Acamprosate formulations, methods of using the same, and combinations comprising the same

Inventors

Fogel, Barry S. • Kerns, William D. • Fong, Kei-Lai

Assignees

Synchroneuron Inc

Abstract

Embodiments disclosed herein generally relate to acamprosate formulations, methods of use of the formulations, to methods of using the formulations in combination with at least one other medication, and to combination products and compositions comprising the formulations and at least one other medication, such as neuroleptic (antipsychotic) and/or antidepressant drugs.

Core Innovation

The invention relates to acamprosate gastric-retentive controlled-release formulations, including tablet compositions that are designed to alter pharmacokinetics. The disclosed gastric-retentive approach is intended to influence exposure metrics such as Cmax, time above a therapeutic threshold, and AUC, to support efficacy with altered drug exposure relationships. The disclosed formulations are described in the context of treating neuropsychiatric disorders, including tardive dyskinesia.

The problem addressed is that conventional dosing can involve reduced tolerability and/or insufficient exposure for efficacy, and that improved delivery can improve tolerability and compliance while maintaining therapeutic effect. The disclosure emphasizes that the gastric-retentive controlled-release formulation can achieve prolonged time above a therapeutic threshold while lowering Cmax, enabling efficacy despite reduced total AUC. This is described as supporting improved tolerability and reduced gastrointestinal side effects.

The disclosure further provides combination products that include gastric-retentive acamprosate with additional active agents such as neuroleptics, SSRIs/SNRIs, and metoclopramide. Additional benefits are described in terms of reduced risk of tardive dyskinesia and metabolic disturbances versus neuroleptics alone. The disclosed systems also include an optional fed mode inducing agent approach, including alpha-lipoic acid, to induce fed-state gastric retention without materially reducing acamprosate bioavailability.

Claims Coverage

The independent claim recites a tablet with acamprosate distributed within a specific polymer matrix, including a specific polymer amount, defining a core formulation architecture. The dependent claims add main refinements involving tablet physical and administration attributes and optional inclusion of additional active agents, with the neuroleptic further constrained to specified named selections in additional dependent claims.

Overall, the claim set centers on an acamprosate-containing tablet where acamprosate is distributed in a polymer matrix comprising or consisting of carbomer homopolymer type B at a specified amount, with further limitations describing swallowability and spheroid shape and optional co-inclusion of neuroleptics or metoclopramide, where neuroleptics are restricted to specified named options including molindone.

Stated Advantages

Documented Applications