Composition for oral use based on s-adenosylmethionine and a process for their preparation

Abstract

The present invention relates to solid dietary and/or nutraceutic pharmaceutical compositions for oral use based on SAMe, or salts thereof, in combination with inositol and/or derivatives thereof and to a process for their preparation. The present invention relates to a method of stabilising a solid composition for oral use based on SAMe or salts thereof, making use of inositol and/or derivatives thereof with the addition of magnesium oxide. The present invention also relates to the use of SAMe, or salts thereof, in combination with inositol and/or derivatives thereof with the possible further addition of melatonine, St. John's Wort and/or lemon balm for the treatment of depressive states and/or panic syndromes.

1 . Dietary and/or nutraceutic oral pharmaceutical composition comprising S-adenosylmethionine para-toluenesulphonate in combination with inositol and/or derivatives thereof and pharmaceutically acceptable excipients. 
     
     
         2 . (canceled) 
     
     
         3 . Composition according to  claim 1 , in which said inositol and/or derivatives is inositol on its own, inositol-1-phosphate or a mixture thereof. 
     
     
         4 . Composition according to  claim 1 , in which the S-adenosylmethionine para-toluenesulphonate is contained in an amount which varies from about 10 to about 90% by weight, relative to the weight of the composition. 
     
     
         5 . Composition according to  claim 4 , in which the S-adenosylmethionine para-toluenesulphonate is contained in an amount which varies from about 10 to 50% by weight, relative to the weight of the composition. 
     
     
         6 . Composition according to  claim 1 , in which the inositol and/or derivatives thereof is contained in an amount which varies from about 50 to about 90% by weight, relative to the weight of the composition. 
     
     
         7 . Composition according to  claim 6 , in which the inositol and/or derivatives thereof is contained in an amount which varies from about 30 to about 85% by weight, relative to the weight of the composition. 
     
     
         8 . Composition according to  claim 1 , comprising at least one other active component, preferably selected from melatonine, St. John's Wort dry extract and lemon balm dry extract or mixtures thereof. 
     
     
         9 . Composition according to  claim 1 , in which at least one of the pharmaceutically acceptable excipients is magnesium oxide. 
     
     
         10 . Composition according to  claim 1 , in the form of a tablet, capsule, granule or powder. 
     
     
         11 . Composition according to  claim 10 , in the form of a tablet, wherein the tablet is a simple, coated, film-coated, layered and/or gastroresistant tablet. 
     
     
         12 . Composition according to  claim 10 , in the form of a tablet, wherein the tablet is a gastroresistant tablet. 
     
     
         13 . Process for the preparation of a tablet according to  claim 1 , which comprises the steps of:
 a) mixing the SAMe or salts thereof with pharmaceutically acceptable excipients;   b) pre-compression, followed by granulation, of the mixture obtained in step a);   c) coating the granulated product obtained in step b) with hydrogenated fatty acids;   d) mixing, pre-compression and granulation of the inositol and/or derivatives thereof with pharmaceutically acceptable excipients;   e) coating of the granulated products obtained in step d) with hydrogenated fatty acids;   f) mixing the granulated products obtained in steps c) and e) with pharmaceutically acceptable excipients;   g) compressing the mixture obtained in step f) with the optional addition of sweeteners and aromas;   h) optionally coating the tablets obtained in step g) with hydrogenated fatty acids; and   i) optionally film-coating in the aqueous phase the tablets obtained in step h).   
     
     
         14 . (canceled) 
     
     
         15 . Process according to  claim 13 , in which said inositol and/or derivatives thereof is inositol on its own, inositol-1-phosphate or a mixture thereof. 
     
     
         16 . Process according to  claim 13 , in which the relative humidity is below about 25% and the temperature is maintained between about 20° C. and 30° C., in particular at about 25° C. 
     
     
         17 . Process according to  claim 13 , in which in step d) it is possible to add, to the mixture, at least one other active component, preferably selected from melatonine, St. John's Wort dry extract and lemon balm dry extract and/or mixtures thereof. 
     
     
         18 . Process according to  claim 13 , in which the coating carried out in step h) is effected with hydrogenated fatty acids in an amount of between 0.5 and 2.5% by weight, relative to the weight of the composition. 
     
     
         19 . Process according to  claim 13 , in which the film-coating in the aqueous phase carried out in step i) is effected with a varnish, preferably selected from rubber varnish and/or salts thereof (Shellac™), methacrylic acid, cellulose acetophthalates, titanium dioxide, talcum, triethyl citrate, PVP K30, riboflavin 6-phosphate, hydroxypropylcellulose, hydroxypropylmethyl-cellulose and/or mixtures thereof. 
     
     
         20 . Process according to  claim 19 , in which the varnish is contained in an amount ranging from about 2.0 to about 8.0% by weight, relative to the composition. 
     
     
         21 . Process according to  claim 13 , in which in step i) it is possible to optionally add lemon balm and/or St. John's Wort oil in an amount which varies from about 0.01 to about 0.2% by weight, relative to the total composition. 
     
     
         22 . Dietary and/or nutraceutic pharmaceutical compositions obtainable by means of the process according to any one of  claims 13 ,  15 - 21 . 
     
     
         23 . Method for the treatment of depressive states and panic syndromes which comprises the administration of SAMe, or salts thereof, in combination with inositol and/or derivatives thereof to a patient in such a need. 
     
     
         24 . (canceled) 
     
     
         25 . Method according to  claim 23 , in which said inositol and/or derivatives thereof is inositol on its own, inositol-1-phosphate or a mixture thereof. 
     
     
         26 . Method of stabilising a solid dietary and/or nutraceutic pharmaceutical composition based on SAMe or salts thereof, which comprises using inositol and/or derivatives thereof. 
     
     
         27 . Method according to  claim 26 , in which the SAMe or salts thereof is contained in an amount of between about 10 and about 90% by weight, calculated relative to the weight of the composition. 
     
     
         28 . Method according to  claim 27 , in which the SAMe or salts thereof is contained in an amount of between about 10 and about 50% by weight, calculated relative to the weight of the composition. 
     
     
         29 . Method according to  claim 26 , in which the inositol and/or derivatives thereof is contained in an amount which varies from about 50 to about 90% by weight, relative to the weight of the composition. 
     
     
         30 . Method according to  claim 29 , in which the inositol and/or derivatives thereof is contained in an amount which varies from about 50 to about 85% by weight, relative to the weight of the composition. 
     
     
         31 . Process according to  claim 13 , wherein said SAMe is S-adenosylmethionine para-toluenesulphonate. 
     
     
         32 . Method according to  claim 23 , wherein said SAMe is S-adenosylmethionine para-toluenesulphonate.