Detailed Analysis of the Scope and Claims of United States Patent 5,314,697
Introduction
United States Patent 5,314,697, titled "Stable extended release oral dosage composition comprising loratadine and pseudoephedrine," is a significant patent in the pharmaceutical industry, particularly in the field of extended-release formulations. Here, we will delve into the scope, claims, and the broader patent landscape surrounding this invention.
Patent Overview
Inventors and Assignees
The patent was filed by inventors associated with Schering Corporation, now part of Merck & Co., Inc. The assignee is Schering Corporation, Kenilworth, NJ[4].
Publication and Expiration Dates
The patent was published on May 24, 1994, and has since expired, marking the end of its lifetime[4].
Scope of the Invention
Extended Release Formulation
The patent describes a stable extended release oral dosage composition that combines loratadine, an antihistamine, and pseudoephedrine, a nasal decongestant. This formulation is designed to treat patients with signs and symptoms associated with upper respiratory diseases and nasal congestion[4].
Composition Components
- Core Matrix: The core matrix contains loratadine and pseudoephedrine, along with other excipients such as silicon dioxide as a glidant and magnesium stearate as a lubricant.
- Film Coating: The core is coated with a film-forming agent, typically hydroxypropyl methyl cellulose (HPMC), and plasticizers like polyethylene glycol (PEG)[4].
Manufacturing Process
The manufacturing process involves dispersing loratadine in purified water, combining it with HPMC and PEG dispersions, and then coating the core matrix with this mixture. Additional coatings may include a polishing coating and branding with ink[4].
Claims of the Patent
Key Claims
- The patent claims cover the specific composition of the extended release oral dosage, including the core matrix and the film coating.
- It specifies the amounts and types of excipients used, such as silicon dioxide and magnesium stearate.
- The claims also detail the film-forming agents and plasticizers used in the coating process[4].
Claim Specificity
The claims are highly specific, outlining the exact formulation and manufacturing steps necessary to achieve the desired extended release profile. For example, the patent specifies that the core matrix should have a thickness of 0.280 ± 0.010 inches and that the tablet hardness should be maintained within a certain range (22 ± 6 Strong-Cobb Units)[4].
Patent Landscape
Prior Art and Related Patents
The patent builds upon prior art related to extended release formulations, including patents such as U.S. Patent 4,863,931 and U.S. Patent 5,595,997, which also deal with similar formulations and coating techniques[2][5].
Competing Patents
Other patents in the same field, such as U.S. Patent 6,979,463, also describe extended release oral dosage compositions but with different active ingredients or coating techniques. These patents highlight the competitive landscape in the development of extended release pharmaceuticals[2].
Patent Analytics and Claim Coverage
To fully understand the patent landscape, patent analytics tools can be used to track patents by claims and scope concepts. This helps in identifying gaps or opportunities in intellectual property protection and ensures that the claims cover the intended technology effectively[3].
Practical Applications
Clinical Use
The extended release formulation described in the patent is clinically useful for treating patients with chronic conditions such as seasonal allergic rhinitis, providing a sustained release of both loratadine and pseudoephedrine over several hours[4].
Manufacturing and Quality Control
The specific manufacturing process and quality control measures outlined in the patent ensure the consistency and efficacy of the dosage form. This is crucial for maintaining the therapeutic effect and patient compliance[4].
Regulatory Considerations
FDA Approval
The FDA approval process for such formulations involves rigorous testing to ensure the safety, efficacy, and stability of the drug product. The approval letter for a similar formulation (loratadine and pseudoephedrine sulfate) highlights the regulatory scrutiny these products undergo[5].
Key Takeaways
- Extended Release Technology: The patent showcases advanced extended release technology, combining loratadine and pseudoephedrine for sustained therapeutic effect.
- Specific Formulation: The claims are highly specific regarding the composition and manufacturing process, ensuring consistency and efficacy.
- Patent Landscape: The patent is part of a broader landscape of extended release formulations, with competing patents and prior art influencing its scope and claims.
- Clinical and Manufacturing Significance: The formulation is clinically useful and requires precise manufacturing and quality control to maintain therapeutic efficacy.
FAQs
Q: What are the primary active ingredients in the extended release formulation described in U.S. Patent 5,314,697?
A: The primary active ingredients are loratadine, an antihistamine, and pseudoephedrine, a nasal decongestant.
Q: What is the purpose of the film coating in the extended release formulation?
A: The film coating, typically made of hydroxypropyl methyl cellulose (HPMC) and polyethylene glycol (PEG), helps in achieving the extended release profile of the active ingredients.
Q: How does the manufacturing process ensure the stability of the dosage form?
A: The manufacturing process involves specific steps, including the use of glidants and lubricants, and precise coating techniques to ensure the stability and consistency of the dosage form.
Q: Is the patent still in effect?
A: No, the patent has expired, marking the end of its lifetime.
Q: What regulatory body oversees the approval of such pharmaceutical formulations in the United States?
A: The FDA (Food and Drug Administration) oversees the approval process for pharmaceutical formulations in the United States.
Sources
- United States Patent 6,979,463 B2 - Stable extended release oral dosage composition[2].
- United States Patent 5,314,697 A - Stable extended release oral dosage composition comprising loratadine and pseudoephedrine[4].
- Patent Analytics | Intellectual Property Law - Schwegman[3].
- FDA Approval Letter for Loratadine and Pseudoephedrine Sulfate - FDA[5].
