Coated Tablet Formulation and Method

Abstract

A coated tablet formulation is provided which includes a medicament such as the DPP4-inhibitor, saxaglipitin or its HCl salt, which is subject to intra-molecular cyclization, which formulation includes a tablet core containing one or more fillers, and other conventional excipients, which tablet core includes a coating thereon which may include two or more layers, at least one layer of which is an inner seal coat layer which is formed of one or more coating polymers, a second layer of which is formed of medicament which is the DPP4-inhibitor and one or more coating polymers, and an optional, but preferable third outer protective layer which is formed of one or more coating polymers. A method for forming the coated tablet is also provided.

What is claimed is: 
     
         1 . A coated tablet comprising
 a) a tablet core;   b) an inner seal coating layer coated on the tablet core, wherein the inner seal coating layer comprises at least one coating layer polymer;   c) a second coating layer coated on the inner seal coating layer, wherein the second coating layer comprises saxagliptin   
       
         
           
           
               
               
           
         
       
       or a pharmaceutically acceptable salt thereof and at least one coating layer polymer, and
 d) optionally a third outer protective coating layer coated on the second coating layer, wherein the third outer protective coating layer comprises at least one coating layer polymer. 
 
     
     
         2 . The coated tablet as defined in  claim 1 , wherein the saxagliptin is present as a hydrochloride salt. 
     
     
         3 . The coated tablet as defined in  claim 1 , wherein the inner seal coating layer comprises at least one coating layer polymer selected from the group consisting of hydroxypropyl methylcellulose, polyvinyl alcohol, ethyl cellulose, methacrylic polymers and hydroxypropyl cellulose. 
     
     
         4 . The coated tablet as defined in  claim 3 , wherein the at least one coating layer polymer is polyvinyl alcohol. 
     
     
         5 . The coated tablet as defined in  claim 1 , wherein the second coating layer coated on the inner seal coating layer comprises saxagliptin 
       
         
           
           
               
               
           
         
       
       or a pharmaceutically acceptable salt thereof and at least one coating layer polymer selected from the group consisting of hydroxypropyl methylcellulose, polyvinyl alcohol, ethyl cellulose, methacrylic polymers and hydroxypropyl cellulose. 
     
     
         6 . The coated tablet as defined in  claim 5 , wherein the at least one coating layer polymer is polyvinyl alcohol. 
     
     
         7 . The coated tablet as defined in  claim 1 , wherein the inner seal coating layer further comprises polyethylene glycol. 
     
     
         8 . The coated tablet as defined in  claim 1 , wherein the second coating layer further comprises polyethylene glycol. 
     
     
         9 . A coated tablet comprising
 a) a tablet core;   b) an inner seal coating layer coated on the tablet core, wherein the inner seal coating layer comprises at least one coating layer polymer;   c) a second coating layer coated on the inner seal coating layer, wherein the second coating layer comprises saxagliptin   
       
         
           
           
               
               
           
         
       
       or a pharmaceutically acceptable salt thereof and at least one coating layer polymer, and
 d) a third outer protective coating layer coated on the second coating layer, wherein the third outer protective coating layer comprises at least one coating layer polymer. 
 
     
     
         10 . The coated tablet as defined in  claim 9 , wherein the saxagliptin is present as a hydrochloride salt. 
     
     
         11 . The coated tablet as defined in  claim 9 , wherein the third outer protective coating layer coated on the second coating layer comprises at least one coating layer polymer selected from the group consisting of hydroxypropyl methylcellulose, polyvinyl alcohol, ethyl cellulose, methacrylic polymers and hydroxypropyl cellulose;wherein the at least one coating polymer. 
     
     
         12 . The coated tablet as defined in  claim 11 , wherein the at least one coating layer polymer is polyvinyl alcohol. 
     
     
         13 . The coated tablet as defined in  claim 9 , wherein the third outer protective coating layer further comprises polyethylene glycol. 
     
     
         14 . A combination formulation comprising
 a) a drug tablet;   b) an inner seal coating layer coated on the drug tablet, wherein the inner seal coating layer comprises at least one coating layer polymer;   c) a second coating layer coated on the inner seal coating layer, wherein the second coating layer comprises saxagliptin   
       
         
           
           
               
               
           
         
       
       or a pharmaceutically acceptable salt thereof and at least one coating layer polymer, and
 d) a third outer protective coating layer coated on the second coating layer, wherein the third outer protective coating layer comprises at least one coating layer polymer; 
 wherein the drug tablet comprises a drug other than saxagliptin or a pharmaceutically acceptable salt thereof. 
 
     
     
         15 . The combination formulation as defined in  claim 14 , wherein the saxagliptin is present as a hydrochloride salt. 
     
     
         16 . The combination formulation as defined in  claim 14 , wherein the inner seal coating layer comprises at least one coating layer polymer selected from the group consisting of hydroxypropyl methylcellulose, polyvinyl alcohol, ethyl cellulose, methacrylic polymers and hydroxypropyl cellulose. 
     
     
         17 . The combination formulation as defined in  claim 16 , wherein the at least one coating layer polymer is polyvinyl alcohol. 
     
     
         18 . The combination formulation as defined in  claim 14 , wherein the second coating layer coated on the inner seal coating layer comprises saxagliptin 
       
         
           
           
               
               
           
         
       
       or a pharmaceutically acceptable salt thereof and at least one coating layer polymer selected from the group consisting of hydroxypropyl methylcellulose, polyvinyl alcohol, ethyl cellulose, methacrylic polymers and hydroxypropyl cellulose. 
     
     
         19 . The combination formulation as defined in  claim 14 , wherein the third outer protective coating layer coated on the second coating layer comprises at least one coating layer polymer selected from the group consisting of hydroxypropyl methylcellulose, polyvinyl alcohol, ethyl cellulose, methacrylic polymers and hydroxypropyl cellulose;wherein the at least one coating polymer. 
     
     
         20 . The combination formulation as defined in  claim 19 , wherein the at least one coating layer polymer is polyvinyl alcohol.