Stable oral solutions for combined API
Inventors
Cohen, Daniel • Chumakov, Ilya • Nabirochkin, Serguei • Bertrand, Viviane
Assignees
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Publication Number
US-10849851-B2
Publication Date
2020-12-01
Expiration Date
Abstract
The present invention relates to a homogeneous, stable, and palatable pharmaceutical solution comprising baclofen, sorbitol and naltrexone.
Core Innovation
The invention describes a stable, homogeneous oral pharmaceutical solution that comprises baclofen, sorbitol, and naltrexone as active ingredients in an acetate or citrate buffer, where the solution has a pH of between about 4 and about 7. The formulation addresses the lack of a single stable solution across wide API concentration differences present in conventional approaches and distributes the active ingredients in a buffered aqueous environment to support chemical stability.
The document states that acetate/citrate buffers maintain chemical stability and minimize microbial contamination, including paraben-free embodiments. The solution is described as meeting regulatory and ICH stability compliance over extended storage time, with comparative discussion showing different stability performance versus phosphate buffer and differences versus capsule or semi-solid dosage forms.
Additional embodiments describe preferred pH ranges and specific buffered compositions, together with optional excipients such as preservatives and flavoring agents. The document describes compositions including isoamyl acetate as a flavoring agent and combinations of sodium methyl paraben and sodium propyl paraben as preservatives in an acetate buffer, with improved palatability while maintaining chemical and microbial stability in the buffered oral solution.
Claims Coverage
The independent claims cover two inventive features centered on an oral pharmaceutical solution of baclofen, sorbitol, and naltrexone with an acetate or citrate buffer and pH 4 to 7, plus a second independent claim specifying a particular excipient set and defined concentrations in an acetate buffer.
Buffered solution of baclofen, sorbitol, and naltrexone at pH 4 to 7
A pharmaceutical composition comprising, in the form of a solution, baclofen or a pharmaceutically acceptable salt thereof, sorbitol or a pharmaceutically acceptable salt thereof, and naltrexone or a pharmaceutically acceptable salt thereof as active ingredients, and an acetate or citrate buffer, or a combination thereof, wherein the solution has a pH of between about 4 and about 7.
Specific acetate-buffered solution with defined concentrations and selected excipients
A pharmaceutical composition comprising, in the form of a solution, sorbitol, naltrexone, baclofen, isoamyl acetate, sodium methyl paraben, sodium propyl paraben, and an acetate buffer, wherein the solution has a pH of between 4 and 7.
Across the independent claims, the core claim coverage is directed to an oral pharmaceutical solution combining baclofen, sorbitol, and naltrexone with an acetate or citrate buffer at pH 4 to 7; a second independent claim further specifies isoamyl acetate and sodium methyl/paropyl parabens in an acetate buffer.
Stated Advantages
Maintains chemical stability in the buffered solution.
Minimizes microbial contamination, including paraben-free embodiments.
Provides stability performance compared to phosphate buffer and capsule/semi-solid alternatives.
Supports regulatory and ICH stability compliance over extended storage.
Improves palatability, including use of isoamyl acetate.
Documented Applications
Treating Charcot-Marie-Tooth disease type 1A (CMT1A) in a human by administering the composition.
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