Magnesium system and use thereof in the cosmetics industry

• US 8,529,950 B2
• Filed: 05/20/2009
• Issued: 09/10/2013
• Est. Priority Date: 05/20/2008
• Status: Active Grant

• Current Assignee: Fabienne Joanny
• Original Assignee: Fabienne Joanny
• Inventors: Joanny, Fabienne
• Primary Examiner(s): Fubara, Blessing
• Assistant Examiner(s): BERRIOS, JENNIFER A
• Application Number:
  US12/993,683
• Publication Number:
  US 20110097400A1
• Time in Patent Office: 1,574 Days
• Field of Search: 424/472, 424/682
• 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 2h 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 the form of a solid, progressive-release tablet for oral ingestion, said first magnesium source being formulated to supply Mg²⁺ ions to a body, the progressive-release tablet comprising a matrix having a protective coating that slows down or retards the dissolution of Mg in the stomach, said matrix being comprised of said first magnesium source (A), hydroxypropylmethylcellulose (B1), glyceryl behenate (B2), an inert filler (C1) acting as a diluent, and an inert filler (C2) acting as a lubricant, with a weight ratio of B1;

B2 being between 8.1;

1 and 9.6;

1, and exhibiting in vitro, after 2h in 0.1N HCl medium, a rate of dissolution (δ

) of the magnesium contained therein of between 20% and 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 by application to skin.

2. 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.

3. The system according to claim 1, wherein said matrix forms a core that comprises:

(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 9/2, 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.

4. The system according to claim 3, wherein said protective coating comprises

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

5. 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.

6. 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.

7. The system according to claim 1, wherein the tablet exhibits a magnesium dissolution rate (δ

), as determined by first treating in 900 ml of a 0.1N HCl medium at 40°

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

C. at pH 6.8 from T=2h to T=8h, relative to the total amount of magnesium administered, such that

at T=4h, δ

is less than or equal to 85%;

at T=6h, δ

is less than or equal to 98%; and

at T=8h, δ

is less than or equal to 100%.

8. The system according to claim 7, wherein the magnesium dissolution rate (δ

), as determined by the treatment in the HCl medium followed by the buffer, is such that

at T=2h, δ

is between 25-58%;

at T=4h, δ

is between 45-82%;

at T=6h, δ

is between 80-95%; and

at T=8h, δ

is between 95-99.9%.

9. The system according to claim 1, wherein the protective coating comprises an inner layer comprised of shellac and an outer layer comprised of a mixture of alkylcelluloses.

10. The system according to claim 9, wherein the mixture of alkylcelluloses comprises hydroxypropylmethylcellulose and hydroxypropylcellulose.

11. The system according to 1 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.

12. A skin care treatment method comprising:

orally administering at least once a day, to a patient in need thereof, a first magnesium source in the form of a solid, progressive-release tablet, said first magnesium source being formulated to supply Mg²⁺ions to the patient'"'"'s body, the tablet comprising a matrix having a protective coating that slows down or retards the dissolution of Mg in the stomach, said matrix being comprised of said first magnesium source (A), hydroxypropylmethylcellulose (B1), glyceryl behenate (B2), an inert filler (C1) acting as a diluent, and an inert filler (C2) acting as a lubricant, with a weight ratio of B1;

B2being between 8.1;

1 and 9.6;

1, and exhibiting in vitro, after 2h in 0.1N HCl medium, a rate of dissolution (δ

) of the magnesium contained therein of between 20% and 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.

13. The method according to claim 12, wherein the tablet exhibits a magnesium dissolution rate (δ

), as determined by first treating in 900 ml of a 0.1N HCl medium at 40°

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

C. at pH 6.8 from T=2h to T=8h, relative to the total amount of magnesium administered, such that;

at T=4h, δ

is between 40-85%;

at T=6h, δ

is between 60-98%; and

at T=8h, δ

is between 90-100%.

14. The method according to claim 12, 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.

15. The method according to claim 12, wherein said matrix forms a core that comprises:

(A) 90 to 110 parts by weight of magnesium originating from a first source selected from MgO, MgCl₂, hydrates of formula MgCl₂.n(H₂O), where n is an integral or fractional number having a value of 1 to 9/2, 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.

16. The method according to claim 15, wherein the first magnesium source in said tablet is MgCl₂.9/2(H₂O).

17. The method according to claim 15, wherein the magnesium dissolution rate (δ

) of the tablet, as determined by the treatment in the HCl medium followed by the buffer, is such that;

at T=2h, δ

is between 25-58%,

at T=4h, δ

is between 45-82%,

at T=6h, δ

is between 80-95%,

at T=8h, δ

is between 95-99.9%,.

18. The method according to claim 12, wherein said protective coating is a single layer coating.

19. The method according to claim 12, wherein said protective coating is a two-layer coating.

20. The method according to claim 12, wherein the protective coating comprises an inner layer comprised of shellac and an outer layer comprised of a mixture of alkylcelluloses.

21. The method according to claim 20, wherein the mixture of alkylcelluloses comprises hydroxypropylmethylcellulose and hydroxypropylcellulose.