patent includes claims related to the methods of preparing these co-crystals. This includes the use of specific solvents, temperatures, and crystallization techniques[1].
Use Claims
The patent claims also cover the use of these co-crystals in pharmaceutical formulations for treating pain. This includes oral formulations, such as tablets and capsules, as well as other delivery methods[1][2].
Patent Landscape
The patent landscape surrounding US 8,598,152 is complex and involves multiple related patents:
Related Patents
Several other patents have been issued to the same inventors and assignees, covering similar but distinct aspects of co-crystals of tramadol and coxibs. These include patents such as US 10,238,668, US 10,245,276, and US 10,548,909, all of which expire on April 19, 2030[2].
Patent Expiration Dates
The patent US 8,598,152 itself is set to expire on April 19, 2030, which is 20 years from the date of filing. This expiration date aligns with other related patents in the series[2].
Competitive Landscape
The development of co-crystals involving tramadol and coxibs is a competitive area, with several pharmaceutical companies and research institutions involved. The patents held by Laboratorios Del Dr. Esteve, S.A. provide a significant advantage in this market by protecting the proprietary formulations and methods of preparation[1][2].
Technical and Analytical Aspects
The patent includes detailed technical and analytical data to support the claims:
Characterization Methods
The co-crystals are characterized using various analytical techniques such as powder X-ray diffraction, Fourier transform infrared spectroscopy, and melting point determination. These methods ensure the identity and purity of the co-crystals[1].
Stability and Solubility
The patent also addresses the stability and solubility of the co-crystals, which are critical factors for their use in pharmaceutical formulations. The co-crystals are designed to have improved solubility and stability compared to the individual components[1][4].
Clinical and Therapeutic Implications
The co-crystals of tramadol and coxibs have significant clinical and therapeutic implications:
Pain Management
These co-crystals offer a novel approach to pain management by combining the analgesic effects of tramadol with the anti-inflammatory effects of coxibs. This combination can provide better pain relief with potentially fewer side effects compared to using each drug separately[1].
Reduced Side Effects
By forming co-crystals, the inventors aim to reduce the side effects associated with each drug. For example, the gastrointestinal side effects of NSAIDs/coxibs can be mitigated when combined with tramadol in a co-crystal form[1].
Key Takeaways
- Co-crystal Formation: The patent describes the formation of co-crystals between tramadol and coxibs.
- Pharmaceutical Uses: These co-crystals are intended for pain management, including acute, chronic, and neuropathic pain.
- Methods of Preparation: Specific methods for preparing these co-crystals are outlined.
- Patent Expiration: The patent expires on April 19, 2030.
- Clinical Implications: The co-crystals offer improved pain relief with potentially reduced side effects.
FAQs
Q: What is the main focus of US Patent 8,598,152?
A: The main focus is on the creation, preparation, and use of co-crystals formed by tramadol and coxibs for pain management.
Q: Who are the inventors and assignees of this patent?
A: The inventors are Carlos Ramon Plata Salaman and Nicolas Tesson, and the assignee is Laboratorios Del Dr. Esteve, S.A.
Q: What are the benefits of forming co-crystals of tramadol and coxibs?
A: The benefits include improved solubility, stability, and potentially reduced side effects, along with enhanced pain relief.
Q: When does the patent expire?
A: The patent expires on April 19, 2030.
Q: What analytical techniques are used to characterize the co-crystals?
A: Techniques such as powder X-ray diffraction, Fourier transform infrared spectroscopy, and melting point determination are used.
Cited Sources
- US8598152B2 - Co-crystals of tramadol and coxibs - Google Patents
- Generic Seglentis Availability - Drugs.com
- Patent Claims and Patent Scope - Hoover Institution
- Drug‑Drug and Drug‑Nutraceutical Cocrystal/Salt as Alternative ... - MDPI
