Title:  Compounds containing biologically active silicon, which are under solid form

United States Patent:  6,197,986

Assignee:  Exsymol S.A.M. (Monaco, FR)

Filed:  March 24, 1998

Foreign Application Priority Data:  Mar 24, 1997[FR] (97 03792)

Organo silicon compound having the following general formula (I): R₄ --Si (OR₁) (OR₂) (R₃) (I) where R₁ and R₂ each one independently represent an atom of hydrogen or an alkyl group, R₃ represents an hydrogen atom, an hydroxyl group, an amine group, an alkyl group, an alkoxy or a carboxylate group, and at least one of the OR₁, OR₂ or R₃ groups represents an hydroxyl group, R₄ represents an alkyl group substituted or not by a functional group such as, notably, an alkyl phosphate group or an alkyl phosphonate group, or any other group for which the R₄ --Si bond is not hydrolyzable, and the compound: is in solid form, and/or is possibly associated with at least one stabilizer, and/or is possibly associated with at least one dispersant.

SUMMARY OF THE INVENTION

The organo silicon compound according to the invention has the following general formula (I):

R₄ --Si (OR₁) (OR₂) (R₃) (I) 

wherein

R₁ and R₂ each one independently represent an atom of hydrogen or an alkyl group, 

R₃ represents an hydrogen atom, an hydroxyl group, an amine group, an alkyl group, an alkoxy or a carboxylate group, 

and at least one of the OR₁, OR₂ or R₃ groups represents an hydroxyl group, 

R₄ represents an alkyl group substituted or not by a functional group such as, notably, an alkyl phosphate group or an alkyl phosphonate group, or any other group for which the R₄ --Si bond is not hydrolyzable, and the said compound:

is under solid form,

and/or is possibly associated with at least one stabilizer,

and/or is possibly associated with at least one dispersant.

Preferably, the compound according to the invention is a compound of formula (I) wherein R₄ represents a diethylphosphatoethyl group and/or OR₁, OR₂ and R₃ groups represent each an hydroxyl group.

According to an embodiment of the invention, the stabilizer is a carboxylic acid, an amino acid or a derived amino acid, a peptide or a protein, an alcohol or a polyol, a polysaccharide, and/or their salts.

Preferably, the carboxylic acid and/or its salt is aspartic acid, glutamic acid, lactic acid, salicylic acid, theophylline acetic acid, carboxylic pyrrolidinone acid and/or their salts.

Preferably, the amino acid and/or its salt is arginine, serine, threonine, hydroxyproline, acetylmethionine, acetyl tyrosine and/or their salts.

Preferably, the peptide is a polypeptide derived from elastin proteins, spirulina, collagen, or vegetal proteins, e.g. oat or wheat proteins.

Advantageously, this polypeptide is hydrolized elastin proteins, hydrolysed spirulina, hydrolysed collagen, or hydrolysed vegetal proteins, e.g. oat or wheat proteins.

Preferably, the protein is an elastin protein, spirulina protein, collagen protein, or a vegetal protein, e.g. oat or wheat protein.

Advantageously, the polyol is lactose.

Preferably, the polysaccharide is a glycosaminoglycanne, a mucopolysaccharide such as particularly hyaluronic acid, pectin or alginic acid.

According to another embodiment of the invention, the dispersant is a polyamiole, a carbohydrate, a polysaccharide, a polyoxethylene such as polyethylene glycol or a non water soluble (or weakly water soluble) fatty compound e.g. a triglyceride.

Another goal of the invention is to propose a pharmaceutical or a cosmetic composition including such a compound, in association with any suitable excipient, and being administered orally, in order to be used in ambulatory medication which does not require the realization of previous medical treatment.

Claim 1 of 11 Claims

What is claimed is:

1. An organosilicon compound having the following formula (I):

R₄ --Si (OR₁) (OR₂) (R₃) (I) 

wherein

R₁ and R₂ each independently represent an atom of hydrogen or an alkyl group,

R₃ represents an hydrogen atom, an hydroxyl group, an amine group, an alkyl group, an alkoxy or a carboxylate group,

and at least one of the OR₁, OR₂ or R₃ groups represents an hydroxyl group,

R₄ represents an alkyl group substituted by a phosphate or phosphonate group,

and said compound is a solid.

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