Patent EA-003161-B1 (EA)
Title: Method for manufacturing coated granules with masked taste and instant release of the active principle
Inventor: NOURI NOUREDDIINE
IPC: A61K47/22
Filed: 2000-06-30
Abstract: 1. A process for manufacturing coated granules with masked taste, and immediate release of the active principle, according to which: the constituents of a powder comprising at least the active principle and a granular disintegrant are first dry-mixed; the powder obtained is then granulated, in the presence of a mixture of excipients comprising at least one binder capable of binding the particles together to give grains and containing no membrane disintegrant; the grains formed are then coated by spraying with a suspension comprising at least one coating agent and a membrane disintegrant; finally, the coated granules obtained are dried. 2. A process for manufacturing coated granules with masked taste, and immediate release of the active principle, according to which: the constituents of a powder comprising at least the active principle and a granular disintegrant are first dry-mixed; the powder obtained is then granulated, and the grains formed are then coated, in the presence of the same mixture of excipients comprising at least one binder capable of binding particles together to give grains; at least one coating agent and a membrane disintegrant; the rate of spraying of the mixture of excipients being higher during the granulation step than during the coating step, and the atomization pressure of the mixture of excipients being lower during the granulation step than during the coating step; finally, the coated granules obtained are dried. 3. The manufacturing process as claimed in claim 2, characterized in that between 10 and 20% of the mixture of excipients is sprayed during the granulation step, the remainder being sprayed during the coating step. 4. The process for manufacturing coated granules as claimed in one of claims 1 to 3, characterized in that the granule and membrane disintegrants are high-performance disintegrants chosen from the group comprising sodium carboxymethylcellulose, crospovidone and carboxymethylstarch. 5. The process for manufacturing coated granules as claimed in one of claims 1 to 3, characterized in that the binder and the coating agent are chosen from the group comprising cellulose polymers and acrylic polymers. 6. The process for manufacturing coated granules as claimed in claim 5, characterized in that the cellulose polymer is chosen from the group comprising ethylcellulose, hydroxypropylcellulose (HPC), carboxymethylcellulose (CMC) and hydroxypropylmethylcellulose (HPMC), alone or as a mixture. 7. The process for manufacturing coated granules as claimed in claim 5, characterized in that the acrylic polymer is chosen from the group comprising acrylic polymers and methacrylic polymers, ammonio-methacrylate copolymer, polyacrylate and methacrylic acid copolymer. 8. The process for manufacturing coated granules as claimed in claim 1, characterized in that the suspension also comprises a permeabilizer. 9. The process for manufacturing coated granules as claimed in claim 1, characterized in that the mixture of excipients used in the granulation step also comprises a permeabilizer. 10. The manufacturing process as claimed in either of claims 2 and 3, characterized in that the mixture of excipients also comprises a permeabilizer. 11. The process for manufacturing coated granules as claimed in one of claims 8 to 10, characterized in that the permeabilizer is chosen from the group comprising povidone and its derivatives, polyethylene glycol, silica, polyols and low-viscosity cellulose polymers. 12. The process for manufacturing coated granules as claimed in claim 1, characterized in that the suspension sprayed during the coating step also comprises a sweetener. 13. The process for manufacturing coated granules as claimed in one of claims 1 to 3, characterized in that the dry mix of initial powder also comprises a sweetener. 14. The manufacturing process as claimed in either of claims 2 and 3, characterized in that the mixture of excipients also comprises a sweetener. 15. The process for manufacturing coated granules as claimed in one of claims 10 to 14, characterized in that the sweetener is chosen from the group comprising aspartame potassium acesulfam, sodium saccharinate, neohesperidine dihydrochalcone, monoammonium glycyrrhizinate, sugars and derivatives, and also polyols and derivatives, alone or as a mixture. 16. The process for manufacturing coated granules as claimed in one of claims 1 to 3, characterized in that the dry-mixing of initial powder, the granulation, the coating and the drying are performed in a fluidized bed. 17. A coated granule which may be obtained by the process which is the subject of one of claims 1 to 16. 18. The coated granule as claimed in claim 17, characterized in that it comprises, by weight of the coated granule: from 5 to 70% of a coating polymer, from 0.5 to 15% of a granule disintegrant, from 1 to 20% of a membrane disintegrant, from 1 to 20% of a permeabilizer. 19. The coated granule as claimed in claim 18, characterized in that it also comprises from 1 to 20% by weight of a sweetener. 20. The coated granule as claimed in claim 19, characterized in that it comprises, by weight of the coated granule: from 10 to 40% ethylcellulose, from 3 to 10% crospovidone, from 2 to 10% polyethylene glycol, from 2 to 10% aspartam. 21. A fast-crumbling multiparticulate tablet comprising the granules which are the subject of one of claims 17 to 20. 22. A fast-dispersible tablet comprising the granules which are the subject of one of claims 17 to 20.