Magnesium threonate compositions and uses thereof
Inventors
Liu, Guosong • Mao, Fei • WEINGER, Jason Gregory
Assignees
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Publication Number
US-11717501-B2
Publication Date
2023-08-08
Expiration Date
Abstract
Provided is a dosage form comprising magnesium threonate having enhanced efficacy. Also provided is a pharmacokinetic profile of magnesium threonate having enhanced efficacy. The dosage forms and pharmacokinetic profile of magnesium threonate are used to treat a variety of diseases, disorders, syndromes and/or conditions.
Core Innovation
The invention provides a dosage form comprising magnesium threonate and a controlled release carrier. At least a portion of magnesium (Mg) and threonate (T) of the magnesium threonate is present in a salt form of MgT2, and the magnesium threonate is present in an amount between about 200 to 6000 mg.
The controlled release carrier is included to produce a targeted in vivo plasma profile and a fluctuation index that is less than about 170%. The document further describes in vivo plasma exposure and shape parameters for threonic acid, including mean Cavg targets, fluctuation-related metrics, skewness constraints, and mean T_max constraints.
The invention includes formulation approaches for dosage forms such as fast, sustained, or controlled tablets, with examples of excipients and dissolution profiles. Human pharmacokinetic crossover data are described, including measures such as AUC0-24, Cmax, Tmax, fluctuation index, and skewness, and cognition/mood outcomes are described as correlating with improved efficacy where the fluctuation index is lower and dosing is based on LBM.
Claims Coverage
The document includes one independent claim. It focuses on a magnesium threonate dosage form with a MgT2 salt form and a controlled release carrier that produces a constrained in vivo plasma profile with a fluctuation index below about 170%.
MgT2 salt-form magnesium threonate dosage form
A dosage form comprising magnesium threonate where at least a portion of magnesium (Mg) and threonate (T) is present in a salt form of MgT2.
200 to 6000 mg magnesium threonate amount
The magnesium threonate is present in an amount between about 200 to 6000 mg.
Controlled release carrier producing low fluctuation index in vivo plasma profile
The dosage form includes a controlled release carrier in an amount sufficient to provide an in vivo plasma profile that exhibits a fluctuation index that is less than about 170%.
In vivo exposure and fluctuation constraints for controlled release dosing
The dosage form provides an in vivo plasma profile with a mean AUC0-24 of at least about 50 μg×h/mL and a mean fluctuation value (Cmax−Cmin) meeting specified ranges or an upper bound, including less than about 10 μg/mL in one refinement.
Plasma profile shape control using skewness constraint
The dosage form includes a controlled release carrier in an amount sufficient to produce an in vivo plasma profile with skewness less than about 0.2.
Timing constraint via mean T_max
The dosage form includes a controlled release carrier in an amount sufficient to produce an in vivo plasma profile with a mean T_max of at least about 4.5 hours.
Controlled release carrier excipient selection including carnauba wax
The dosage form includes one or more excipients that include carnauba wax.
Overall, the claim set centers on magnesium threonate in a MgT2 salt form combined with a controlled release carrier. The carrier amount is selected to achieve a reduced in vivo fluctuation index below about 170% and, in refinements, additional in vivo plasma exposure and shape constraints such as mean AUC0-24, mean fluctuation value, skewness, and mean T_max, with example excipient limitation including carnauba wax.
Stated Advantages
Enhanced efficacy associated with improved mood/cognition outcomes correlated with reduced peak/trough plasma variability.
Reduced in vivo plasma profile fluctuation, including fluctuation index less than about 170%.
Controlled/sustained release kinetics that reduce peak/trough variability.
Documented Applications
Treating disease states using magnesium threonate dosage forms with controlled release carrier configurations designed to achieve targeted in vivo plasma profiles and mood/cognition outcomes.
Human pharmacokinetic and cognition/mood evaluation, including correlation of improved efficacy with lower fluctuation index and LBM-based dosing.
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