Details for Patent: 8,101,209

Which drugs does patent 8,101,209 protect, and when does it expire?

Patent 8,101,209 protects COREG CR and is included in one NDA.

Protection for COREG CR has been extended six months for pediatric studies, as indicated by the *PED designation in the table below.

This patent has twenty-four patent family members in fourteen countries.

Summary for Patent: 8,101,209

Title:	Microparticulate oral galenical form for the delayed and controlled release of pharmaceutical active principles
Abstract:	The invention relates to a microparticulate system for the delayed and controlled release of active principles (AP) whose absorption window in vivo is essentially limited to the upper parts of the gastrointestinal tract, this system being intended for oral administration. The object of the invention is to provide a system ensuring that the AP is released with certainty by means of a dual mechanism of "time-dependent" and "pH-dependent" release. To achieve this object, the invention proposes a multimicrocapsular oral galenical form which is designed so as to guarantee therapeutic efficacy, and in which the release of the AP is governed by a dual release triggering mechanism that is "time-triggering" and "pH-triggering". This system comprises of microcapsules (200 to 600 .mu.m) comprising a core of AP coated with a film (maximum 40% by weight) comprising a hydrophilic polymer A (Eudragit.RTM. L) and a hydrophobic compound B (vegetable wax, melting point=40-90.degree. C.), B/A being between 0.2 and 1.5. These microcapsules have a dissolution behavior in vitro such that, at a constant pH of 1.4, a latency phase of between 1 and 5 hours is observed, followed by a release of the AP, and such that the change from pH 1.4 to pH 6.8 results in a release of the AP without a latency period in vitro.
Inventor(s):	Legrand; Valerie (Lyons, FR), Castan; Catherine (Orlienas, FR), Meyrueix; Remi (Lyons, FR), Soula; Gerard (Meyzieu, FR)
Assignee:	Flamel Technologies (FR)
Application Number:	10/826,690
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 8,101,209
Patent Claim Types: see list of patent claims	Formulation; Compound; Dosage form; Delivery;

United States Patent 8,101,209: A Detailed Analysis of Scope and Claims

Introduction

The United States Patent 8,101,209, assigned to Flamel Technologies, pertains to a microparticulate oral galenical form designed for the delayed and controlled release of pharmaceutical active principles. This patent is crucial in the field of pharmaceuticals, particularly in the development of extended-release formulations.

Background

Pharmaceutical patents, such as US 8,101,209, play a significant role in protecting intellectual property and encouraging innovation in the pharmaceutical industry. These patents can cover a wide range of inventions, including chemical compounds, methods of use, and methods of manufacture or administration[4].

Patent Overview

Title and Assignee

The patent titled "Microparticulate oral galenical form for the delayed and controlled release of pharmaceutical active principles" is assigned to Flamel Technologies. This company has been at the forefront of developing innovative drug delivery systems.

Publication and Prior Art

The patent was published on January 24, 2012, with a prior art date of August 26, 2004. It builds upon earlier research and technologies related to controlled release formulations[2].

Scope of the Patent

Claims

The patent includes several claims that define the scope of the invention. Here are some key aspects:

• Microparticulate System: The patent describes a microparticulate system composed of microcapsules or microspheres that encapsulate the active pharmaceutical ingredient (API). This system is designed to release the API in a delayed and controlled manner[1].
• Coating Films: The microparticles are coated with at least one film, which can include hydrophilic polymers. These coatings can have different triggering mechanisms for drug release, such as pH-dependent or time-dependent release[2].
• Active Principles: The patent specifies that the microparticulate system can be used for a variety of active principles, emphasizing those whose absorption window in vivo needs to be managed carefully[1].

Independent and Dependent Claims

The patent includes both independent and dependent claims. Independent claims define the broad scope of the invention, while dependent claims narrow down the scope by adding specific details or limitations. For example, one independent claim might describe the general composition of the microparticulate system, while a dependent claim might specify the type of polymer used in the coating film[3].

Key Components and Materials

Microcapsules and Microspheres

The microparticulate system consists of microcapsules or microspheres that encapsulate the API. These microcapsules are designed to protect the API and control its release over a specified period[1].

Coating Materials

The coating materials include hydrophilic polymers and other substances like talc, lanolin, and cellulose. These materials are chosen for their ability to control the release of the API based on specific triggers such as pH or time[1].

Triggering Mechanisms

The patent describes different triggering mechanisms for the release of the API. For instance, the coating films can be designed to release the drug at a specific pH, which is particularly useful for drugs that need to be released in the intestinal tract rather than the stomach[2].

Patent Landscape

Related Patents and Applications

Other patents and applications in the same field include those related to extended-release compositions of carvedilol phosphate. For example, U.S. Patent Application Publication No. 2012/0245212 describes a controlled release formulation comprising immediate and slow release subunits of carvedilol[2].

Regulatory and Legal Aspects

Pharmaceutical patents, including US 8,101,209, are subject to various regulatory and legal frameworks. These include the Hatch-Waxman Act and the Biologics Price Competition and Innovation Act, which govern the approval and marketing of generic and biosimilar drugs. The patent holder has exclusive rights to make, use, sell, and import the invention for approximately 20 years from the filing date of the patent application[4].

Impact on the Pharmaceutical Industry

Innovation and Competition

The patent encourages innovation by providing exclusive rights to the inventor, allowing them to recoup their investment in research and development. However, it also delays the entry of generic or biosimilar versions of the drug into the market, which can affect competition and drug pricing[4].

Extended Release Formulations

The technology described in US 8,101,209 has significant implications for the development of extended-release formulations. These formulations can improve patient compliance by reducing the frequency of dosing and can also enhance the therapeutic efficacy of the drug by maintaining a steady drug concentration over a longer period[2].

Challenges and Controversies

Patent Scope and Quality

There is ongoing debate about the scope and quality of pharmaceutical patents. Some argue that broader patents can diminish innovation by increasing licensing and litigation costs. Metrics such as independent claim length and count can be used to measure patent scope and its impact on innovation[3].

Regulatory Exclusivities

In addition to patent protection, pharmaceutical products may also be granted regulatory exclusivities, which can further delay the market entry of generic or biosimilar drugs. These exclusivities can range from six months to 12 years, depending on the type of pharmaceutical product and its approval status[4].

Conclusion

The United States Patent 8,101,209 is a significant contribution to the field of pharmaceuticals, particularly in the area of controlled release formulations. It highlights the importance of intellectual property protection in driving innovation and the complex regulatory landscape that governs the pharmaceutical industry.

Key Takeaways

• Microparticulate System: The patent describes a microparticulate system for delayed and controlled release of pharmaceutical active principles.
• Coating Films: The microparticles are coated with films that can include hydrophilic polymers with different triggering mechanisms.
• Regulatory Framework: The patent is subject to regulatory frameworks such as the Hatch-Waxman Act and Biologics Price Competition and Innovation Act.
• Impact on Industry: The patent encourages innovation but can delay the entry of generic drugs into the market.
• Challenges: There are ongoing debates about patent scope and quality, and regulatory exclusivities can further impact market competition.

FAQs

What is the main focus of United States Patent 8,101,209?

The main focus of US 8,101,209 is the development of a microparticulate oral galenical form for the delayed and controlled release of pharmaceutical active principles.

What materials are used in the coating films of the microparticulate system?

The coating films can include hydrophilic polymers, talc, lanolin, and cellulose.

How does the patent impact the pharmaceutical industry?

The patent encourages innovation by providing exclusive rights but can delay the market entry of generic or biosimilar drugs, affecting competition and drug pricing.

What regulatory frameworks govern this patent?

The patent is governed by frameworks such as the Hatch-Waxman Act and the Biologics Price Competition and Innovation Act.

How long does the exclusive right granted by this patent last?

The exclusive right granted by the patent lasts approximately 20 years from the filing date of the patent application.

Sources

1. US8101209B2 - Microparticulate oral galenical form for the delayed and controlled release of pharmaceutical active principles - Google Patents
2. Extended release compositions of carvedilol phosphate - Justia Patents
3. Patent Claims and Patent Scope - SSRN
4. Drug Prices: The Role of Patents and Regulatory Exclusivities - Congressional Research Service

Drugs Protected by US Patent 8,101,209

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Waylis Therap	COREG CR	carvedilol phosphate	CAPSULE, EXTENDED RELEASE;ORAL	022012-001	Oct 20, 2006	AB	RX	Yes	No					Y
Waylis Therap	COREG CR	carvedilol phosphate	CAPSULE, EXTENDED RELEASE;ORAL	022012-002	Oct 20, 2006	AB	RX	Yes	No					Y
Waylis Therap	COREG CR	carvedilol phosphate	CAPSULE, EXTENDED RELEASE;ORAL	022012-003	Oct 20, 2006	AB	RX	Yes	Yes					Y
Waylis Therap	COREG CR	carvedilol phosphate	CAPSULE, EXTENDED RELEASE;ORAL	022012-004	Oct 20, 2006	AB	RX	Yes	No					Y

Foreign Priority and PCT Information for Patent: 8,101,209

Foriegn Application Priority Data
Foreign Country	Foreign Patent Number	Foreign Patent Date
France	01 12999	Oct 09, 2001

International Family Members for US Patent 8,101,209

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Australia	2002362712
Brazil	0213175
Brazil	PI0213175
Canada	2463134
Canada	2563689
China	100341493