Process for the preparation of delayed release solid formulations

Abstract

A process for the preparation of oral delayed release solid formulations and the formulations obtainable from said process are now described. Said process comprises the following steps: a) melting at least one lipid; b) spraying said at least one melted lipid on at least one active ingredient in the form of a moving powder; c) cooling the resulting mixture; d) optional granulation of the mixture; e) optional compression of the mixture.

1 . Process for the preparation of a delayed release formulation for oral use comprising the following steps:
 a) melting at least one lipid to form a melted lipid;   b) spraying said at least one melted lipid on at least one active ingredient in the form of a moving powder to form a resulting mixture;   c) cooling the resulting mixture.   
     
     
         2 . Process according to  claim 1 , characterized in that the lipid melting step a) is performed at a temperature of between 55 and 80° C. 
     
     
         3 . Process according to  claim 1 , characterized in that the lipid spraying step b) is performed through nozzles arranged linearly with respect to the surface of the active ingredient advancement plane. 
     
     
         4 . Process according to  claim 3 , characterized in that the number of said nozzles is greater than 5. 
     
     
         5 . Process according to  claim 1 , characterized in that the lipid spraying step b) is performed at a flow rate of 0.005-0.04 l/min per kg of active ingredient. 
     
     
         6 . Process according to  claim 1 , characterized in that the lipid spraying step b) is performed through nozzles inclined of 35°-55°. 
     
     
         7 . Process according to  claim 3 , characterized in that said nozzles have a diameter of between 0.2 and 4 mm. 
     
     
         8 . Process according to  claim 3 , characterized in that said nozzles are spaced apart by 0.5-1 cm. 
     
     
         9 . Process according to  claim 3 , characterized in that the orifices of said nozzles are positioned at 10-40 cm from the powder surface. 
     
     
         10 . Process according to  claim 1 , characterized in that the powder advances at a speed of between 0.10 and 0.40 m/sec. 
     
     
         11 . Process according to  claim 1 , characterized in that said at least one active ingredient in the form of a powder has a particle size of between 50 and 800 μm. 
     
     
         12 . Process according to  claim 1 , characterized in that during step c) the mixture is cooled to a temperature lower than 35° C. 
     
     
         13 . Process according to  claim 12 , characterized in that the cooling is performed by insufflation of air at a temperature of between 30 and 35° C. 
     
     
         14 . Process according to  claim 1 , characterized in that said lipid is a triglyceride, a diglyceride, a fatty acid, or a mixture thereof. 
     
     
         15 . Process according to  claim 14 , characterized in that the fatty acidhas a chain length of between 8 and 20 carbon atoms. 
     
     
         16 . Process according to  claim 14 , characterized in that said fatty acid is saturated. 
     
     
         17 . Process according to  claim 1 , characterized in that said at least one active ingredient is pharmaceutically, nutraceutically, dietetically and/or alimentary active. 
     
     
         18 . Process according to  claim 1 , characterized in that said lipid is present in an amount of between 5 and 60% by weight. 
     
     
         19 . Process according to  claim 1 , characterized in that said at least one active ingredient is mixed with at least one physiologically acceptable excipient.