Composition comprising a mixture of active principles, and method of preparation

Abstract

Active principle-based coated particle, in which both the core and the coating contain active principle, includes a core which contains a first active principle while the coating contains a second active principle, which is different in nature.

1 . An active principle-based coated particle having a size between 50 μm and 2 mm and comprising a core and a coating, wherein the core contains from 60 to 99% by weight of a first active principle, and the coating contains from 60 to 99% by weight of a second active principle that is different in nature from the first active principle, and wherein the rest up to 100% by weight of each of the core and coating consists of
 a) at least one binding agent; or 
 b) at least one binding agent and an antistatic agent. 
 
     
     
         2 . The coated particle as claimed in  claim 1 , wherein the first active principle and the second active principle have a different concentration in the coated particle, and the first active principle in the core has a higher dose amount than the second active principle in the coating. 
     
     
         3 . The coated particle as claimed in  claim 2 , wherein a dose ratio between the first active principle and the second active principle is equal to or greater than 5. 
     
     
         4 . The coated particle as claimed in  claim 1 , wherein the coating contains from 80 to 99% by weight of the second active principle. 
     
     
         5 . The coated particle as claimed in  claim 1 , wherein the core contains from 80 to 99% by weight of the first active principle. 
     
     
         6 . The coated particle as claimed in  claim 1 , wherein the rest up to 100% of the coating and the core consists exclusively of a binding agent, which may be identical or different. 
     
     
         7 . The particle as claimed in  claim 1 , wherein the at least one binding agent is chosen from the group consisting of cellulosic polymers, acrylic polymers, povidones, copovidones, polyvinyl alcohols, alginic acid, sodium alginate, starch, pregelatinized starch, sucroses and derivatives thereof, guar gum and polyethylene glycols, alone or as a mixture. 
     
     
         8 . The coated particle as claimed in  claim 1 , wherein the rest up to 100% of the core and/or the coating consists of at least one binding agent and an antistatic agent, the antistatic agent being present in proportions ranging respectively up to 10% by weight relative to the weight of the core and up to 10% by weight relative to the weight of the coating. 
     
     
         9 . The coated particle as claimed in  claim 1 , which comprises, in addition to the coating, an additional functional layer, composition of which is chosen as a function of desired characteristics of taste masking and/or of release of active principle. 
     
     
         10 . The particle as claimed in  claim 9 , wherein the additional functional layer comprises at least one coating polymer chosen from the group consisting of cellulosic polymers and acrylic polymers, alone or as a mixture. 
     
     
         11 . The particle as claimed in  claim 1 , which comprises, between the core and the coating, an intermediate layer based on a polymer chosen from the group consisting of cellulosic polymers, acrylic polymers, povidones, copovidones, polyvinyl alcohols, alginic acid, sodium alginate, starch, pregelatinized starch, sucroses and derivatives thereof, guar gum and polyethylene glycols, alone or as a mixture. 
     
     
         12 . A pharmaceutical or cosmetic composition comprising the coated particle of  claim 1 . 
     
     
         13 . The composition as claimed in  claim 12 , which is in the form of a multiparticulate tablet which is orodispersible or dispersible. 
     
     
         14 . A method for producing an active principle-based coated particle having a size between 50 μm and 2 mm and comprising a core and a coating, each of which contains an active principle, wherein the core contains from 60 to 99% by weight of a first active principle, and the coating contains from 60 to 99% by weight of a second active principle that is different in nature from the first active principle, wherein the rest up to 100% by weight of each of the core and coating consists of
 a) at least one binding agent; or 
 b) at least one binding agent and an antistatic agent, 
 
       wherein the binding agent and antistatic agent in the core and coating may be the same or different, said method comprising the following steps:
 (i) preparing the core comprising the first active principle, 
 (ii) coating the core thus obtained by spraying a solution or suspension comprising either:
 A) from 60 to 99% by weight of a second active principle and at least one binding agent; or 
 B) from 60 to 99% by weight of a second active principle, at least one binding agent, and an antistatic agent, and 
 
 (iii) drying. 
 
     
     
         15 . The method as claimed in  claim 14 , wherein the step of preparing the core comprises granulation of the first active principle in the form of a powder, using a binding agent in the form of an aqueous or organic solution or a solvent mixture, and then drying. 
     
     
         16 . The method as claimed in  claim 14 , wherein the step of preparing the core comprises granulometric selection of microcrystals of between 50 μm and 400 μm in size, constituting the first active principle. 
     
     
         17 . The method as claimed in  claim 14 , further comprising an additional step of coating with an additional functional layer, the composition of which is chosen as a function of the desired characteristics of taste masking and/or of release of an active principle. 
     
     
         18 . The method as claimed in  claim 14 , wherein the at least one binding agent is chosen from the group consisting of cellulosic polymers, acrylic polymers, povidones, copovidones, polyvinyl alcohols, alginic acid, sodium alginate, starch, pregelatinized starch, sucroses and derivatives thereof, guar gum and polyethylene glycols, alone or as a mixture. 
     
     
         19 . The coated particle as claimed in  claim 3 , wherein a dose ratio between the first active principle and the second active principle is equal to or greater than 10. 
     
     
         20 . The coated particle as claimed in  claim 4 , wherein the core contains from 80 to 99% by weight of the first active principle.