Taste masked pharmaceutical particles

Abstract

Taste masked particles and chewable tablets made therefrom are disclosed. The taste masked particles comprise a core containing an active ingredient and a polymeric coating covering said core, said coating comprising a mixture of a) an enteric polymer; and b) an insoluble film forming polymer, the surface of said particle being free of active ingredient. The chewable tablets provide immediate release of the active ingredient.

1 . A taste masked particle comprising a core containing an active ingredient and a continuous polymeric coating covering said core, said coating comprising a mixture of a) an enteric polymer selected from the group consisting of hydroxypropyl methylcellulose phthalate, hydroxypropyl methylcellulose acetate succinate, cellulose acetate phthalate, polyvinylacetate phthalate, and mixtures thereof; and b) a water insoluble film forming polymer selected from the group consisting of cellulose acetate, ethylcellulose, and mixtures thereof, wherein the active ingredient is a nonsteroidal anti-inflammatory drug and wherein the weight ratio of enteric polymer to water insoluble film forming polymer in the coating is in the range of about 55:45 to about 80:20.  
   
   
       2 . The particle of  claim 1 , wherein the surface of said particle is substantially free of active ingredient.  
   
   
       3 . The particle of  claim 1 , wherein the coating is substantially free of plasticizer.  
   
   
       4 . The particle of  claim 1 , wherein the active ingredient is a nonsteroidal anti-inflammatory drug selected from the group consisting of ibuprofen, ketoprofen, flurbiprofen, naproxen, diclofenac, rofecoxib, celecoxib, aspirin, pharmaceutically acceptable salts and metabolites thereof, and mixtures thereof.  
   
   
       5 . (canceled)  
   
   
       6 . (canceled)  
   
   
       7 . The particle of  claim 1  further comprising a non-enteric, water soluble polymer.  
   
   
       8 . The particle of  claim 1  further comprising a surfactant.  
   
   
       9 . (canceled)  
   
   
       10 . (canceled)  
   
   
       11 . A chewable tablet comprising taste masked particles, each particle comprising a core containing an active ingredient and a continuous polymeric coating covering said core, said coating comprising a mixture of a) an enteric polymer selected from the group consisting of hydroxypropyl methylcellulose phthalate, hydroxypropyl methylcellulose acetate succinate, cellulose acetate phthalate, polyvinylacetate phthalate, and mixtures thereof; and b) a water insoluble film forming polymer selected from the group consisting of cellulose acetate, ethylcellulose, and mixtures thereof, wherein the active ingredient is a nonsteroidal anti-inflammatory drug and wherein the weight ratio of enteric polymer to water insoluble film forming polymer in the coating is in the range of about 55:45 to about 80:20.  
   
   
       12 . The chewable tablet of  claim 11 , wherein the surfaces of the particles are substantially free of active ingredient.  
   
   
       13 . The chewable tablet of  claim 11 , wherein the coating is substantially free of plasticizer.  
   
   
       14 . The chewable tablet of  claim 11 , wherein the active ingredient is a nonsteroidal anti-inflammatory drug selected from the group consisting of ibuprofen, ketoprofen, flurbiprofen, naproxen, diclofenac, rofecoxib, celecoxib, aspirin, pharmaceutically acceptable salts and metabolites thereof, and mixtures thereof.  
   
   
       15 . (canceled)  
   
   
       16 . (canceled)  
   
   
       17 . The chewable tablet of  claim 11 , wherein said coating further comprises an ingredient selected from the group consisting of non-enteric, water soluble polymers and surfactants.  
   
   
       18 . (canceled)  
   
   
       19 . A method of taste masking particles comprising an active ingredient, which comprises applying a continuous polymeric coating over said particles, said coating comprising a mixture of a) an enteric polymer selected from the group consisting of hydroxypropyl methylcellulose phthalate, hydroxypropyl methylcellulose acetate succinate, cellulose acetate phthalate, polyvinylacetate phthalate, and mixtures thereof; and b) an insoluble film forming polymer selected from the group consisting of cellulose acetate ethylcellulose, and mixtures thereof, wherein the active ingredient is a nonsteroidal anti-inflammatory drug and wherein the weight ratio of enteric polymer to water insoluble film forming polymer in the coating is in the range of about 55:45 to about 80:20.  
   
   
       20 . The method of  claim 19 , wherein the surfaces of the particles are substantially free of active ingredient.  
   
   
       21 . The method of  claim 19 , wherein the coating is substantially free of plasticizer.  
   
   
       22 . The method of  claim 19 , wherein the active ingredient is a nonsteroidal anti-inflammatory drug selected from the group consisting of ibuprofen, ketoprofen, flurbiprofen, naproxen, diclofenac, rofecoxib, celecoxib, aspirin, pharmaceutically acceptable salts and metabolites thereof, and mixtures thereof.  
   
   
       23 . (canceled)  
   
   
       24 . (canceled)  
   
   
       25 . The method of  claim 19 , wherein the active ingredient is at least 80% dissolved in 30 minutes in pH 7.2 phosphate buffer when tested according to USP method II at 50 rpm and is at least 70% dissolved in 60 minutes in pH 5.6 acetate buffer when tested according to USP method 11 at 50 rpm.  
   
   
       26 . The particle of  claim 1 , wherein the active ingredient is ibuprofen.  
   
   
       27 . The chewable tablet of  claim 11 , wherein the active ingredient is ibuprofen.  
   
   
       28 . The method of  claim 19 , wherein the active ingredient is ibuprofen.