Pharmaceutical Composition of Rosuvastatin Calcium

Abstract

The invention relates to pharmaceutical compositions containing rosuvastatin calcium of formula (I) and processes for their manufacture.

1 . A process for formation of a pharmaceutical formulation comprising a rosuvastatin calcium containing layer, said process comprising spray coating a solution comprising rosuvastatin calcium and a first coating polymer in water onto a tablet, pellet or granule core. 
     
     
         2 . A process as claimed in  claim 1  comprising:
 a) Coating a tablet, pellet or granule core with a sub-coating layer of a second coating polymer; and 
 b) Spray coating the solution comprising rosuvastatin calcium and a first coating polymer in water onto the coated tablet, pellet or granule core to provide a rosuvastatin calcium containing layer. 
 
     
     
         3 . A process as claimed in  claim 1  or  2  comprising:
 a) Optionally coating a tablet, pellet or granule core with a sub-coating layer of a second coating polymer; 
 b) Spray coating the solution comprising rosuvastatin calcium and a first coating polymer in water onto the (optionally coated) tablet, pellet or granule core to provide a rosuvastatin calcium containing layer; and 
 c) Coating the rosuvastatin calcium containing layer with an outer coating comprising a third coating polymer. 
 
     
     
         4 . A process as claimed in any one of  claims 1  to  3  wherein the tablet, pellet or granule core comprises an active ingredient which is not rosuvastatin calcium. 
     
     
         5 . A process as claimed in  claim 4  wherein the core contains an active ingredient which is not selected from any one or more of: niacin or a niacin analogue, a fibrate, metformin, a CETP inhibitor and/or aspirin. 
     
     
         6 . A process as claimed in  claim 4  or  5 , wherein the core comprises an active ingredient which is selected from:
 sulfonylureas, thiazolidinediones, DPP-4 inhibitors, SGLT-2 inhibitors, aldose reductase inhibitors, phosphodiesterase-5 inhibitors, phosphodiesterase-3 inhibitor, platelet aggregation inhibitors, Factor Xa inhibitors, dipyridamole, peripheral calcium channel blockers, diuretics, angiotensin converting enzyme inhibitors, angiotensin II receptor antagonists, direct thombin inhibitors, coenzyme Q-10, vitamin D1 (ergocalciferol), vitamin D3 (cholecalciferol), GPR40 agonists and antiobesity drugs. 
 
     
     
         7 . A process as claimed in any one of the previous claims wherein the first coating polymer is an HMPC/PEG polymer. 
     
     
         8 . A process as claimed in any one of the previous claims wherein the first coating polymer further comprises a stabilization agent. 
     
     
         9 . A process as claimed in  claim 8  wherein the stabilization agent is calcium acetate or BHA. 
     
     
         10 . A process as claimed in  claim 8  wherein the stabilization agent is calcium acetate. 
     
     
         11 . A process as claimed in any one of the preceding claims wherein all the coating polymers are HMPC/PEG polymers. 
     
     
         12 . A process as claimed in any one of  claims 3  to  11  wherein the outer coating also contains ferric oxide. 
     
     
         13 . A process as claimed in any one of the preceding claims wherein the rosuvastatin containing layer comprises rosuvastatin calcium and the first coating polymer in a ratio of between approximately 1:8 to 2:1 
     
     
         14 . A process as claimed in any one of the preceding claims wherein the core is a tablet core. 
     
     
         15 . A process as claimed in any one of the preceding claims wherein the core is a pellet or granule core. 
     
     
         16 . A process as claimed in  claim 15  wherein the coated pellet or granule core is further processed to form a pharmaceutical product. 
     
     
         17 . A product obtainable by the process as claimed in any one of the preceding claims. 
     
     
         18 . A pharmaceutical formulation comprising a tablet, pellet or granule core spray coated with a layer comprising rosuvastatin calcium in an HMPC/PEG polymer, further coated with an outer layer comprising an HMPC polymer and ferric oxide, wherein the rosuvastatin calcium containing layer is coated onto the tablet, pellet or granule core by spray coating a solution of rosuvastatin calcium and an HPMC/PEG polymer in water.