Acamprosate formulations, methods of using the same, and combinations comprising the same
Inventors
Fogel, Barry S. • Kerns, William D. • Fong, Kei-Lai
Assignees
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Publication Number
US-10166207-B2
Publication Date
2019-01-01
Expiration Date
Abstract
Embodiments disclosed herein generally relate to acamprosate formulations, methods of use of the formulations, to methods of using the formulations optionally in combination with at least one other medication, and to combination products and compositions comprising acamprosate and at least one other medication, such as neuroleptic (antipsychotic) and/or antidepressant drugs.
Core Innovation
The invention reformulates an acamprosate sustained-release pill for oral administration to a human subject in a fasted state. The pill comprises about 20-95% by weight acamprosate, or a pharmaceutically acceptable salt thereof, and about 1-30% by weight of a carbomer homopolymer type B.
In the disclosed embodiments, an acamprosate pill is administered in a fasted state with an acamprosate dose within the range of 400 mg-1500 mg. The formulation is characterized by release and pharmacokinetic parameters, including an in vitro release profile and a fasted-state Tmax range, and sustained-release behavior based on diffusion release kinetics.
The document also describes reformulation aimed at improving fed-fasted equivalence and GI tolerability relative to an enteric-coated Campral® product. It reports substantially similar AUC and Cmax in fed versus fasting states and reduced GI side effects, alongside altered GI retention/release location in fed versus fasted states using gamma scintigraphy.
Claims Coverage
The independent claims cover two method approaches for oral administration of an acamprosate sustained-release pill to a human subject in a fasted state. Each approach includes quantitative formulation constraints, with additional fasted-state pharmacokinetic and in vitro release refinements in dependent claims.
Fasted-state acamprosate pill with carbomer homopolymer type B
Orally administering to a human subject in a fasted state a pill comprising about 20-95% by weight acamprosate, or a pharmaceutically acceptable salt thereof, and about 1-30% by weight of a carbomer homopolymer type B.
Fasted-state acamprosate dose range
Orally administering to a human subject in a fasted state an acamprosate pill comprising acamprosate in a dose within the range of 400 mg-1500 mg.
Overall, the claim set focuses on administering an acamprosate sustained-release pill in a fasted state, where the pill includes specified amounts of acamprosate and a carbomer homopolymer type B, and where fasted-state performance is constrained by parameters such as Tmax and, in dependent claims, in vitro release thresholds and specific pharmaceutically acceptable salt forms.
Stated Advantages
Fed-fasted equivalence with substantially similar AUC and Cmax in fed versus fasting states.
Reduced GI side effects, including diarrhea, despite higher per-pill doses, relative to an enteric-coated Campral® product.
Sustained-release behavior based on diffusion release kinetics.
Enables once- or twice-daily dosing and reduced pill burden.
Documented Applications
Oral administration of an acamprosate sustained-release pill to a human subject in a fasted state.
Use of the acamprosate pill in combination with neuroleptics/antidepressants as fixed-dose or co-administered kits.
Assessment of GI retention/release location in fed versus fasted states using gamma scintigraphy.
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