Pellet and multi-unit pellet system (mups)

Abstract

A pellet contains a core, which contains one or more biologically active ingredients, and a coating layer on the core. The coating layer contains a mixture of a first polymer and a second polymer. The first polymer is a core-shell polymer, containing 50 to 90% by weight of a core, containing polymerized units of 60 to 80% by weight of ethyl acrylate and 20 to 40% by weight of methyl methacrylate; and 10 to 50% by weight of a shell, containing polymerized units of 40 to 60% by weight of ethyl acrylate and 40 to 60% by weight of methacrylic acid. The second polymer contains polymerized units of 40 to 60% by weight of methacrylic acid and 60 to 40% by weight of ethyl acrylate or methyl methacrylate. A Multi-Unit Pellet System (MUPS) contains a multitude of the pellets.

1 - 28 . (canceled) 
     
     
         29 . A pellet, comprising:
 a core, comprising one or more biologically active ingredients, and   a coating layer onto the core,   wherein the coating layer comprises a mixture of a first polymer and a second polymer,   wherein the first polymer is a core-shell polymer, comprising 50 to 90 by weight of a core-shell polymer core, comprising polymerized units of 60 to 80% by weight of ethyl acrylate and 20 to 40% by weight of methyl methacrylate, and
 wherein the core-shell polymer comprises 10 to 50% by weight of a core-shell polymer shell, comprising polymerized units of 40 to 60% by weight of ethyl acrylate and 40 to 60% by weight of methacrylic acid, and 
 wherein the second polymer comprises polymerized units of 40 to 60 by weight of methacrylic acid and 60 to 40% by weight of ethyl acrylate or methyl methacry late, and 
 wherein a ratio of the first polymer to the second polymer is from about 1:0.1 to 1:10. 
   
     
     
         30 . The pellet according to  claim 29 , wherein the core and/or the coating layer comprises a pharmaceutically or nutraceutically acceptable excipient. 
     
     
         31 . The pellet according to  claim 29 , wherein the coating layer comprises 2% by weight or less of a plasticizer. 
     
     
         32 . The pellet according to  claim 29 , wherein the one or more biologically active ingredients are selected from the group consisting of an active pharmaceutical ingredient and an active nu raceutical ingredient. 
     
     
         33 . The pellet according to  claim 29 , wherein the one or more biologically active ingredients are selected from the group consisting of an analgetic, an antibiotic, an anti-infective, an antibody, an antiepileptic, an antigen from plants, an antirheumatic, betablocker, a benzimidazole derivative, a beta-blocker, a cardiovascular drug, a chemotherapeutic, a CNS drug, a digitalis glycoside, a gastrointestinal drug, a combination of proton pump inhibitors with a nonsteroidal anti-inflammatory drug (NSAID), an enzyme, a hormone, a liquid or solid natural extract, an oligonucleotide, a peptide hormone protein, a therapeutical bacteria, a peptide, a protein, a urology drug, a vaccine, and a salt-form thereof. 
     
     
         34 . The pellet according to  claim 29 , wherein the one or more biologically active ingredients are selected from the group consisting of gastrointestinal drugs. 
     
     
         35 . A Multi-Unit Pellet System (MUPS), comprising a multitude of the pellets according to  claim 29 . 
     
     
         36 . The Multi-Unit Pellet System (MUPS) according to  claim 35 , wherein the multitude of pellets is comprised in a capsule, in a sachet, or in a tablet. 
     
     
         37 . The Multi-Unit Pellet System (MUPS) according to  claim 36 , wherein the tablet is a compressed tablet, comprising the multitude of pellets embedded in matrix excipients. 
     
     
         38 . The Multi-Unit Pellet System (MUPS) according to  claim 37 , wherein the compressed tablet comprises 30 to 80% by weight of the matrix excipients and 70 to 20% by weight of the pellets. 
     
     
         39 . The Multi-Unit Pellet System (MUPS) according to  claim 38 , wherein the matrix excipients are selected from the group consisting of antioxidants, brighteners, binding agents, cushioning agents, flavoring agents, flow aids, glidants, penetration-promoting agents, pigments, plasticizers, polymers, pore-forming agents, stabilizers, and a combination thereof. 
     
     
         40 . The Multi-Unit Pellet System (MUPS) according to  claim 38 , wherein the matrix excipients comprise microcrystalline cellulose, glycerol monostearate, or lactose. 
     
     
         41 . The Multi-Unit Pellet System (MUPS) according to  claim 38 , wherein a release curve of the one or more biologically active ingredients from the pellets and that of the compressed tablets show an F2-value of 50 or more. 
     
     
         42 . A process for preparing Multi-Unit Pellet System (MUPS according to  claim 38 , the process comprising:
 providing the multitude of pellets,   adding the matrix excipients, to obtain a mixture, and   compressing the mixture to a compressed tablet.   
     
     
         43 . A method of therapy and treatment of a disease of a human or animal body with the Multi-Unit Pellet System (MUPS) according to  claim 36 , the method comprising:
 administering the Multi-Unit Pellet System (MUPS) as a medicament to or animal in need thereof,   wherein the disease is selected from the group consisting of an ulcer of the stomach and duodenum, a NSAID-induced ulcer, a Helicobacter pylori infection, gastrointestinal reflux disease, Zollinger-Ellison syndrome, arthrosis, pain, and inflammation, and   wherein the one or more biologically active ingredients is selected from the group consisting of esomeprazole, dexlansoprazole, lansoprazole, omeprazole, pantoprazole, rabeprazole, a combination thereof, and a combination of esomeprazole and naproxen.   
     
     
         44 . The pellet according to  claim 33 , wherein the salt-form is an aspartate or a hydrochloride. 
     
     
         45 . The pellet according to  claim 34 , wherein the one or more biologically active ingredients are selected from the group consisting of proton pump inhibitors. 
     
     
         46 . The pellet according to  claim 34 , wherein the one or more biologically active ingredients are selected from the group consisting of esomeprazole, dexlansoprazole, lansoprazole, omeprazole, pantoprazole, rabeprazole, a combination thereof, and a combination of esomeprazole and naproxen.