# US 8,465,770 B2 · Low dose controlled release tablet > Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt - Number: US 8,465,770 B2 - Document ID: US8465770B2 - Status: Granted - Kind: B2 - Application number: 12/634,890 - Filed: 2009-12-10 - Published: 2010-04-15 - Granted: 2013-06-18 - Earliest claimed: 2008-12-24 - Assignees: Synthon BV - Applicants: Korinde Annemarie Jansen; Dirk Pamperin - Inventors: Korinde Annemarie Jansen; Dirk Pamperin - Web page: https://patentgrep.com/patent/US8465770B2 ## CPC - A61K 31/18: Sulfonamides (compounds containing a para-N-benzene-sulfonyl-N- group A61K31/63) - A61K 9/2027: {obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates} - A61K 9/2054: {Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose} - A61K 9/2086: {Layered tablets, e.g. bilayer tablets; Tablets of the type inert core-active coat (active cores with a complete drug-free outer coat A61K9/28)} - A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D) ## Abstract Low dose pharmaceuticals can be delivered for a prolonged period using a tablet-in-tablet design wherein the drug is contained in a controlled release matrix in the outer compression coating layer but not in the inner tablet core. ## Claims ### Claim 1 A controlled release pharmaceutical tablet, comprising: (a) an inner tablet core having a size within the range of 3 to 7 mm and comprising at least one pharmaceutically acceptable excipient but substantially free from any pharmaceutically active agent; and (b) an outer compression coating layer surrounding said inner tablet core and which comprises a controlled release matrix having a pharmaceutically active agent dispersed therein; wherein the total amount of pharmaceutically active agent contained in said tablet is within the range of 0.1 to 5 mg. ### Claim 2 (depends on 1) The pharmaceutical tablet according to claim 1, wherein said inner tablet core contains no pharmaceutical active agent. ### Claim 3 (depends on 2) The pharmaceutical tablet according to claim 2, wherein said outer compression coating layer adds at least 2 mm to the total controlled release tablet size. ### Claim 4 (depends on 3) The pharmaceutical tablet according to claim 3, wherein said pharmaceutical active agent is tamsulosin or a pharmaceutically acceptable salt thereof. ### Claim 5 A controlled release tamsulosin tablet comprising: (a) an inner tablet core having a size within the range of 3 to 7 mm and comprising at least one pharmaceutically acceptable excipient and substantially free from any pharmaceutically active agent; and (b) an outer compression coating layer surrounding said inner tablet core and which comprises 0.1 to 2 mg of tamsulosin or salt thereof dispersed in a water-swellable matrix comprising (i) at least one pH-sensitive swellable hydrophilic polymer, which is a cross-linked polyacrylic acid polymer, and (ii) at least one pH-insensitive swellable hydrophilic polymer; and optionally a water insoluble binder. ### Claim 6 (depends on 5) The tamsulosin tablet according to claim 5, wherein said inner tablet core contains no pharmaceutical active agent. ### Claim 7 (depends on 6) The tamsulosin tablet according to claim 6, wherein said tamsulosin is tamsulosin hydrochloride. ### Claim 8 (depends on 6) The tamsulosin tablet according to claim 6, wherein said tamsulosin or salt thereof is contained in an amount between 0.1 to 1 mg. ### Claim 9 (depends on 6) The tamsulosin tablet according to claim 6, wherein said pH-insensitive polymer is a linear polymer. ### Claim 10 (depends on 6) The tamsulosin tablet according to claim 6, wherein said pH-sensitive polymer is a carbomer. ### Claim 11 (depends on 10) The tamsulosin tablet according to claim 10, wherein said pH-insensitive polymer is a hydroxypropyl methylcellulose. ### Claim 12 (depends on 11) The tamsulosin tablet according to claim 11, wherein said hydroxypropyl methylcellulose has a nominal dynamic viscosity of at least about 100,000 mPa/s. ### Claim 13 (depends on 6) The tamsulosin tablet according to claim 6, wherein said outer compression coating layer contains a water insoluble binder. ### Claim 14 (depends on 13) The tamsulosin tablet according to claim 13, wherein said water insoluble binder is microcrystalline cellulose. ### Claim 15 (depends on 6) The tamsulosin tablet according to claim 6, wherein said inner tablet core has a diameter of 5-6 mm. ### Claim 16 (depends on 6) The tamsulosin tablet according to claim 6, wherein said at least one excipient in said inner tablet core comprises a water-swellable matrix composition and optionally a water insoluble binder. ### Claim 17 (depends on 11) The tamsulosin tablet according to claim 11, wherein said at least one excipient in said inner tablet core comprises a water-swellable matrix composition and optionally a water insoluble binder. ### Claim 18 (depends on 17) The tamsulosin tablet according to claim 17, wherein said water-swellable matrix composition of said inner tablet core comprises at least one pH-sensitive swellable hydrophilic polymer, which is a cross-linked polyacrylic acid polymer, and at least one pH-insensitive swellable hydrophilic polymer. ### Claim 19 (depends on 18) The tamsulosin tablet according to claim 18, wherein said inner tablet core contains a water insoluble binder and wherein said water insoluble binder is microcrystalline cellulose. ### Claim 20 (depends on 6) The tamsulosin tablet according to claim 6, wherein said inner tablet core and said outer compression coating layer contain the same water-swellable matrix composition and water insoluble binder in the same mass ratios +/−10%. ### Claim 21 (depends on 6) The tamsulosin tablet according to claim 6, wherein the mass ratio of said inner tablet core to said outer compression coating layer is from 15:85 to 30:70, respectively. ### Claim 22 (depends on 6) The tamsulosin tablet according to claim 6, wherein said tamsulosin tablet exhibits an in vitro dissolution profile such that said tamsulosin is still being released after 18 hours in artificial intestinal fluid.