Detailed Analysis of the Scope and Claims of United States Patent 5,922,682
Introduction
United States Patent 5,922,682, titled "Polyol esters, their preparation and use in depot forms of pharmacologically active agents," is a significant patent in the field of pharmaceuticals, particularly in the development of depot formulations. This analysis will delve into the scope, claims, and the broader patent landscape surrounding this invention.
Scope of the Invention
The patent describes the preparation and use of novel polyol esters, specifically those derived from polyols containing at least three hydroxyl groups and having a molecular weight of up to 20,000. These polyol esters are combined with poly- or co-poly-lactic acid residues, each with a molecular weight of at least 5,000, to form depot formulations for pharmacologically active agents[1].
Depot Formulations
Depot formulations are designed to release active pharmaceutical ingredients over an extended period, providing a sustained therapeutic effect. The polyol esters described in this patent are particularly useful for parenteral depot formulations, which are administered via injection or implantation.
Active Agents
The depot formulations can be used to administer a wide variety of pharmacologically active agents, including but not limited to:
- Contraceptives
- Sedatives
- Steroids
- Sulphonamides
- Vaccines
- Vitamins
- Anti-migraine drugs
- Enzymes
- Bronchodilators
- Cardiovascular drugs
- Analgesics
- Antibiotics
- Antigens
- Anti-convulsive drugs
- Anti-inflammatory drugs
- Anti-parkinson drugs
- Prolactin secretion inhibitors
- Anti-asthmatic drugs
- Geriatrics
- Anti-malarial drugs[1].
Claims of the Patent
The patent includes several key claims that define the scope of the invention:
Claim 1
A polyol ester having a molecular weight of 20,000 to 200,000, where the polyol contains at least three hydroxyl groups, and at least one hydroxyl group is in the form of an ester with a poly- or co-poly-lactic acid residue[5].
Claim Details
- The polyol esters must have a specific molecular weight range.
- The polyol must contain at least three hydroxyl groups.
- At least one hydroxyl group must be esterified with a poly- or co-poly-lactic acid residue.
- The poly- or co-poly-lactic acid residue must have a molecular weight of at least 5,000[1][5].
Preparation of Polyol Esters
The patent outlines the methods for preparing these polyol esters, which involve the reaction of polyols with lactic acid or its derivatives. This process can be tailored to produce esters with varying molecular weights and properties, making them suitable for different pharmaceutical applications[1].
Use in Pharmaceutical Formulations
The polyol esters are used to create depot formulations that can be administered in various forms, such as injectable solutions, suspensions, or implants. These formulations are designed to release the active pharmaceutical ingredient over a prolonged period, enhancing patient compliance and therapeutic efficacy[1].
Patent Landscape
Related Patents
Other patents, such as the Canadian patent CA2501978A1, also discuss the use of similar polymer-based formulations for pharmaceutical applications. For example, this patent describes the use of octreotide microparticles in pharmaceutical compositions, which involves similar polymer chemistry[2].
Intellectual Property Protection
Understanding the patent landscape is crucial for companies involved in pharmaceutical research and development. Tools like patent analytics can help identify which patents and claims are actively protecting intellectual property and where gaps or opportunities exist. This involves categorizing patents by claims and scope concepts to filter, search, and analyze large numbers of patent claims efficiently[3].
Industry Impact
The invention described in US Patent 5,922,682 has significant implications for the pharmaceutical industry:
Sustained Release Formulations
The ability to create sustained-release formulations using polyol esters enhances the therapeutic profile of various drugs by reducing the frequency of administration and improving patient compliance.
Broad Applicability
The wide range of active agents that can be formulated using these polyol esters makes this technology versatile and valuable across multiple therapeutic areas.
Competitive Advantage
Companies that hold or license this patent can gain a competitive advantage by developing unique depot formulations that offer improved efficacy and convenience over traditional dosage forms.
Key Takeaways
- Polyol Esters: The patent describes novel polyol esters with poly- or co-poly-lactic acid residues for depot formulations.
- Depot Formulations: These formulations are designed for sustained release of pharmacologically active agents.
- Broad Applicability: The technology can be applied to a wide range of active agents across various therapeutic areas.
- Intellectual Property: Understanding the patent landscape is crucial for protecting and leveraging this technology.
FAQs
What is the primary use of the polyol esters described in US Patent 5,922,682?
The primary use is in the creation of depot formulations for pharmacologically active agents, providing sustained release over an extended period.
Which types of active agents can be formulated using these polyol esters?
A wide variety of active agents, including contraceptives, sedatives, steroids, sulphonamides, vaccines, vitamins, and many others.
How are the polyol esters prepared?
The polyol esters are prepared through the reaction of polyols with lactic acid or its derivatives, resulting in esters with specific molecular weights and properties.
What is the significance of the molecular weight range of the polyol esters?
The molecular weight range (20,000 to 200,000) is critical for ensuring the appropriate physical and chemical properties necessary for depot formulations.
How does this patent impact the pharmaceutical industry?
It provides a versatile technology for creating sustained-release formulations, enhancing therapeutic efficacy and patient compliance, and offering a competitive advantage to companies that leverage this technology.
Sources
- US5922682A - Polyol esters, their preparation and use in depot forms of pharmacologically active agents - Google Patents
- CA2501978A1 - Pharmaceutical composition comprising octreotide microparticles - Google Patents
- Patent Analytics | Intellectual Property Law - SLWIP
- OCTREOTIDE ACETATE - Generic Drug Details - DrugPatentWatch
- Claims for Patent: 5,922,682 - DrugPatentWatch
