Synergistic medicinal compositions for treating dysfunctional D-serine signaling
Inventors
SAMANT, Rajaram • Tongra, Rajendra Prasad
Assignees
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Publication Number
US-11376277-B2
Publication Date
2022-07-05
Expiration Date
Abstract
The invention disclosed herein relates to novel synergistic medicinal compositions for treating dysfunctional D-serine (DSR) signaling. Particularly the invention provides potent synergistic medicinal composition comprising combination of N-acetyl taurinate salt of divalent metal (M2+AT) as serine racemase enzyme (SR) activator/stimulator and benzoic acid ester salt of monovalent or divalent metals (M+/2+Bz) as d-amino acid oxidase enzyme (DAAO) inhibitor, which are present in weight ratio of 1:0.001 to 1:1.5 along with pharmaceutically acceptable excipients. Further the present synergistic medicinal composition is useful for treating certain neuropsychiatric disorders, neurological disorders and metabolic disorders.
Core Innovation
The invention provides a synergistic medicinal composition for dysfunctional D-serine signaling. The composition comprises magnesium acetyl taurate and sodium benzoate as therapeutically active, medicinal ingredients, together with pharmaceutically acceptable excipients.
The synergy is defined by a specific weight ratio of magnesium acetyl taurate to sodium benzoate of 1:0.001 to 1:1.5. Magnesium acetyl taurate is characterized as a serine racemase activator/stimulator and sodium benzoate as a D-amino acid oxidase inhibitor.
The composition is proposed to be effective for treating dysfunctional D-serine signaling, including amelioration of DSR-mediated NMDAR signaling and reduction of neurotoxicity and oxidative stress, including reduction of H2O2 and ammonia. The described objectives and indications include neuropsychiatric disorders, neurological disorders, and metabolic disorders, including schizophrenia/psychosis and other neuropsychiatric disorders.
The description additionally reports animal pharmacokinetic data indicating increased plasma and brain D-serine exposure for the combination of magnesium acetyl taurate and sodium benzoate compared with individual components, and it references a comparative antipsychotic.
Claims Coverage
The independent claim covers a synergistic medicinal composition containing magnesium acetyl taurate and sodium benzoate at a defined weight ratio (1:0.001 to 1:1.5) that is effective for treating dysfunctional D-serine signaling.
Synergistic medicinal composition for dysfunctional D-serine signaling
A synergistic medicinal composition comprising magnesium acetyl taurate and sodium benzoate in a weight ratio of 1:0.001 to 1:1.5, together with pharmaceutically acceptable excipients, wherein the composition is effective for treating dysfunctional D-serine signaling.
Magnesium acetyl taurate weight fraction range
The synergistic medicinal composition wherein magnesium acetyl taurate is present in a range of 20% to 98% by weight of the total composition.
Sodium benzoate weight fraction range
The synergistic medicinal composition wherein sodium benzoate is present in a range of 1% to 50% by weight of the total composition.
Pharmaceutically acceptable excipients selected with defined ranges
The synergistic medicinal composition wherein pharmaceutically acceptable excipients are selected from diluent, binder, lubricant, glidant, additive, surfactant, stabilizer, and plasticizer, each present within specified by-weight ranges of the total composition.
Oral unit dose range
The synergistic medicinal composition formulated for oral administration with an effective unit dose range of 10 mg to 1000 mg.
Overall, the claims focus on a synergistic medicinal composition of magnesium acetyl taurate and sodium benzoate with a specified weight ratio, further constrained by by-weight ranges of each active, excipient selection categories with defined by-weight ranges, and an oral effective unit dose range.
Stated Advantages
Amelioration of DSR-mediated NMDAR signaling.
Reduction of neurotoxicity and oxidative stress.
Reduction of H2O2.
Reduction of ammonia.
Increased plasma and brain D-serine exposure for the combination compared with individual components.
Documented Applications
Treating dysfunctional D-serine signaling.
Ameliorating DSR-mediated NMDAR signaling and reducing neurotoxicity/oxidative stress in neuropsychiatric disorders, including schizophrenia/psychosis and other neuropsychiatric disorders.
Neuropsychiatric, neurological, and metabolic disorder indications are described, including schizophrenia/psychosis and other neuropsychiatric disorders.
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