United States Patent 10,058,554: A Detailed Analysis of Scope, Claims, and Patent Landscape
Introduction
The United States Patent 10,058,554, titled "Sustained Release Small Molecule Drug Formulation," is a significant patent in the pharmaceutical industry, particularly in the field of drug delivery systems. This patent, granted to inventors who have developed innovative formulations for sustained release of small molecule drugs, is crucial for understanding the current state and future directions of drug formulation technology.
Patent Overview
Invention Description
The patent describes an injectable depot formulation designed for the sustained release of small molecule drugs. This formulation includes a biocompatible polymer, an organic solvent combined with the polymer to form a viscous gel, and the small molecule drug incorporated within this gel. The invention is based on the discovery that incorporating a sparingly soluble small molecule drug into a depot gel vehicle results in a near zero-order release profile in vivo, characterized by minimal lag time and burst release[4].
Key Components
- Biocompatible Polymer: The polymer used is biocompatible and may be bioerodible, gradually decomposing or eroding in situ.
- Organic Solvent: The solvent is present in the depot gel vehicle in a specific weight range, typically between 20% to 95% by weight.
- Small Molecule Drug: The drugs used are sparingly soluble in water, with a preferred molecular weight range of 200 to 2,000 Daltons.
Scope of the Patent
Claims
The patent includes several claims that define the scope of the invention:
- Claim 1: An injectable depot formulation comprising a biocompatible polymer, an organic solvent, and a small molecule drug, where the formulation exhibits an in vivo release profile with a C max to C min ratio less than 200 and a lag time less than 0.2[4].
- Dependent Claims: These include variations of the formulation, such as different types of polymers, solvents, and drug concentrations.
Release Profile
The release profile is a critical aspect of the patent, ensuring a controlled release over at least a week, and more preferably over a month. The profile is characterized by:
- C max to C min Ratio: Less than 200.
- Lag Time: Less than 0.2.
- Zero-Order Release: The formulation achieves a near zero-order release, which is surprising given the prevailing thought in the art that such a release profile is virtually impossible without special steps like coatings or microencapsulation[4].
Patent Landscape
Prior Art
The patent builds upon existing knowledge in drug formulation but introduces a novel approach to achieving sustained release. Prior art keywords include copolymer, formulation, lactic acid, and others, indicating the integration of various existing technologies into this new invention[4].
International Patent Databases
To understand the global patent landscape, one can refer to international patent databases such as those provided by the European Patent Office (EPO), Japan Patent Office (JPO), World Intellectual Property Organization (WIPO), and others. These databases offer insights into similar or related patents filed in different jurisdictions[1].
Competing Patents
Other patents in the field of sustained release formulations may offer competing or complementary technologies. For instance, patents related to microencapsulation, coatings, or other drug delivery systems could be relevant. A thorough search using resources like the USPTO's Patent Public Search tool or the Global Dossier can help identify these patents[1].
Economic and Research Implications
Patent Claims Research Dataset
The USPTO's Patent Claims Research Dataset provides detailed information on claims from U.S. patents, including those related to drug formulations. This dataset can be used to analyze trends and measurements of patent scope, offering insights into the economic and research implications of patents like 10,058,554[3].
Market Impact
The sustained release formulation described in this patent has significant market potential, particularly in treating chronic conditions where consistent drug levels are crucial. The ability to achieve a near zero-order release profile without the need for complex coatings or microencapsulation makes this formulation highly attractive for pharmaceutical companies.
Legal Status and Enforcement
Current Status
As of the latest information, the patent is listed as active. However, it is important to note that the legal status is an assumption and not a legal conclusion, and Google or other search engines may not have performed a legal analysis[4].
Office Actions and Litigation
The Global Dossier and other resources provided by the USPTO can help track office actions and any litigation related to this patent. Understanding these aspects is crucial for enforcing the patent and navigating potential legal challenges[1].
Practical Applications
Clinical Implications
The formulation described in this patent has several clinical implications, including the potential to improve patient compliance by reducing the frequency of drug administration. The controlled release profile ensures that the drug concentration in the body remains within a therapeutic window, minimizing side effects and maximizing efficacy.
Manufacturing Considerations
The manufacturing process for this formulation involves combining the biocompatible polymer and organic solvent to form a viscous gel, followed by the incorporation of the small molecule drug. This process must be carefully controlled to ensure the desired release profile is achieved.
Future Directions
Research and Development
Future research could focus on expanding the range of small molecule drugs that can be used with this formulation, as well as exploring different polymers and solvents to further optimize the release profile.
Regulatory Approvals
Obtaining regulatory approvals from agencies such as the FDA will be crucial for bringing this formulation to market. Clinical trials and other regulatory requirements must be met to ensure the safety and efficacy of the formulation.
Key Takeaways
- Innovative Formulation: The patent describes a novel injectable depot formulation for sustained release of small molecule drugs.
- Near Zero-Order Release: The formulation achieves a near zero-order release profile, which is a significant advancement in drug delivery technology.
- Biocompatible Components: The use of biocompatible polymers and organic solvents ensures the formulation is safe for use in the human body.
- Market Potential: The formulation has significant market potential, particularly for treating chronic conditions.
- Regulatory and Legal Considerations: Understanding the legal status and navigating regulatory approvals are crucial for commercialization.
FAQs
Q: What is the main innovation of United States Patent 10,058,554?
A: The main innovation is the development of an injectable depot formulation that achieves a near zero-order release profile for small molecule drugs, characterized by minimal lag time and burst release.
Q: What are the key components of the formulation described in the patent?
A: The key components include a biocompatible polymer, an organic solvent, and a small molecule drug that is sparingly soluble in water.
Q: How does the release profile of this formulation differ from existing technologies?
A: The formulation achieves a near zero-order release profile, which is unusual without special steps like coatings or microencapsulation, and it has a C max to C min ratio less than 200 and a lag time less than 0.2.
Q: What are the potential clinical implications of this patent?
A: The formulation could improve patient compliance by reducing the frequency of drug administration and ensure that the drug concentration remains within a therapeutic window, minimizing side effects and maximizing efficacy.
Q: How can one search for similar patents or prior art related to this invention?
A: One can use resources like the USPTO's Patent Public Search tool, Global Dossier, and international patent databases such as those provided by the EPO, JPO, and WIPO.
Sources
- USPTO - Search for patents. Retrieved from https://www.uspto.gov/patents/search
- U.S. Patent and Trademark Office (USPTO) | USAGov. Retrieved from https://www.usa.gov/agencies/u-s-patent-and-trademark-office
- Patent Claims Research Dataset - USPTO. Retrieved from https://www.uspto.gov/ip-policy/economic-research/research-datasets/patent-claims-research-dataset
- US10058554B2 - Sustained release small molecule drug formulation - Google Patents. Retrieved from https://patents.google.com/patent/US10058554B2/en
