# US 5,705,506 A · Pharmaceutical compositions of alkylsulphonamides 5HT1 agonists for rectal administration > Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt - Number: US 5,705,506 A - Document ID: US5705506A - Status: Granted - Kind: A - Application number: 08/331,485 - Filed: 1994-12-29 - Granted: 1998-01-06 - Earliest claimed: 1992-05-07 - Assignees: Laboratoires Glaxo SA - Inventors: Nadine Merlet; Isabelle Richard; Isabelle Thielemans - Web page: https://patentgrep.com/patent/US5705506A ## CPC - A61K 9/02: Suppositories; Bougies; Bases therefor; {Ovules}(apparatus for making A61J3/08; devices for introducing into the body A61M31/00) - A61K 31/00: Medicinal preparations containing organic active ingredients - A61K 31/40: having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil - A61K 31/445: Non condensed piperidines, e.g. piperocaine - A61P 25/04: Centrally acting analgesics, e.g. opioids - A61P 25/06: Antimigraine agents - 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 present invention relates to a pharmaceutical composition for rectal administration in solid dosage form which comprises a compound acting as a 5HT-1 like receptor agonist in the form of its free base or a physiologically acceptable hard fat base carrier having a hydroxyl value of more than 15 in the method for the treament of a mammal suffering from a susceptible to conditions associated with cephalic pain. ## Claims ### Claim 1 A pharmaceutical composition for rectal administration in solid dosage form which comprises an effective amount of a compound which acts as a 5HT.sub.1 -like receptor agonist in the form of its free base or a physiologically acceptable solvate thereof as active ingredient and a pharmaceutically acceptable hard fat base carrier having a Hydroxyl Value of more than 15. ### Claim 2 (depends on 1) A pharmaceutical composition as claimed in claim 1 wherein the active ingredient is selected from the group consisting of 3-›2-(dimethylamino)ethyl!-N-methyl-1H-indole-5-methanesulphonamide N-methyl-3-(1-methyl-4-piperidinyl)-1H-indole-5-ethanesulphonamide and pharmaceutically acceptable solvates thereof. ### Claim 3 (depends on 1) A pharmaceutical composition as claimed in claim 1 wherein the active ingredient 3-›2-(dimethylamino)ethyl!-N-methyl-1H-indole-5-methanesulphonamide or a pharmaceutically acceptable solvate thereof. ### Claim 4 (depends on 1) A pharmaceutical composition as claimed in claim 1 wherein the active ingredient is N-methyl-3-(1-methyl-4-piperidinyl)-1H-indole-5-ethanesulphonamide or a pharmaceutically acceptable solvate thereof. ### Claim 5 (depends on 1) A pharmaceutical composition as claimed in claim 1 in the form of a suppository. ### Claim 6 (depends on 1) A pharmaceutical composition as claimed in claim 1 wherein the hard fat base has a Hydroxyl Value in the range of 20 to 100. ### Claim 7 (depends on 1) A pharmaceutical composition as claimed in claim 1 which comprises 0.1 to 20% by weight of active ingredient. ### Claim 8 (depends on 1) A pharmaceutical composition as claimed in claim 1 which comprises about 1 to about 200 mg of active ingredient. ### Claim 9 (depends on 8) A pharmaceutical composition as claimed in claim 8 which comprises 5 to 30 mg of active ingredient. ### Claim 10 (depends on 1) A pharmaceutical composition as claimed in claim 1 wherein the active ingredient is micronised. ### Claim 11 A method for the treatment of a mammal, including man, suffering from or susceptible to conditions associated with cephalic pain such as cluster headache, chronic paroxysmal hemicrania, headache associated with vascular disorders, headache associated with substances or their withdrawal (for example drug withdrawal), tension headache and in particular migraine which comprises rectal administration of a pharmaceutical composition comprising a compound which acts as a 5HT.sub.1 -like receptor agonist in the form of its free base or a pharmaceutically acceptable solvate thereof. ### Claim 12 (depends on 11) A method as claimed in claim 11 wherein the 5HT.sub.1 -like receptor agonist is 3-›2-(dimethylamino)ethyl!-N-methyl-1H-indole-5-methanesulphonamide or a pharmaceutically acceptable solvate thereof. ### Claim 13 (depends on 3) A pharmaceutical composition as claimed in claim 3 in the form of a suppository. ### Claim 14 (depends on 3) A pharmaceutical composition as claimed in claim 3 wherein the hard fat base has a Hydroxyl Value in the range of 20 to 100. ### Claim 15 (depends on 5) A pharmaceutical composition as claimed in claim 5 wherein the hard fat base has a Hydroxyl Value in the range of 20 to 100. ### Claim 16 (depends on 3) A pharmaceutical composition as claimed in claim 3 which comprises 0.1 to 20% by weight of active ingredient. ### Claim 17 (depends on 5) A pharmaceutical composition as claimed in claim 5 which comprises 0.1 to 20% by weight of active ingredient. ### Claim 18 (depends on 6) A pharmaceutical composition as claimed in claim 6 which comprises 0.1 to 20% by weight of active ingredient. ### Claim 19 (depends on 3) A pharmaceutical composition as claimed in claim 3 which comprises about 1 to 200 mg of active ingredient. ### Claim 20 (depends on 5) A pharmaceutical composition as claimed in claim 5 which comprises about 1 to 200 mg of active ingredient. ### Claim 21 (depends on 6) A pharmaceutical composition as claimed in claim 6 which comprises about 1 to 200 mg of active ingredient. ### Claim 22 (depends on 7) A pharmaceutical composition as claimed in claim 7 which comprises about 1 to 200 mg of active ingredient. ### Claim 23 (depends on 3) A pharmaceutical composition as claimed in claim 3 which comprises 5 to 30 mg of active ingredient.