Injectable buprenorphine formulation
Inventors
Tiberg, Fredrik • Johnsson, Markus • Harwigsson, Ian
Assignees
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Publication Number
US-12029813-B2
Publication Date
2024-07-09
Expiration Date
Abstract
The present invention provides an injectable liquid formulation comprising: a) a lipid controlled-release matrix comprising at least 50% triacyl lipids; b) at least one oxygen containing organic solvent; c) at least 16% by weight of at least one active agent selected from buprenorphine and salts thereof, calculated as buprenorphine free base. The invention also provides a method for the treatment of pain, for opioid maintenance therapy or for the treatment of opioid dependence by detoxification and/or maintenance or for the treatment or prophylaxis of the symptoms of opioid withdrawal and/or cocaine withdrawal by injecting such a liquid composition.
Core Innovation
The invention relates to an injectable liquid formulation for subcutaneous administration that provides controlled-release delivery of buprenorphine or salts thereof. The formulation comprises a lipid controlled-release matrix and at least one oxygen containing organic solvent, and the active agent is present at a high drug loading level.
In particular, the lipid controlled-release matrix comprises at least 80% triglycerides, and the injectable liquid formulation comprises at least 16% by weight of the active agent, calculated as buprenorphine free base. The formulation is stated to form controlled-release upon injection.
The document describes sustained release of buprenorphine for therapeutic purposes including opioid maintenance therapy and treatment of opioid dependence by detoxification and/or maintenance, as well as symptoms of opioid withdrawal and/or cocaine withdrawal. It also reports plasma concentration control within a functional plasma concentration window over extended dosing intervals.
Claims Coverage
The document contains one independent claim directed to a treatment method using a defined injectable liquid formulation, with the independent claim covering a therapeutically effective dosing regimen and several formulation constraints. The main inventive features include the formulation architecture, the high triglyceride content, the oxygen-containing solvent requirement, the high buprenorphine loading expressed as buprenorphine free base, and a defined subcutaneous dosing interval.
Subcutaneous treatment with every-2-or-3-month administration
A method for the treatment of pain, for opioid maintenance therapy, for the treatment of opioid dependence by detoxification and/or maintenance, or for the treatment of the symptoms of opioid withdrawal and/or cocaine withdrawal, comprising subcutaneous administration to a human or non-human animal subject in need thereof a therapeutically effective amount of an injectable liquid formulation administered every 2 or 3 months.
Lipid controlled-release matrix with high triglyceride content
The injectable liquid formulation comprises a lipid controlled-release matrix comprising at least 80% triglycerides.
Oxygen-containing organic solvent in the injectable liquid formulation
The injectable liquid formulation comprises at least one oxygen containing organic solvent.
High buprenorphine loading expressed as buprenorphine free base
The injectable liquid formulation comprises 50-600 mg of at least one active agent selected from buprenorphine and salts thereof, calculated as buprenorphine free base, and the injectable liquid formulation comprises at least 16% by weight of the active agent.
Overall, the claim coverage is centered on subcutaneous administration every 2 or 3 months using an injectable liquid formulation defined by a lipid controlled-release matrix containing at least 80% triglycerides, inclusion of at least one oxygen containing organic solvent, and a high buprenorphine loading.
Stated Advantages
Maintaining buprenorphine above about 16 wt% is unexpectedly required for effective sustained release.
Provides plasma concentration control within a functional plasma concentration window over extended dosing intervals.
Documented Applications
Treatment of pain.
Opioid maintenance therapy.
Treatment of opioid dependence by detoxification and/or maintenance.
Treatment of the symptoms of opioid withdrawal and/or cocaine withdrawal.
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