MAGNESIUM SYSTEM AND USE THEREOF IN THE COSMETICS INDUSTRY

• US 20110097400A1
• Filed: 03/20/2009
• Published: 04/28/2011
• Est. Priority Date: 05/20/2008
• Status: Active Grant

• Current Assignee: Fabienne Joanny
• Original Assignee: Fabienne Joanny
• Inventors: Joanny, Fabienne
• Granted Patent: US 8,529,950 B2
• Time in Patent Office: Days
• US Class Current: 424/472
• CPC Class Codes: A61K 33/06 Aluminium, calcium or magnesium; Compounds thereof , e.g. clay
• CPC Class Codes: A61K 36/02 Algae
• CPC Class Codes: A61K 36/15 Pinaceae (Pine family), e.g. pine or cedar
• CPC Class Codes: A61K 36/42 Cucurbitaceae (Cucumber family)
• CPC Class Codes: A61K 36/53 Lamiaceae or Labiatae (Mint family), e.g. thyme, rosemary or lavender
• CPC Class Codes: A61K 36/73 Rosaceae (Rose family), e.g. strawberry, chokeberry, blackberry, pear or firethorn
• CPC Class Codes: A61K 36/84 Valerianaceae (Valerian family), e.g. valerian
• CPC Class Codes: A61K 36/899 Poaceae or Gramineae (Grass family), e.g. bamboo, corn or sugar cane
• CPC Class Codes: A61K 9/06 Ointments; Bases therefor; Other semi-solid forms, e.g. creams, sticks, gels composition of ointments, creams or gels A61K47/00
• CPC Class Codes: A61K 9/2009 Inorganic compounds
• CPC Class Codes: A61K 9/2013 Organic compounds, e.g. phospholipids, fats
• CPC Class Codes: A61K 9/2018 Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
• CPC Class Codes: A61K 9/205 Polysaccharides, e.g. alginate, gums; Cyclodextrin
• CPC Class Codes: A61K 9/2054 Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
• CPC Class Codes: A61K 9/286 Polysaccharides, e.g. gums; Cyclodextrin
• CPC Class Codes: A61K 9/2886 having two or more different drug-free coatings; Tablets of the type inert core-drug layer-inactive layer of the type active core-drug layer-inactive layer A61K9/209
• CPC Class Codes: A61K 9/7015 Drug-containing film-forming compositions, e.g. spray-on
• CPC Class Codes: A61P 17/00 Drugs for dermatological disorders

Abstract

A magnesium-based system suitable for use in skincare comprises (a) a first magnesium source in the form of a progressive-release oral tablet exhibiting in vitro, after 2 h in 0.1N HCl medium, a rate of dissolution (δ) of the magnesium contained therein of less than or equal to 60% by weight relative to the total weight of the Mg provided by the first magnesium source, and (b) a second magnesium source in a topical preparation. A method for treating skin for stress, fatigue or skin barrier deficiencies, as well as for stratum corneum hydration, includes orally and topically administering magnesium sources (a) and (b), respectively.

Claims

1. A magnesium-based system suitable for use in skincare, comprising:

(a) a first magnesium source in an oral preparation, in the form of a progressive-release tablet, said first magnesium source being formulated to supply Mg²⁺ ions to a body, the tablet form exhibiting in vitro, after 2 h in 0.1N HCl medium, a rate of dissolution (δ

) of the magnesium contained therein of less than or equal to 60% by weight relative to the total weight of the Mg provided by said first magnesium source, and

(b) a second magnesium source in a topical preparation formulated to supply Mg²⁺ ions to skin.

2. The system according to claim 1, wherein said rate of dissolution (δ

) is between 20% and 60%, in vitro, after 2 h in 0.1N HCl medium.

3. The system according to claim 1, wherein said progressive-release tablet is selected from the group consisting of:

(I) a single-layer tablet containing the entirety of the first magnesium source, and

(II) a two-layer tablet comprising

(a) a first layer which is enteric, or which is housed in an enteric shell, said first layer containing 80% to 40% of the magnesium provided by the first magnesium source, and

(b) a second layer, which is hydrophilic, which surrounds said first layer, which dissolves in the stomach, and which contains 20% to 60% of the magnesium provided by the first magnesium source.

4. The system according to claim 3, wherein the progressive-release single-layer tablet comprises a matrix having a non-enteric protective coating that slows down or retards the dissolution of Mg in the stomach, said matrix being comprised of said first magnesium source (A), a hydrophilic retardant (B1), a hydrophobic retardant (B2), an inert filler (C1) acting as a diluent, and an inert filler (C2) acting as a lubricant.

5. The system according to claim 4, wherein said tablet comprises, for oral administration of magnesium, with progressive release,

a matrix forming a core comprising, in a mixture:

(A) 90 to 110 parts by weight of magnesium originating from a source selected from MgO, MgCl₂, hydrates of the formula MgCl₂.n(H₂O), where n is a whole or fractional number having a value of 1 to 6, and mixtures thereof,

(B1) 180 to 190 parts by weight of hydroxypropylmethylcellulose,

(B2) 19.8 to 22.2 parts by weight of glyceryl behenate,

(C1) 10 to 12 parts by weight of lactose, and

(C2) 10 to 12 parts by weight of colloidal silica; and

a protective coating disposed around the matrix that slows down the release of magnesium in the stomach and that is not enteric.

6. The system according to claim 5, wherein said protective coating comprises

(D) 15 to 75 parts of a substance selected from shellac, cellulose ethers and mixtures thereof.

7. The system according to claim 1, wherein the second magnesium source is a physiologically-acceptable derivative of magnesium selected from the group consisting of

(α

) magnesium oxide, MgO,

(β

) salts of Mg with inorganic acids,

(γ

) salts of Mg with organic acids,

(δ

) hydrates of said inorganic and organic salts, and

(ε

) mixtures thereof.

8. The system according to claim 1, wherein the first magnesium source is selected from the group consisting of MgO, MgCl₂, hydrates MgCl₂.n(H₂O) where n is a whole or fractional number having a value of 1 to 9/2, marine magnesium, and a salt of Mg with at least one of aspartic acid, glutamic acid, asparagine, lysine, pidolic acid and orotic acid.

9. The system according to claim 1, wherein the oral preparation exhibits an Mg dissolution rate (δ

), which is determined by first treating in a 0.1N HCl medium (900 ml;

40°

C.) from T=0 to T=2 h, and then by treating in a buffer (900 ml, at 40°

C.) at pH 6.8 from T=2 h to T=8 h, relative to the Mg administered, such that

at T=2 h, δ

is less than or equal to 60%;

at T=4 h, δ

is less than or equal to 85%;

at T=6 h, δ

is less than or equal to 98%; and

at T=8 h, δ

is less than or equal to 100%.

13. The system according to claim 9, wherein the oral preparation exhibits an Mg dissolution rate (δ

), relative to the Mg administered, such that

at T=2 h, δ

is between 25-58%;

at T=4 h, δ

is between 45-82%;

at T=6 h, δ

is between 80-95%; and

at T=8 h, δ

is between 95-99.9%.

14. The system according to claim 13, wherein the oral preparation is a progressive-release single-layer tablet comprising a matrix having a non-enteric protective coating that slows down or retards the dissolution of Mg in the stomach, said matrix being comprised of an admixture of said first magnesium source (A), a hydrophilic retardant (B1), a hydrophobic retardant (B2), an inert filler (C1) acting as a diluent, and an inert filler (C2) acting as a lubricant.

15. The system according to claim 14, wherein the protective coating comprises an inner layer comprised of shellac and an outer layer comprised of a mixture of alkylcelluloses.

16. The system according to claim 15, wherein the mixture of alkylcelluloses comprises hydroxypropylmethylcellulose and hydroxypropylcellulose.

17. The system according to claim 14, wherein the topical preparation is selected from the group consisting of cream, gel, lotion, emulsion, aqueous solution, aqueous-alcoholic solution and atomizable composition, and contains 0.5% to 4% by weight of Mg relative to the total weight of the topical preparation.

10-12. -12. (canceled)

18. A method comprising:

orally administering at least once a day, to a patient in need thereof, a first magnesium source in the form of a progressive-release tablet, said source being formulated to supply Mg²⁺ ions to the patient'"'"'s body, the tablet exhibiting in vitro, after 2 h in 0.1N HCl medium, a rate of dissolution (δ

) of the magnesium contained therein of less than or equal to 60% by weight relative to the total weight of the Mg provided by the first magnesium source, and

topically administering at least once a day, to the patient in need thereof, a second magnesium source formulated to supply Mg²⁺ ions to the patient'"'"'s skin.

19. The method according to claim 18, wherein, by determination in vitro in accordance with a dissolution system comprising first treating said composition in a 0.1N HCl medium from T=0 to T=2 h, and then treating it in a buffer at pH 6.8 from T=2 h to T=8 h, the progressive-release tablet exhibits an Mg dissolution rate (δ

), relative to the Mg administered, such that;

at T=2 h, δ

is between 25-60%;

at T=4 h, δ

is between 45-85%;

at T=6 h, δ

is between 80-98%; and

at T=8 h, δ

is between 95-100%.

20. The method according to claim 19, wherein the progressive-release tablet comprises a matrix having a non-enteric protective coating that slows down or retards the dissolution of Mg in the stomach, said matrix being comprised of said first magnesium source, a hydrophilic retardant, a hydrophobic retardant, an inert filler acting as a diluent, and an inert filler acting as a lubricant.

21. The method according to claim 20, wherein the protective coating comprises an inner layer comprised of shellac and an outer layer comprised of a mixture of alkylcelluloses.

22. The method according to claim 21, wherein the mixture of alkylcelluloses comprises hydroxypropylmethylcellulose and hydroxypropylcellulose.

23. The method according to claim 22, wherein the topical preparation is selected from the group consisting of cream, gel, lotion, emulsion, aqueous solution, aqueous-alcoholic solution and atomizable composition, and contains 0.5% to 4% by weight of Mg relative to the total weight of the topical preparation.