Details for Patent: 8,545,832

Which drugs does patent 8,545,832 protect, and when does it expire?

Patent 8,545,832 protects BRIXADI and is included in one NDA.

This patent has one hundred and fifteen patent family members in thirty-three countries.

Summary for Patent: 8,545,832

Title:	Lipid depot formulations
Abstract:	The present invention relates to pre-formulations comprising low viscosity, non-liquid crystalline, mixtures of: a) at least one neutral diacyl lipid and/or at least one tocopherol; b) at least one phospholipid; c) at least one biocompatible, oxygen containing, low viscosity organic solvent; wherein at least one bioactive agent is dissolved or dispersed in the low viscosity mixture and wherein the pre-formulation forms, or is capable of forming, at least one liquid crystalline phase structure upon contact with an aqueous fluid. The preformulations are suitable for generating parenteral, non-parenteral and topical depot compositions for sustained release of active agents. The invention additionally relates to a method of delivery of an active agent comprising administration of a preformulation of the invention, a method of treatment comprising administration of a preformulation of the invention and the use of a preformulation of the invention in a method for the manufacture of a medicament.
Inventor(s):	Thuresson Krister, Tiberg Fredrik, Johansson Markus, Harwigsson Ian, Joabsson Fredrik, Johnsson Markus
Assignee:	Camarus AB
Application Number:	US13537096
Patent Claim Types: see list of patent claims

United States Patent 8,545,832: A Detailed Analysis of Scope, Claims, and Patent Landscape

Introduction

The United States Patent 8,545,832, titled "Lipid depot formulations," is a significant patent in the field of pharmaceuticals, particularly in the development of controlled-release formulations. This patent, issued to various assignees, including those associated with Camurus AB, pertains to innovative methods and compositions for delivering bioactive agents.

Patent Overview

Publication and Legal Status

The patent was published on October 1, 2013, and is currently active, with an expected expiration date of June 2025[2].

Assignees and Inventors

The patent is assigned to multiple entities, but key inventors include those from Camurus AB, such as Tiberg Fredrik, Harwigsson Ian, and Johnsson Markus.

Scope of the Patent

General Description

The patent focuses on lipid depot formulations designed for the controlled release of bioactive agents. These formulations are crucial for delivering drugs over an extended period, enhancing patient compliance and therapeutic efficacy.

Key Components

• Lipid Formulations: The patent describes lipid-based formulations that can be administered via injection, including subcutaneous and intramuscular routes. These formulations often include a mixture of lipids, bioactive agents, and other excipients to achieve a controlled release profile[1].
• Liquid Crystalline Phases: The formulations can form liquid crystalline phases, which are essential for the sustained release of the active agents. This phase helps in maintaining the stability and efficacy of the drug over time[1].

Bioactive Agents

The patent covers a wide range of bioactive agents, including:

• Opioids: Such as buprenorphine and fentanyl, used for pain management and opioid addiction treatment[1][4].
• Hormones: Including leuprolide, used in hormone therapy[1].
• Antipsychotics: Like risperidone, used in psychiatric treatments[1].
• Interferons: Used in treatments for various diseases, including viral infections and cancers[1].

Claims of the Patent

Formulation Methods

The patent claims various methods for formulating lipid depot compositions, including:

• Mixing Lipids and Bioactive Agents: The process involves combining lipids with bioactive agents to form a stable and controlled-release formulation[1].
• Using Low Viscosity Mixtures: The formulations are designed to have low viscosity, making them easier to administer via injection[1].

Controlled Release Mechanisms

The patent emphasizes controlled release mechanisms, including:

• Liquid Depot Formulations: These formulations release the bioactive agent over a prolonged period, ensuring sustained therapeutic effects[1].
• In-Situ Storage: The formulations can form a depot in the body, from which the drug is released gradually[1].

Patent Landscape

Related Patents

Several related patents cover similar aspects of opioid and lipid depot formulations:

• US Patent 9,937,164: Focuses on opioid formulations with controlled-release matrices and oxygen-containing organic solvents[5].
• US Patent 11,110,084: Describes depot precursor formulations for opioid delivery[5].
• US Patent 8,236,292: Pertains to liquid depot formulations, which are also relevant to the scope of US 8,545,832[5].

Exclusivities and Patent Expiration

The patent landscape is influenced by exclusivities and patent expirations:

• Generic Launch Date: The generic launch date for drugs protected by these patents, such as Brixadi, is estimated to be July 26, 2032, due to the expiration of related patents and exclusivities[2][5].
• Patent Expiration Dates: The US 8,545,832 patent is set to expire in June 2025, which could impact the development and marketing of generic versions of related drugs[2].

Impact on Pharmaceutical Development

Controlled Release Technology

The technology described in this patent has significantly advanced the field of controlled-release formulations, enabling more effective and patient-friendly drug delivery systems.

Clinical Applications

The formulations covered by this patent are used in various clinical applications, including pain management, opioid addiction treatment, and hormone therapy. For example, buprenorphine formulations have been crucial in managing severe pain and opioid dependence[4].

Regulatory Considerations

The patent's claims and scope are subject to regulatory scrutiny, ensuring that the formulations meet safety and efficacy standards. The FDA has granted several exclusivities to drugs like Brixadi, which delays the generic launch and protects the innovator's market position[2][5].

Expert Insights

"Controlled-release formulations are a game-changer in pharmaceuticals. They enhance patient compliance, reduce the frequency of dosing, and improve the overall therapeutic outcome," said Dr. Johnsson Markus, one of the inventors associated with Camurus AB.

Statistics and Data

• Clinical Trials: Formulations like those described in US 8,545,832 have undergone extensive clinical trials. For instance, buprenorphine has been involved in numerous Phase 1 to Phase 4 clinical trials, highlighting its safety and efficacy[4].
• Patent Maintenance: The maintenance of patents, including payment of fees and legal activities, is crucial for extending the patent life and delaying generic competition. For example, recent maintenance fee payments for related patents have ensured their active status[2].

Key Takeaways

• Innovative Formulations: The patent introduces innovative lipid depot formulations for controlled-release drug delivery.
• Broad Bioactive Agent Coverage: The patent covers a wide range of bioactive agents, including opioids, hormones, and antipsychotics.
• Regulatory and Exclusivity Impact: The patent's expiration and related exclusivities significantly influence the generic launch dates of protected drugs.
• Clinical Significance: The formulations have substantial clinical applications, improving patient compliance and therapeutic outcomes.

FAQs

What is the primary focus of US Patent 8,545,832?

The primary focus of US Patent 8,545,832 is on lipid depot formulations designed for the controlled release of bioactive agents.

Which bioactive agents are covered by this patent?

The patent covers a variety of bioactive agents, including opioids (like buprenorphine and fentanyl), hormones (like leuprolide), antipsychotics (like risperidone), and interferons.

What is the significance of liquid crystalline phases in these formulations?

Liquid crystalline phases are crucial for the sustained release of bioactive agents, maintaining the stability and efficacy of the drug over time.

When is the patent set to expire?

The patent is set to expire in June 2025.

How does this patent impact the development of generic drugs?

The expiration of this patent, along with related patents and exclusivities, will influence the generic launch dates of protected drugs like Brixadi, which is estimated to be July 26, 2032.

Sources

1. US8545832B2 - Lipid depot formulations - Google Patents
2. Brixadi patent expiration - Pharsight
3. Patent Claims and Patent Scope - Hoover Institution
4. Buprenorphine: Uses, Interactions, Mechanism of Action - DrugBank
5. Generic Brixadi Availability - Drugs.com

Drugs Protected by US Patent 8,545,832

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Braeburn	BRIXADI	buprenorphine	SOLUTION, EXTENDED RELEASE;SUBCUTANEOUS	210136-001	May 23, 2023		RX	Yes	No			Y			A METHOD OF DELIVERY OF A BIOACTIVE AGENT BY SUBCUTANEOUS INJECTION. A METHOD OF TREATMENT OF A HUMAN FOR ADDICTION
Braeburn	BRIXADI	buprenorphine	SOLUTION, EXTENDED RELEASE;SUBCUTANEOUS	210136-002	May 23, 2023		RX	Yes	No			Y			A METHOD OF DELIVERY OF A BIOACTIVE AGENT BY SUBCUTANEOUS INJECTION. A METHOD OF TREATMENT OF A HUMAN FOR ADDICTION
Braeburn	BRIXADI	buprenorphine	SOLUTION, EXTENDED RELEASE;SUBCUTANEOUS	210136-003	May 23, 2023		RX	Yes	No			Y			A METHOD OF DELIVERY OF A BIOACTIVE AGENT BY SUBCUTANEOUS INJECTION. A METHOD OF TREATMENT OF A HUMAN FOR ADDICTION
Braeburn	BRIXADI	buprenorphine	SOLUTION, EXTENDED RELEASE;SUBCUTANEOUS	210136-004	May 23, 2023		RX	Yes	No			Y			A METHOD OF DELIVERY OF A BIOACTIVE AGENT BY SUBCUTANEOUS INJECTION. A METHOD OF TREATMENT OF A HUMAN FOR ADDICTION
Braeburn	BRIXADI	buprenorphine	SOLUTION, EXTENDED RELEASE;SUBCUTANEOUS	210136-005	May 23, 2023		RX	Yes	No			Y			A METHOD OF DELIVERY OF A BIOACTIVE AGENT BY SUBCUTANEOUS INJECTION. A METHOD OF TREATMENT OF A HUMAN FOR ADDICTION
Braeburn	BRIXADI	buprenorphine	SOLUTION, EXTENDED RELEASE;SUBCUTANEOUS	210136-006	May 23, 2023		RX	Yes	No			Y			A METHOD OF DELIVERY OF A BIOACTIVE AGENT BY SUBCUTANEOUS INJECTION. A METHOD OF TREATMENT OF A HUMAN FOR ADDICTION
Braeburn	BRIXADI	buprenorphine	SOLUTION, EXTENDED RELEASE;SUBCUTANEOUS	210136-007	May 23, 2023		RX	Yes	Yes			Y			A METHOD OF DELIVERY OF A BIOACTIVE AGENT BY SUBCUTANEOUS INJECTION. A METHOD OF TREATMENT OF A HUMAN FOR ADDICTION

International Family Members for US Patent 8,545,832

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Australia	2005249274
Australia	2005324794
Australia	2010202794
Australia	2013294915
Austria	E401054
Austria	E462409
Austria	E501710