Detailed Analysis of the Scope and Claims of United States Patent 6,727,286
Introduction
United States Patent 6,727,286, titled "Pharmaceutical composition of 2-(4-isobutylphenyl) propionic acid," is a significant patent in the pharmaceutical industry, particularly in the formulation and administration of ibuprofen. Here, we will delve into the scope, claims, and the broader patent landscape surrounding this invention.
Background of the Patent
The patent, filed on November 2, 2001, and granted on April 27, 2004, pertains to a pharmaceutical composition that includes an aqueous solution of ibuprofen and arginine. Ibuprofen, known for its analgesic, anti-inflammatory, and antipyretic properties, is a widely used nonsteroidal anti-inflammatory drug (NSAID)[1][4].
Scope of the Patent
Pharmaceutical Composition
The patent describes a unique pharmaceutical composition that combines ibuprofen with arginine in an aqueous solution. This formulation is designed to enhance the solubility and bioavailability of ibuprofen, which is typically poorly soluble in water. The molar ratio of arginine to ibuprofen is a critical aspect of this composition, ensuring optimal solubilization and stability[1].
Therapeutic Applications
The invention is intended for treating conditions such as pain, inflammation, fever, and other conditions alleviated by ibuprofen. The aqueous solution can be administered in various forms, including injectable solutions, which is a significant advancement over traditional oral or topical formulations[1][4].
Claims of the Patent
Key Claims
- The patent claims a pharmaceutical composition comprising an aqueous solution of ibuprofen and arginine, with a specified molar ratio.
- It also claims methods of treating pain, inflammation, fever, and other related conditions using this composition.
- The claims include specific pharmacokinetic parameters such as maximum concentration (Cmax), area under the curve (AUC), and half-life (t1/2), which were determined through clinical studies[1].
Dependent Claims
Dependent claims further detail the composition, including the concentration of ibuprofen and arginine, the pH range of the solution, and the method of preparation. These claims provide a comprehensive description of how the composition should be formulated and administered[1].
Prior Art and Related Patents
Previous Formulations
Previous patents, such as U.S. Pat. No. 5,200,558 and U.S. Pat. No. 4,279,926, described the use of basic amino acid salts of propionic acids, including ibuprofen, for pain relief and inflammatory conditions. However, these approaches required the formation of a salt before solubilization, which was a significant drawback[1].
Advancements
The current patent (U.S. Pat. No. 6,727,286) improves upon these earlier methods by providing a direct aqueous solution without the need for salt formation, making the process more efficient and the product more stable[1].
Patent Landscape
Patent Scope Metrics
The scope of a patent can be measured using metrics such as independent claim length and independent claim count. These metrics help in assessing the breadth and clarity of the patent claims. In the case of U.S. Pat. No. 6,727,286, the claims are specific and well-defined, indicating a narrower scope that is associated with higher grant probabilities and shorter examination processes[3].
Cited By and Family Applications
The patent has been cited by 16 other patents and has a continuation-in-part application (US10/739,050), indicating its influence and relevance in the field of pharmaceutical formulations[1].
Clinical and Pharmacokinetic Data
Pharmacokinetic Parameters
The patent includes detailed pharmacokinetic data from clinical studies, which were conducted to evaluate the bioavailability and efficacy of the ibuprofen-arginine solution. Parameters such as Cmax, AUC, and t1/2 were analyzed to ensure the composition met the required therapeutic standards[1].
Commercial Applications
Caldolor™
The patent is associated with the commercial product Caldolor™, an intravenous ibuprofen solution manufactured by Cumberland Pharmaceuticals Inc. This product is diluted to a final concentration of 4 mg/mL or less before infusion, highlighting the practical application of the patented composition[2].
Conclusion
United States Patent 6,727,286 represents a significant advancement in the formulation of ibuprofen, offering a stable and bioavailable aqueous solution that enhances the therapeutic efficacy of the drug. The patent's scope and claims are well-defined, addressing specific needs in the pharmaceutical industry.
Key Takeaways
- Pharmaceutical Composition: The patent describes an aqueous solution of ibuprofen and arginine.
- Therapeutic Applications: The composition is used for treating pain, inflammation, fever, and related conditions.
- Claims: Specific molar ratios, pharmacokinetic parameters, and methods of treatment are claimed.
- Prior Art: Improves upon earlier methods by avoiding the need for salt formation.
- Patent Landscape: Cited by 16 other patents and has a continuation-in-part application.
- Clinical Data: Includes detailed pharmacokinetic parameters from clinical studies.
- Commercial Application: Associated with the commercial product Caldolor™.
FAQs
Q: What is the main composition described in U.S. Pat. No. 6,727,286?
A: The main composition is an aqueous solution of ibuprofen and arginine.
Q: What are the therapeutic applications of this composition?
A: The composition is used for treating pain, inflammation, fever, and other related conditions.
Q: How does this patent improve upon previous formulations?
A: It avoids the need for salt formation before solubilization, making the process more efficient.
Q: What is the commercial product associated with this patent?
A: The commercial product is Caldolor™, an intravenous ibuprofen solution.
Q: What pharmacokinetic parameters are included in the patent?
A: Parameters such as Cmax, AUC, and t1/2 are included.
Sources
- US6727286B2 - Pharmaceutical composition of 2-(4-isobutylphenyl) propionic acid - Google Patents
- Dilution Caldolor ™ - Ibuprofen - GlobalRPH
- Patent Claims and Patent Scope - SSRN
- Pharmaceutical composition of 2-(4-isobutylphenyl) propionic acid - PubChem
- Treating patients with intravenous ibuprofen - Google Patents
