# US 7,608,282 B2 · Transdermal granisetron > Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt - Number: US 7,608,282 B2 - Document ID: US7608282B2 - Status: Granted - Kind: B2 - Application number: 10/544,259 - Filed: 2004-02-05 - Published: 2006-08-10 - Granted: 2009-10-27 - Earliest claimed: 2003-02-05 - Assignees: Strakan International Limited - Inventors: Peter Altenschöpfer; Adam Charles Watkinson - Web page: https://patentgrep.com/patent/US7608282B2 ## CPC - A61K 9/7061: {Polyacrylates} - A61K 31/439: the ring forming part of a bridged ring system, e.g. quinuclidine (8-azabicyclo [3.2.1] octanes A61K31/46) - A61P 1/00: Drugs for disorders of the alimentary tract or the digestive system - A61P 1/04: for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants - A61P 1/08: for nausea, cinetosis or vertigo; Antiemetics - A61P 1/14: Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents - A61P 7/12: Antidiuretics, e.g. drugs for diabetes insipidus (ADH A61P5/10) - A61P 11/00: Drugs for disorders of the respiratory system - A61P 13/02: of urine or of the urinary tract, e.g. urine acidifiers - A61P 13/10: of the bladder - A61P 15/00: Drugs for genital or sexual disorders (for disorders of sex hormones A61P5/24); Contraceptives - A61P 15/08: for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis - A61P 17/04: Antipruritics - A61P 25/00: Drugs for disorders of the nervous system - A61P 25/04: Centrally acting analgesics, e.g. opioids - A61P 25/06: Antimigraine agents - A61P 25/14: for treating abnormal movements, e.g. chorea, dyskinesia - A61P 25/18: Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia - A61P 25/22: Anxiolytics - A61P 25/24: Antidepressants - A61P 25/28: for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia - A61P 25/30: for treating abuse or dependence - A61P 25/32: Alcohol-abuse - A61P 25/36: Opioid-abuse - A61P 29/00: Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID] - A61P 37/00: Drugs for immunological or allergic disorders - A61P 37/02: Immunomodulators - A61P 39/00: General protective or antinoxious agents - A61P 39/02: Antidotes - 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 Adhesive patches for the transdermal administration of granisetron, comprise an acrylic adhesive containing non-acidic nucleophilic moieties which substantially increase flux of granisetron across the skin. ## Claims ### Claim 1 An adhesive patch suitable for the transdermal administration of granisetron to a subject in need thereof, said patch comprising: an acrylic adhesive consisting essentially of: 50 to 98% w/w of a primary acrylate monomer wherein said primary acrylate monomer is either 2-ethylhexyl acrylate or butyl acrylate, and 0.5 to 20% w/w of a monomer containing non-acidic hydroxyl moieties, and a physiologically effective amount of granisetron loaded in the acrylic adhesive, wherein the granisetron content of said patch remains substantially unchanged when stored at 25° C. for six weeks. ### Claim 2 (depends on 1) A patch according to claim 1, wherein the monomer containing non-acidic hydroxyl moieties is selected from the group consisting of hydroxymethyl acrylates, hydroxyethyl acrylates and hydroxypropyl acrylates. ### Claim 3 (depends on 1) A patch according to claim 1, wherein the monomer containing non-acidic hydroxyl moieties is selected from the group consisting of hydroxymethyl methacrylates and hydroxyethyl methacrylates. ### Claim 4 (depends on 1) A patch according to claim 1, which is pressure sensitive. ### Claim 5 (depends on 1) A patch according to claim 1, containing 50 to 90% w/w of said primary acrylate monomer. ### Claim 6 (depends on 1) A patch according to claim 1, adapted to provide a pharmacologically effective amount of granisetron to said subject within about 2 hours after administration thereof. ### Claim 7 (depends on 1) A patch according to claim 1, having up to about 10% by weight of granisetron. ### Claim 8 (depends on 7) A patch according to claim 7, having less than 8% w/w granisetron. ### Claim 9 (depends on 1) A patch according to claim 1, having a level of granisetron above 4% w/w. ### Claim 10 (depends on 7) A patch according to claim 7, having a level of between 6% and 7.7% w/w of granisetron. ### Claim 11 (depends on 1) A patch according to claim 1, wherein no crystallisation is observed after one month storage at room temperature and pressure. ### Claim 12 (depends on 1) A patch according to claim 1, for the treatment and/or prophylaxis of chemically induced emesis. ### Claim 13 (depends on 12) A patch according to claim 12, wherein the emesis is acute. ### Claim 14 (depends on 12) A patch according to claim 12, wherein the emesis is delayed. ### Claim 15 (depends on 1) A patch according to claim 1, for the treatment and/or prophylaxis of emesis associated with fractionated chemotherapy. ### Claim 16 (depends on 1) A patch according to claim 1, for the treatment and/or prophylaxis of postoperative nausea and vomiting. ### Claim 17 (depends on 1) A patch according to claim 1, for the treatment and/or prophylaxis of nausea and vomiting associated with radiotherapy. ### Claim 18 (depends on 1) A patch according to claim 1, for the treatment and/or prophylaxis of nausea and vomiting associated with fractionated cancer therapy. ### Claim 19 (depends on 1) A patch according to claim 1, wherein the acrylic adhesive is loaded with between 3 and 12% w/w granisetron. ### Claim 20 (depends on 19) A patch according to claim 19, wherein the acrylic adhesive is loaded with between 4 and 10% w/w granisetron. ### Claim 21 (depends on 19) A patch according to claim 19, wherein the acrylic adhesive is loaded with between 5 and 8% w/w granisetron. ### Claim 22 (depends on 1) A patch according to claim 1, incorporating no plasticizers or permeation enhancers. ### Claim 23 (depends on 1) A patch according to claim 1, wherein, at an acrylic adhesive loading of 6% w/w of active granisetron, the acrylic adhesive has a surface area of between 10 and 100 cm2. ### Claim 24 (depends on 23) A patch according to claim 23, wherein the acrylic adhesive has a surface area of between 15 and 50 cm2. ### Claim 25 (depends on 1) A method for the treatment and/or prophylaxis of any form of nausea or emesis associated with 5-HT3 receptor activity in a patient in need thereof, said method comprising applying an adhesive patch according to claim 1 to the skin of the patient. ### Claim 26 (depends on 1) A method for the treatment and/or prophylaxis of chemotherapy induced nausea and vomiting in a patient in need thereof, said method comprising applying an adhesive patch according to claim 1 to the skin of the patient. ### Claim 27 (depends on 1) A patch according to claim 1, for the treatment and/or prophylaxis of chemotherapy-induced nausea and vomiting. ### Claim 28 (depends on 1) A patch according to claim 1, wherein the granisetron content of said patch remains substantially unchanged when stored at 40° C. for six weeks.