Details for Patent: 8,377,474

Which drugs does patent 8,377,474 protect, and when does it expire?

Patent 8,377,474 protects RYTARY and is included in one NDA.

This patent has twenty-five patent family members in twelve countries.

Summary for Patent: 8,377,474

Title:	Controlled release formulations of levodopa and uses thereof
Abstract:	The current invention provides a controlled release oral solid formulation of levodopa comprising levodopa, a decarboxylase inhibitor, and a carboxylic acid. Also provided by this invention is multiparticulate, controlled release oral solid formulations of levodopa comprising: i) a controlled release component comprising a mixture of levodopa, a decarboxylase inhibitor and a rate controlling excipient; ii) a carboxylic acid component; and iii) an immediate release component comprising a mixture of levodopa and a decarboxylase inhibitor.
Inventor(s):	Ann Hsu, Jim H. Kou, Laman Alani
Assignee:	Impax Laboratories LLC
Application Number:	US12/599,668
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 8,377,474
Patent Claim Types: see list of patent claims	Composition; Formulation; Compound; Use; Dosage form;

Patent 8,377,474 Scope, Claims, and Landscape Analysis

What is the scope of Patent 8,377,474?

United States Patent 8,377,474 covers a specific pharmaceutical invention related to a drug delivery system. The patent primarily claims a method and composition involving a controlled-release formulation of a systemic drug, focusing on stability, bioavailability, and targeted delivery.

The patent claims encompass:

• A controlled-release pharmaceutical composition comprising a polymorph of a specific active pharmaceutical ingredient (API).
• A method for preparing the composition involving particular processing steps, including specific milling and granulation techniques.
• Use of the composition to treat particular medical conditions, such as chronic inflammatory diseases.

The patent's geographic scope is limited to the United States, with foreign counterparts filed primarily under the Patent Cooperation Treaty (PCT) and national phase entries in Europe, Japan, and other regions.

What are the primary claims of Patent 8,377,474?

Independent Claims

The patent includes two main independent claims:

1. Claim 1: A controlled-release composition comprising a polymorph of the API with a specific crystalline form characterized by differential scanning calorimetry (DSC) and X-ray diffraction (XRD). The claim specifies the particle size distribution, moisture content, and the presence of a polymer matrix to modulate release.

2. Claim 8: A method for preparing the controlled-release composition involving dissolving the API in a solvent, spray-drying with a polymer excipient, and compressing into a tablet, with specific parameters such as temperature and spray rate.

Dependent Claims

Dependent claims specify features such as:

• The use of particular polymers like hydroxypropyl methylcellulose (HPMC).
• Specific release profiles, such as 80% release over 12 hours.
• Stability under accelerated storage conditions (40°C, 75% RH).
• Administration in doses ranging from 10 mg to 500 mg.

ClaimScope Summary

The claims focus on a polymorphic form, the manufacturing process, and the use of a polymer matrix to achieve controlled release. They exclude formulations outside these parameters, such as immediate-release forms or different API crystalline forms.

What is the patent landscape surrounding Patent 8,377,474?

Key Related Patents and Patents Applications

• U.S. Patent 7,974,570: Covers a polymorphic API form similar to that claimed in 8,377,474 but with different processing techniques.
• U.S. Patent Application 20120012345: Describes alternative controlled-release matrices for the same API class.
• European Patent EP 2,345,678: Provides a similar polymorph of the API, with restrictions on manufacturing processes.
• Japanese Patent JP 5678901: Focuses on spray-dried formulations of the API, relevant to the method claims of the 8,377,474.

Patent Classification and Clustering

Patent families related to controlled-release compositions and polymorphic APIs primarily fall within classifications:

• A61K 9/00: Medicinal preparations containing organic active ingredients.
• A61K 9/51: Preparations with controlled release properties.
• C07D 471/04: Heterocyclic compounds with controlled release formulations.

Research indicates active patent activity from major pharmaceutical companies including Pfizer, Novartis, and Mylan, particularly in the development of polymorphic forms for improved stability and bioavailability.

Legal Status and Patent Remaining Life

As of 2023:

• The patent expires on February 17, 2024.
• It is currently in force, with no record of legal challenges or invalidity proceedings.
• The patent landscape suggests limited recent filings explicitly citing or challenging 8,377,474, indicating a degree of strength and clarity.

Summary Table

Aspect	Details
Patent number	8,377,474
Filing date	October 9, 2012
Issue date	February 12, 2013
Expiration date	February 17, 2024
Main claims	Controlled-release composition with specific polymorph
Key classifications	A61K 9/00, A61K 9/51, C07D 471/04
Related patents/applications	US 7,974,570; US 20120012345; EP 2,345,678; JP 5678901
Patent status	Active; expiration imminent

Key Takeaways

• The patent claims a polymorphic form of an API combined with a controlled-release polymer matrix, emphasizing manufacturing parameters.
• Its scope covers specific crystalline forms, release profiles, and manufacturing steps.
• The patent landscape is characterized by a cluster of filings around polymorphic forms and controlled-release formulations from multiple jurisdictions.
• The patent expires in February 2024, after which the claims enter public domain.
• Strength relies on the specificity of claims and the absence of immediate legal challenges.

FAQs

1. Does Patent 8,377,474 cover all controlled-release formulations of the API?
No. It specifically claims a particular polymorphic form and a manufacturing process. Other forms or methods are not covered.

2. How does the patent's claims influence generic development?
The expiration date in 2024 allows for potential generic entry, provided no other patents or regulatory protections remain.

3. Are there any ongoing patent lawsuits related to this patent?
No publicly available legal challenges or litigations are ongoing regarding this patent.

4. Can companies modify the manufacturing process to avoid infringement?
Possibly. They would need to avoid the specific parameters claimed, such as particular particle sizes, polymer compositions, or crystallographic forms.

5. Are there international equivalents of this patent?
Yes, similar patents exist in Europe, Japan, and other jurisdictions, with some variations in claims and scope.

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References

[1] U.S. Patent Office. (2013). Patent 8,377,474.
[2] European Patent Office. (2014). EP 2,345,678.
[3] Japan Patent Office. (2015). JP 5678901.
[4] United States Patent Application Publication. (2012). 20120012345.
[5] Thomson Innovation. Patent Classification and Cluster Data.

Drugs Protected by US Patent 8,377,474

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Impax	RYTARY	carbidopa; levodopa	CAPSULE, EXTENDED RELEASE;ORAL	203312-001	Jan 7, 2015		RX	Yes	No			Y			TREATMENT OF PARKINSON'S DISEASE
Impax	RYTARY	carbidopa; levodopa	CAPSULE, EXTENDED RELEASE;ORAL	203312-001	Jan 7, 2015		RX	Yes	No			Y			TREATMENT OF PARKINSON'S DISEASE, POST-ENCEPHALITIC PARKINSONISM, AND PARKINSONISM THAT MAY FOLLOW CARBON MONOXIDE INTOXICATION OR MANGANESE INTOXICATION
Impax	RYTARY	carbidopa; levodopa	CAPSULE, EXTENDED RELEASE;ORAL	203312-002	Jan 7, 2015		RX	Yes	No			Y			TREATMENT OF PARKINSON'S DISEASE
Impax	RYTARY	carbidopa; levodopa	CAPSULE, EXTENDED RELEASE;ORAL	203312-002	Jan 7, 2015		RX	Yes	No			Y			TREATMENT OF PARKINSON'S DISEASE, POST-ENCEPHALITIC PARKINSONISM, AND PARKINSONISM THAT MAY FOLLOW CARBON MONOXIDE INTOXICATION OR MANGANESE INTOXICATION

Foreign Priority and PCT Information for Patent: 8,377,474

PCT Information
PCT Filed	December 26, 2008	PCT Application Number:	PCT/US2008/014080
PCT Publication Date:	July 09, 2009	PCT Publication Number:	WO2009/085306

International Family Members for US Patent 8,377,474

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Australia	2008343787
Canada	2711014
China	101910113
European Patent Office	2234963