SLOW RELEASE MAGNESIUM COMPOSITION AND USES THEREOF
The present invention provides compositions that contain magnesium and threonate, or a threonate precursor molecule, formulated for extended or modified release to provide physiological concentrations over a desired time period. The extended release or modified release form is particularly useful in providing Mg to a subject while avoiding adverse side effects such as diarrhea.
1 . An oral dosage form comprising magnesium (Mg) and threonate (T) in a controlled release formulation, wherein the magnesium of said controlled release formulation has an in vitro dissolution profile in a dissolution medium, and wherein said dissolution profile ranges between less than or equal to 35% in 1 hour, and greater than or equal to 70% in 4 to 12 hours as measured using a USP type II (paddle) dissolution system at 75 rpm, at a temperature of 37° C.
2 . The oral dosage form of claim 1 , wherein said magnesium and threonate in said oral dose form is encapsulated in a tablet.
3 . The oral dosage form of claim 1 , wherein at least a portion of said magnesium (Mg) and threonate (T) are complexed in a salt form of MgT 2 .
4 . The oral dosage form of claim 1 , wherein at least a portion of said magnesium (Mg) and threonate (T) are complexed in a salt form of MgT 2 present in an amount equal to at least about 20 mg of Mg by weight.
5 . The oral dosage form of claim 1 , wherein said oral dosage form comprises at least 10 mg of elemental magnesium.
6 . The oral dosage form of claim 1 , wherein said oral dosage form comprises at least 20 mg of elemental magnesium.
7 . The oral dosage form of claim 1 , wherein said magnesium (Mg) is present in an amount greater than about 1% by weight.
8 . The oral dosage form of claim 1 , wherein said magnesium (Mg) is present in an amount greater than about 5% by weight.
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12 . The oral dosage form of claim 1 further comprising one or more antioxidant selected from the group consisting of resveratrol, ellagic acid, quercetin, lipoic acid and vitamin C.
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14 . The oral dosage form of claim 1 , wherein said oral dose form further comprises magnesium and threonate in an immediate release formulation that releases at least 80% of the magnesium from said immediate release formulation within 1 hour as measured in a dissolution medium using a USP type II (paddle) dissolution system at 75 rpm, at a temperature of 37° C.
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23 . The oral dosage form of claim 1 , wherein upon administering said oral dosage form to a Sprague-Dawley rat at a dosage of equal to or less than 75 mg/kg/day yields an incidence of diarrhea of less than 20%.
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25 . The oral dosage form of claim 1 , wherein the magnesium of said controlled release formulation has a dissolution rate of magnesium of about 40-80% within about 6 to 10 hours.
26 . The oral dosage form of claim 23 , wherein said oral dosage form provides for an incidence of diarrhea of less than 50% when administered at a dosage of equal to or less than about 130 mg/kg/day.
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33 . The oral dosage form of claim 1 , wherein upon administering said oral dosage form to a subject at least about 50% of said administered magnesium is absorbed in said subject, or at least 30% of the magnesium administered to the subject is retained over a period of at least two days when said oral dosage form is administered at a dose of 20 mg/kg/day or higher.
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39 . A method of treating a condition related to magnesium deficiency comprising administering to a subject in need thereof an oral dosage form of claim 1 .
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