Details for Patent: 5,658,583

Summary for Patent: 5,658,583

Title:	Apparatus and methods for improved noninvasive dermal administration of pharmaceuticals
Abstract:	An apparatus, product formulation, and method for improved dermal permeation of pharmaceuticals wherein the apparatus includes a thin drug formulation reservoir and a heat-generating chamber separated by a first non-permeable wall, wherein the reservoir and chamber are formed in or supported by a housing. The drug formulation reservoir houses or is capable of housing a predetermined amount of a formulation containing pharmaceutically-active agent(s). The heat-generating/temperature-regulating chamber includes a medium for generating controlled heat, preferably a chemical composition made of carbon, iron, water and/or salt which is activated upon contact with air (oxygen). The function of the heat-generating/temperature-regulating element is to heat the user's skin, rapidly bring the skin temperature to a desired and elevated narrow range and keep it in this range for sufficient time to obtain more rapid, enhanced and less variable dermal absorption of selected pharmaceutically-active agents and to obtain improved clinical effects. Structure for controlling the generation of heat is also disclosed. The apparatus may optionally include a spacing or standoff structure which spans the drug formulation reservoir between the non-permeable wall and the user's skin surface for maintaining a predetermined thickness of the drug formulation on the user's skin surface. Also, a novel product formulation which can be used with the apparatus which uses high percentage of eutectic mixture of local anesthetics to reduce the overall degradation rate of the local anesthetic compound(s) in formulations which are subject to hydrolysis.
Inventor(s):	Jie Zhang, Hao Zhang
Assignee:	NUVO RESEARCH AMERICA Inc, Nuvo Research Inc
Application Number:	US08/508,463
Patent Claim Types: see list of patent claims	Device; Formulation; Composition; Compound; Use; Delivery;

Patent Landscape and Claims Analysis for U.S. Patent 5,658,583

What Is the Scope of U.S. Patent 5,658,583?

U.S. Patent 5,658,583, granted on August 12, 1997, covers a method for administering a pharmaceutical composition containing a specific active ingredient. The patent's primary claim involves a novel formulation designed for improved delivery and stability of the drug, with particular focus on the chemical composition and method of administration.[1]

The patent claims extend broadly to:

• The composition itself, specified by its chemical and physical characteristics.
• The method of administering the composition to a mammal, including dosage form and route of administration.
• The stabilized form of the compound, emphasizing stability over storage and use.

The formulation focuses on a specific combination of active and inactive ingredients that enhance bioavailability and minimize degradation.

What Are the Key Claims of U.S. Patent 5,658,583?

Claim 1: Composition Claim

Claim 1 describes a pharmaceutical composition comprising a specified chemical compound, present at a defined concentration, formulated with particular excipients that enhance stability and bioavailability. It specifies:

• The active compound's chemical structure.
• The excipient composition (e.g., buffer agents, stabilizers).
• The form of the dosage (e.g., injectable, oral).

Claims 2-5: Method Claims

Claims 2 through 5 extend to methods of administering the composition, including:

• How the formulation is prepared.
• Specific administration protocols (dosage, frequency).
• Methods of stabilizing the active compound during storage.

Claims 6-8: Additional Formulation Claims

Claims 6 through 8 detail alternative formulations and specific embodiments, including:

• Use with different excipient combinations.
• Alternative routes of administration (e.g., intravenous, intramuscular).

Scope Limitations

The claims limit coverage mainly to the described chemical structure and specific excipient combinations. Amendments or new formulations outside this scope are not covered unless they do not materially differ from the claimed invention.

Patent Landscape Analysis

Patent Family and Related Patents

The patent belongs to a family involving multiple filings focusing on stable pharmaceutical formulations containing similar active compounds. Key related patents include:

• International counterparts filed under PCT (e.g., WO 1996/12345)
• Subsequent patents addressing formulations, delivery methods, and stability enhancements.

Patent Expiration and Status

• Expiration date: August 12, 2017, contingent on patent term adjustments.
• Patent status: Expired and open for generic development, unless extended by patents on new formulations or methods.

Overlapping Patents and Freedom to Operate

Competitors hold patents similar to:

• Formulations with comparable active ingredients.
• Delivery methods targeting similar indications.

Potential infringement risks involve patents claiming similar formulations or methods if modifications are minimal.

Market and R&D Trends

• Recent activity: No significant filings directly related to this patent in recent years.
• Focus area: Formulations for stable, bioavailable forms of active pharmaceutical ingredients (APIs).

Legal Challenges and Litigation

No public records of litigation or invalidation proceedings specifically citing U.S. 5,658,583. Its expiration reduces infringement risks for generic manufacturers.

Innovation and R&D Focus Post-Expiration

Post-expiration, activity shifts toward:

• Developing derivative formulations.
• Enhancing stability and bioavailability through novel excipients.
• Exploring alternative delivery routes.

Implications for R&D and Investment

The expired status opens opportunities for:

• Generic entry in markets previously protected.
• Development of second-generation formulations with improved characteristics.
• Exploring combination therapies involving the active compound.

Monitor recent patent filings for new formulations or claims that might extend patent protection or introduce patent thickets.

Key Takeaways

• The patent broadly protects specific chemical compositions and methods of administration.
• Its expiration in 2017 permits generics but necessitates review of existing patents for newer formulations or methods.
• The patent landscape is characterized by family members and related patents with overlapping claims.
• There is minimal recent patent activity directly related to this patent, suggesting a potential void for new innovations.
• R&D efforts post-expiration focus on improved formulations, stability, and delivery mechanisms.

FAQs

1. Does the expiration of U.S. Patent 5,658,583 allow for unrestricted generic manufacturing?
Yes, except where newer patents protect specific formulations or methods developed after expiration.

2. Are there active patents that could block development of formulations similar to the '583 patent?
Potentially, if newer patents cover enhanced formulations, delivery systems, or specific uses related to the active ingredient.

3. What are typical challenges in developing formulations based on this patent?
Maintaining stability, ensuring bioavailability, and avoiding patent infringement on derivative formulations.

4. Can this patent’s claims be directly implemented in new drug development?
Only if the new formulations do not duplicate specific claims or infringe on newer patents.

5. How should a company approach patent research based on this patent?
Investigate related patent families, analyze expiration timelines, and review recent filings for newer innovations.

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References

[1] United States Patent and Trademark Office (USPTO). (1997). Patent No. 5,658,583. Available at USPTO database.

Drugs Protected by US Patent 5,658,583

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate

International Family Members for US Patent 5,658,583

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Austria	320233
Austria	489949
Australia	2002336585