US2007025933A1PendingUtilityA1

Photoprotector and/or photoimmunoprotector compositions of the skin and their uses

Assignee: CANTABRIA IND FARMACEUTICA SAPriority: Apr 1, 2004Filed: Sep 29, 2006Published: Feb 1, 2007
Est. expiryApr 1, 2024(expired)· nominal 20-yr term from priority
A61K 8/60A61K 8/365A61K 8/37A61K 31/7024A61Q 17/04A61K 8/35A61K 31/216A61K 8/602A61K 31/315A61K 8/36A61K 8/368A61K 8/678
45
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Claims

Abstract

The composition comprises of a component A selected from a hydroxylated derivative of benzoic acid or of cinamic acid, their esters, amides or salts, a glycoside of a hexose, and their mixtures; and a component B selected from quinic acid, shikimic acid, their alkaline metal or alkaline earth salts, their methyl esters, and mixtures of the same. This composition is suitable for protecting the skin against ultraviolet radiation coming from the sun or artificial sources, such as those used in phototherapy units and in sun tanning rooms. For application in the field of dermatology and nutrition, and, in particular, in the photoprotection of the skin and mucosa, photo-ageing and photocarcinogenesis, including protection of the immune system associated with the skin.

Claims

exact text as granted — not AI-modified
1 . A composition which comprises of a component A and a component B, where; 
 (A) aforementioned component A is selected from a group formed by: 
 (A.1) a component A.1 of formula (I)  
                     
 where  
 R 1  is H or CH 3    
 X represents 
 OH:  
 OR 2 , where R 2  is alkyl C 1 -C 2  or the residue of a hydroxylated carboxylic acid of formula  
                     
 NH 2 ;  
 m is 0 or 1; y  
 q is 0 or 1: or  
 
 a salt of the same;  
   (A.2) a component A.2 of formula (II)                        where 
 R 3  is H or CH 3 ;  
 Y represents 
 OH;  
 OR 2 , where R 2  has the previously mentioned significances; or  
 NH 2 ;  
 
 n is 0 or 1; y  
 r is 0 or 1; or  
   a salt of the same;      (A.3) a component A.3 of formula (III)                        where R represents 
 (I) a residue of formula (I)  
                     
 where R 1 , X, m and q have the previously mentioned significances; or  
 (II) a residue of formula (II)  
                     
 where R , Y, n and r have the previously mentioned significances;  
   (A.4) a component A.4 of formula (IV)                            where R has the previously indicated significance;    (A.5) a component A.5 of formula (V)                        where R has the previously indicated significance; and      (A.6) mixtures of the same; and    (B) the aforementioned component B is selected from a group made up of quinic acid, shikimic acid, their alkaline metal or alkaline earth salts, their methyl esters and mixtures of the same.    
   
   
       2 . A composition according to  claim 1 , in which the aforementioned components A and B are to be present in a ratio of component A: component B of 1-10:1 by weight, preferably between 1.6-9:1 by weight, and more preferably between 2-9:1 by weight.  
   
   
       3 . A composition according to  claim 1 , where in the aforementioned component A.1, X is OR 2  where R 2  is a C 1 -C 2  alkyl.  
   
   
       4 . A composition according to  claim 1 , where in the aforementioned component A.1, X is NH 2 .  
   
   
       5 . A composition according to  claim 1 , where in the aforementioned component A.1 is in the form of a alkaline metal or alkaline earth salt.  
   
   
       6 . A composition according to  claim 1 , where in the aforementioned component A.2, Y is OR 2  where R 2  is a C 1 -C 2  alkyl.  
   
   
       7 . A composition according to  claim 1 , where in the aforementioned component A.2, Y is NH 2 .  
   
   
       8 . A composition according to  claim 1 , where in the aforementioned component A.2 is in the form of a alkaline metal or alkaline earth salt  
   
   
       9 . A composition according to  claim 1 , where in the aforementioned component A.2 is the trans isomer.  
   
   
       10 . A composition according to  claim 1 , where in the aforementioned component A.3 is glucose glycoside.  
   
   
       11 . A composition according to  claim 1 , where in the aforementioned component A.4 is fructose glycoside.  
   
   
       12 . A composition according to  claim 1 , where in the aforementioned component A.5 is a rhamnose glycoside.  
   
   
       13 . A composition according to  claim 1 , in which the aforementioned component A is composed of one or more components (A.1), or of one or more of components (A.2), or of one or more components (A.3), or of one or more components (A.4), or of one or more components (A.5), or of any mixture of 2 or more of the aforementioned components (A.1) to (A.5), where each one of the components (A.1) to (A.5) can be composed, in their part, by one or more components of the same group.  
   
   
       14 . A composition according to  claim 13 , in which the aforementioned component A comprises (i) at least two different components (A.1), and at least, two different components (A.2).  
   
   
       15 . Composition according to  claim 14 , in which the molar component (A.1):component (A.2) ratio is between 0.5 and 2.  
   
   
       16 . Composition according to  claim 1 , where the aforementioned component B is selected between quinic acid, an alkaline or alkaline earth metal salt of quinic acid a methyl ester of quinic acid, shikimic acid, an alkaline or alkaline earth metal salt of shikimic acid, a methyl ester of shikimic acid and their mixtures.  
   
   
       17 . Composition according to  claim 1 , which comprises, besides, one or more components selected from the group formed by component C, component D, component E, component F and their mixtures, in which: 
 aforementioned component C is selected from the group made up of:    (C.1) a component C.1 of the formula (VI)                          where 
 R 4 , R 5 , R 6 , R 7 , R 8 , R 9 , R 10 , and R 11 , equal or different, independent of each other, represent H, OH, OR 3 , —CH═CH—COY, or —COY where R 3  is H or CH 3 , or a CH═CH—COY group, where Y represents OH, OR 2  where R 2  is C 1 -C 2  alkyl or the residue of a hydroxylated carboxylic acid of the formula;  
                     
 NH 2 ; or  
 a salt of the same;  
 with the condition that (i) at least two of R 4 , R 5 , R 6 , R 7 , R 8 , R 9 , R 10 , or R 11  are, simultaneously, OH, (ii) one of R 4 , R 5 , R 6 , R 7 , R 8 , R 9 , R 10 , or R 11  is OR 3  , (iii) the maximum number of hydroxyl groups present is 3, and (iv) one of R 4 , R5, R 6 , R 7 , R 8 , R 9 , R 10 , or R 11  is —CH═CH—COY or  
 —COY;  
   (C.2) a component C.2 of formula (VII)                          where 
 R 6  represents H or an OH, OR 3 , or —CH═CH—COY group where R 3  and Y have the significances previously mentioned, or a salt of the same;  
   (C.3) a component C.3 of formula (VIII)                          where 
 R 12  and R 13 , equal or different, independently of each other, represent H or  
 CH 3 ;  
 Z represents —CH 2 —, O, S or NH;  
 o is 0 or 1; and  
 p is 0 or 1, and  
   (C.4) their mixtures;    said component D is selected between one or more free monosaccharides;    aforementioned component E is selected from the group made up of an acid of the Krebs cycle, an alkaline metal or alkaline earth salt of an acid of the Krebs cycle, a mono-, di-, or trimethyl ester of an acid of the Krebs cycle, aldaric acid, an alkaline metal or alkaline earth salt of aldaric acid, a lactonised derivative of aldaric acid, aldonic acid, an alkaline metal or alkaline earth salt of aldonic acid, a lactonised derivative of aldonic acid, or mixtures of these compounds; and    aforementioned component F is selected from a group made up of a water soluble vitamin, a water soluble derivative of a lipid soluble vitamin, and their mixtures.    
   
   
       18 . Composition according to  claim 17 , which comprises of the aforementioned component C in a concentration of between 0.1% and 10% by weight in respect to the total composition, preferably between 0.5% and 5%.  
   
   
       19 . Composition according to  claim 18 , in which the aforementioned component C.1 is the trans isomer.  
   
   
       20 . Composition according to  claim 18 , in which the aforementioned component C.2 is the trans isomer.  
   
   
       21 . Composition according to  claim 18 , in which the aforementioned component C.3 is the trans-trans isomer.  
   
   
       22 . Composition according to  claim 18 , in which the aforementioned component C is composed of one or more components (C.1); or one or more components (C.2); or one or more components (C.3); or mixtures of one or more components (C.1) and (C.2); or mixtures of one or more components (C.1) and (C.3); or mixtures of one or more components (C.2) and (C.3); or mixtures of one or more components (C.1), (C.2) and (C.3).  
   
   
       23 . Composition according to  claim 18 , in which the aforementioned component C comprises of at least, a component (C.3).  
   
   
       24 . Composition according to  claim 17 , which comprises of the aforementioned component D in a concentration comprising of between 35% and 90% by weight in respect to the total weight of the composition, preferably between 45% and 65%.  
   
   
       25 . Composition according to  claim 24 , in which the aforementioned component D is selected from glucose, rhamnose and fructose, in any of their possible configurations.  
   
   
       26 . Composition according to  claim 17 , in which the aforementioned component E is in a concentration comprising of between 5% and 30% by weight in respect of the total of the composition, preferably between 10% and 20%.  
   
   
       27 . Composition according to  claim 26 , in which the aforementioned component E comprises of one or more acids of the Krebs cycle, preferably, citric, fumaric or malic acid, and/or one or more of their alkaline metal or alkaline earth salts, and/or one or more of their mono-, di-, or tri-methyl esters, and/or one or more aldaric acids, and/or one or more aldonic acids, and/or one or more of the alkaline metal or alkaline earth salts of the aforementioned aldaric and/or aldonic acids, and/or one or more aldaric and/or aldonic acids in lactone form.  
   
   
       28 . Composition according to  claim 17 , in which the aforementioned component F is in a concentration comprising of between 4% and 20% by weight in respect of the total of the composition, preferably between 8% and 12%.  
   
   
       29 . Composition according to  claim 28 , in which the aforementioned component F comprises of ascorbic acid or a water soluble derivative of tocopherol, or its mixtures.  
   
   
       30 . Composition according to  claim 1 , consisting of 65-90% by weight of component A and 35-10% by weight of component B, preferably, between 74-86% by weight of component A and between 26-14% by weight of component B, in which the ratio of component A: component B is 1-10:1 by weight.  
   
   
       31 . Composition according to  claim 1 , consisting of a ternary mixture made up of components A and B and a third component selected from component C, component D, component E and component F.  
   
   
       32 . Composition according to  claim 1 , consisting of a quaternary mixture made up of components A and B and two other components selected from components C, D, E and F.  
   
   
       33 . Composition according to  claim 32 , consisting of components A, B, D and E.  
   
   
       34 . Composition according to  claim 33 , consisting of: 
 5-35% by weight of component A+component B, where the ratio of component A: component B is 1-10:1 by weight;    35-90% by weight of component D, and    5-30% by weight of component E.    
   
   
       35 . Composition according to  claim 1 , consisting of a mixture of 5 components made up of components A and B and three components selected from components C, D, E and F.  
   
   
       36 . Composition according to  claim 35 , consisting of components A, B, D, E and F.  
   
   
       37 . Composition according to  claim 36 , consisting of; 
 5-35% by weight of component A+component B, where the ratio of component A: component B is 1-10:1 by weight;    30-85% by weight of component D,    5-20% by weight of component E; and    5-15% by weight of component F.    
   
   
       38 . Composition according to  claim 1 , consisting of components A, B, C, D, E and F.  
   
   
       39 . Composition according to  claim 38 , consisting of; 
 5-30% by weight of component A+component B, where the ratio of component A: component B is I - 10:1 by weight;    1-5% by weight of component C;    30-84% by weight of component D,    5-20% by weight of component E; and    5-15% by weight of component F.    
   
   
       40 . Composition according to  claim 1 , in solid phase.  
   
   
       41 . Composition according to  claim 1 , in liquid phase.  
   
   
       42 . Composition according to  claim 41 , in the form of an aqueous solution with a pH of between 4.8 and 6.8, preferably, between 5 and 6.5.  
   
   
       43 . A pharmaceutical composition which consists of a therapeutically effective quantity of a composition according to  claim 1  together with, at least, one pharmaceutically acceptable excipient.  
   
   
       44 . A pharmaceutical composition according to  claim 43 , in a pharmaceutical form suitable for its oral or topical administration.  
   
   
       45 . Use of a composition according to  claim 1 , in the preparation of a drug or pharmaceutical composition to protect the skin from ultraviolet radiation.  
   
   
       46 . Use of a composition according to  claim 1 , in the preparation of a drug or pharmaceutical composition to prevent or minimise the harmful effects produced by UV radiation on the skin.  
   
   
       47 . A cosmetic composition which comprises of a composition according to  claim 1 , together with, a cosmetically acceptable excipient.  
   
   
       48 . A food supplement which comprises of a composition according to  claim 1 , together with, one or more acceptable vehicles.  
   
   
       49 . A food supplement according to  claim 48 , in which the aforementioned supplement comprises of amino acids, plant extracts, antioxidant molecules, prebiotic lactic bacteria, yeasts for food use or mixtures of the same.  
   
   
       50 . A functional food which consists of a composition according to  claim 1 , together with one or more acceptable vehicles.  
   
   
       51 . A functional food according to  claim 50 , of which the food basis of the aforementioned food comprises of milk, cheese, yoghourt, fermented products based on milk, ice creams, products based on fermented cereals, biscuits, fruit juices, cold drinks or plant infusions.  
   
   
       52 . A method to protect the skin of an individual from UV radiation which comprises of administering to the aforementioned individual a therapeutically effective quantity of a composition according to  claim 1.

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