# US 2011/0033537 A1 · Sustained Drug Release Composition > Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt - Number: US 2011/0033537 A1 - Document ID: US20110033537A1 - Status: Published application - Kind: A1 - Application number: 12/905,577 - Filed: 2010-10-15 - Published: 2011-02-10 - Earliest claimed: 2005-09-09 - Assignees: Angelini Pharma S.P.A. - Inventors: Sonia Gervais; Damon Smith; Pauline Contamin; Rachid Ouzerourou; My Linh Ma - Web page: https://patentgrep.com/patent/US20110033537A1 ## CPC - A61K 9/2072: {characterised by shape, structure or size; Tablets with holes, special break lines or identification marks; Partially coated tablets; Disintegrating flat shaped forms (A61K9/0004, A61K9/0056, A61K9/0065 take precedence)} - A61K 9/205: {Polysaccharides, e.g. alginate, gums; Cyclodextrin} - A61K 9/2054: {Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose} - A61K 9/2059: {Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin} - A61K 9/28: Dragees; Coated pills or tablets {, e.g. with film or compression coating (A61K9/2072 takes precedence, e.g. partially coated tablets A61K9/2072, coated multilayer tablets A61K9/2086, tablets with drug-coated core A61K9/209)} - A61K 9/2866: {Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose} - A61K 31/135: having aromatic rings {, e.g. ketamine, nortriptyline (methadone A61K31/137)} - A61K 31/16: Amides, e.g. hydroxamic acids - A61K 31/167: having the nitrogen of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol - A61K 31/4402: only substituted in position 2, e.g. pheniramine, bisacodyl - A61K 31/496: Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin - A61P 9/08: Vasodilators for multiple indications - A61P 25/04: Centrally acting analgesics, e.g. opioids - A61P 25/18: Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia - A61P 25/20: Hypnotics; Sedatives - A61P 25/24: Antidepressants - A61P 29/00: Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID] - A61P 29/02: without antiinflammatory effect - 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) - A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS ## Abstract The invention relates to a sustained release formulation for delivering one or more pharmaceutically active agents. The formulation comprises cross-linked high amylose starch and at least one pharmaceutically active agent, and optionally can be subdivided into smaller dosage forms where the smaller dosage forms have substantially the same sustained release properties as the formulation from which they were derived. The formulations can provide sustained release for up to at least 24 hours, and because of their divisability permits a recipient of the active agent or the person administering the active agent to titrate the dosage of the agent. ## Claims ### Claim 1 A solid, monolithic sustained release pharmaceutical composition, the composition comprising: a. a sustained release matrix having a solvent accessible surface, wherein the matrix comprises cross-linked high amylose starch; and b. an effective amount of at least one pharmaceutically active agent disposed within the matrix, wherein the composition has a hardness of greater than about 100 N. ### Claim 2 (depends on 1) The composition of claim 1, wherein the hardness is in the range of about 100N to about 350 N. ### Claim 3 (depends on 1) The composition of claim 1, wherein the composition, when administered to a mammal, achieves an effective plasma concentration of the active agent from at least about 1 hour to at least about 24 hours after initial administration. ### Claim 4 (depends on 1) The composition of claim 1, wherein the solvent accessible surface defines a score that permits the composition to be fractured along the score to produce at least two subunits each having a new solvent accessible surface. ### Claim 5 (depends on 4) The composition of claim 4, wherein at least one of the subunits has substantially the same release kinetics of the active agent as the intact composition from which it was derived. ### Claim 6 (depends on 4) The composition of claim 4, wherein the dissolution profiles of at least one of the subunits and the composition from which it was derived have a similarity factor of at least 50%. ### Claim 7 (depends on 6) The composition of claim 6, wherein the similarity factor is at least 55%. ### Claim 8 A solid, monolithic sustained release pharmaceutical composition comprising: a. a sustained release matrix having a solvent accessible surface, wherein the matrix comprises cross-linked high amylose starch; and b. an effective amount of a pharmaceutically active agent disposed within the matrix, wherein the composition displays substantially the same release kinetics when the composition is broken to create a new solvent accessible surface. ### Claim 9 A solid, monolithic sustained release pharmaceutical composition comprising: a. a sustained release matrix comprising cross-linked high amylose starch; and b. an effective amount of a pharmaceutically active agent disposed within the matrix, wherein the composition can be divided into at least two subunits where each subunit releases the active agent with substantially the same release profile as the composition from which it was derived. ### Claim 10 (depends on 8) The composition of claim 8, wherein the composition has a hardness of greater than about 100 N. ### Claim 11 (depends on 10) The composition of claim 10, wherein the composition has a hardness in the range of from about 100 N to about 180 N. ### Claim 12 (canceled) ### Claim 13 (depends on 9) The composition of claim 9, wherein the dissolution profiles of at least one subunit and the composition from which it was derived have a similarity factor of at least 50%. ### Claim 14 (depends on 13) The composition of claim 13, wherein the similarity factor is at least 55%. ### Claim 15 (depends on 4) The composition of claim 4, wherein the new solvent accessible surface is capable of forming a barrier upon contact with a solvent. ### Claim 16 (depends on 4) The composition of claim 4, wherein the subunits and the intact composition from which they are derived are bioequivalent. ### Claim at position 17 17-22. (canceled) ### Claim 23 (depends on 1) The composition of claim 1, comprising from about 15% to about 60% by weight of the active ingredient and from about 15% to about 85% by weight of the starch. ### Claim 24 (depends on 23) The composition of claim 23 comprising from about 20% to about 50% by weight of the active ingredient and from about 20% to about 50% by weight of the starch. ### Claim 25 (depends on 24) The composition of claim 24 comprising from about 35% to about 50% by weight of the active ingredient and from about 20% to about 50% by weight of the starch. ### Claim 26 (depends on 1) The composition of claim 1, wherein the starch is crosslinked with phosphorus oxychloride. ### Claim 27 (depends on 1) The composition of claim 1, wherein the starch comprises hydroxypropyl side chains. ### Claim 28 (depends on 1) The composition of claim 1, wherein the active agent is selected from the group consisting of an antidepressant or an analgesic. ### Claim 29 (depends on 28) The composition of claim 28, wherein the antidepressant is trazodone. ### Claim at position 25 30-35. (canceled) ### Claim 36 (depends on 1) The composition of claim 1, wherein the composition is in the form of a tablet. ### Claim 37 (depends on 36) The composition of claim 36, wherein the tablet has a score. ### Claim 38 (depends on 1) The composition of claim 1, wherein the composition is in the form of a caplet. ### Claim 39 (depends on 38) The composition of claim 38, wherein the caplet has a score. ### Claim 40 (depends on 37) The composition of claim 37, wherein the composition, when fractured along the score creates a new solvent accessible surface. ### Claim at position 31 41-42. (canceled)