United States Patent 5,639,480: A Detailed Analysis of Scope, Claims, and Patent Landscape
Introduction
The United States Patent 5,639,480, titled "Sustained release formulations of water soluble peptides," is a significant patent in the field of pharmaceuticals, particularly in the development of controlled drug release systems. This patent, granted to innovators in the field of biodegradable and biocompatible polymers, has far-reaching implications for the delivery of water-soluble peptides.
Background and Prior Art
Before delving into the specifics of US 5,639,480, it is essential to understand the prior art that laid the groundwork for this invention. Previous patents, such as U.S. Pat. No. 3,773,919, described controlled drug release formulations using biodegradable and biocompatible linear polylactide or polylactide-co-glycolide polymers[1][2].
Invention Overview
The patent US 5,639,480 discloses microparticles comprising a polypeptide, preferably somatostatin or an analog or derivative thereof, more preferably octreotide. These microparticles are designed for sustained release, ensuring a continuous and controlled delivery of the peptide over an extended period.
Key Components
- Polypeptide: The primary active ingredient is a water-soluble peptide, such as somatostatin or its analogs like octreotide.
- Biodegradable Polymer: The peptide is encapsulated in a biodegradable and biocompatible polymer, typically polylactide or polylactide-co-glycolide.
- Microparticles: The formulation involves the creation of microparticles, which can be produced using various techniques such as phase separation, spray drying, or triple emulsion[1][2].
Claims and Scope
The patent includes several claims that define the scope of the invention:
Independent Claims
- The patent claims cover the composition of the microparticles, including the specific types of peptides and polymers used.
- It also claims the process for producing these microparticles, which involves dispersing the peptide in a solvent, adding a phase-inducing agent, and hardening the microparticles in an oil-in-water emulsion[1][2].
Dependent Claims
- These claims further specify the characteristics of the microparticles, such as their size, shape, and the rate of peptide release.
- They also cover various forms of the sustained release formulations, including implants and injectable solutions[1][2].
Production Process
The process for producing these microparticles is detailed in the patent:
Step-by-Step Process
- Step a): A solution of the peptide is added and dispersed in an appropriate solvent, which is a non-solvent for the polymer.
- Step b): A phase-inducing agent is added to the dispersion to induce microparticle formation.
- Step c): The mixture is then added to an oil-in-water emulsion to harden the microparticles[1].
Patent Landscape
The patent landscape surrounding US 5,639,480 is complex and influenced by several factors:
Related Patents
- Other patents, such as U.S. Pat. No. 4,293,539, describe anti-bacterial formulations in microparticle form, indicating a broader application of microparticle technology in pharmaceuticals[1][2].
- European patent applications, like 0 203 031, describe somatostatin octapeptide analogs, highlighting the international scope of research in this area[1][2].
Patent Scope Metrics
Research on patent scope, such as the study by Alan C. Marco et al., suggests that the scope of a patent can be measured by metrics like independent claim length and independent claim count. These metrics can indicate the breadth and clarity of the patent claims, which are crucial for understanding the patent's impact on innovation and litigation[3].
Impact on Pharmaceutical Industry
The invention disclosed in US 5,639,480 has significant implications for the pharmaceutical industry:
Controlled Drug Release
- The sustained release formulations ensure a consistent and prolonged delivery of the peptide, which can improve patient compliance and therapeutic outcomes.
- This technology can be applied to various water-soluble peptides, expanding the range of treatable conditions[1][2].
Biodegradable and Biocompatible Materials
- The use of biodegradable and biocompatible polymers reduces the risk of adverse reactions and ensures the safe degradation of the microparticles within the body[1][2].
Future Directions
The technology described in US 5,639,480 opens up several avenues for future research and development:
Advanced Delivery Systems
- Further innovations in microparticle technology could lead to more sophisticated delivery systems, such as targeted delivery to specific tissues or organs.
- Integration with other technologies, like nanotechnology, could enhance the efficacy and precision of peptide delivery[1][2].
Expanding Therapeutic Applications
- The sustained release formulations could be adapted for other therapeutic peptides, expanding the treatment options for various diseases.
- This technology could also be applied to other areas, such as vaccine delivery and gene therapy[1][2].
Key Takeaways
- Sustained Release Formulations: The patent describes microparticles for sustained release of water-soluble peptides, ensuring continuous and controlled delivery.
- Biodegradable Polymers: The use of biodegradable and biocompatible polymers ensures safe and effective delivery.
- Production Process: The process involves dispersing the peptide in a solvent, adding a phase-inducing agent, and hardening the microparticles in an oil-in-water emulsion.
- Impact on Industry: The invention has significant implications for improving patient compliance and therapeutic outcomes, and it opens up future directions for advanced delivery systems and expanded therapeutic applications.
FAQs
What is the primary active ingredient in the microparticles described in US 5,639,480?
The primary active ingredient is a water-soluble peptide, preferably somatostatin or its analogs like octreotide.
What type of polymers are used in the microparticles?
The microparticles use biodegradable and biocompatible polymers, typically polylactide or polylactide-co-glycolide.
How are the microparticles produced?
The microparticles are produced by dispersing the peptide in a solvent, adding a phase-inducing agent, and hardening the mixture in an oil-in-water emulsion.
What are the potential therapeutic applications of this technology?
The technology can be applied to various diseases treated with water-soluble peptides, and it has potential applications in vaccine delivery and gene therapy.
How does this patent impact the pharmaceutical industry?
The patent improves patient compliance and therapeutic outcomes by ensuring sustained and controlled delivery of peptides, and it opens up avenues for future innovations in drug delivery systems.
Sources
- US5639480A - Sustained release formulations of water soluble peptides - Google Patents
- US5538739A - Sustained release formulations of water soluble peptides - Google Patents
- Patent Claims and Patent Scope - Hoover Institution Working Paper Series No. 16001
