# US 2024/0197751 A1 · Pharmaceutical composition and use thereof > Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt - Number: US 2024/0197751 A1 - Document ID: US20240197751A1 - Status: Published application - Kind: A1 - Application number: 18/586,055 - Filed: 2024-02-23 - Published: 2024-06-20 - Earliest claimed: 2020-06-26 - Inventors: Usso Barnas - Web page: https://patentgrep.com/patent/US20240197751A1 ## CPC - A61K 31/5513: 1,4-Benzodiazepines, e.g. diazepam {or clozapine} - A61K 31/135: having aromatic rings {, e.g. ketamine, nortriptyline (methadone A61K31/137)} - A61K 31/167: having the nitrogen of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol - A61K 31/196: the amino group being directly attached to a ring, e.g. anthranilic acid, mefenamic acid, diclofenac, chlorambucil - A61K 31/197: the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid or pantothenic acid (carnitine A61K31/205) - A61K 31/4415: Pyridoxine, i.e. Vitamin B6 (pyridoxal phosphate A61K31/675) - A61K 31/455: Nicotinic acids, e.g. niacin; Derivatives thereof, e.g. esters, amides - A61K 31/51: Thiamines, e.g. vitamin B1 - A61K 31/519: ortho- or peri-condensed with heterocyclic rings - A61K 31/525: Isoalloxazines, e.g. riboflavins, vitamin B2 - A61K 31/573: substituted in position 21, e.g. cortisone, dexamethasone, prednisone or aldosterone - A61K 31/714: Cobalamins, e.g. cyanocobalamin, i.e. vitamin B12 - 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 The present invention discloses a pharmaceutical composition, wherein the pharmaceutical composition is an injectable or infusable pharmaceutical composition, the pharmaceutical composition comprising: a) a pharmaceutically acceptable solvent, b) a first compound comprising diclofenac or a pharmaceutically acceptable salt or solvate thereof, c) a second compound comprising metamizole or tramadol or a pharmaceutically acceptable salt or solvate thereof, and d) a third compound selected as at least one benzodiazepine or a pharmaceutically acceptable salt or solvate thereof, the pharmaceutical composition further comprising a cortisone derivative or a pharmaceutically acceptable salt or solvate thereof. ## Claims ### Claim 1 A pharmaceutical composition, wherein the pharmaceutical composition is an injectable or infusable pharmaceutical composition, the pharmaceutical composition comprising: a) a pharmaceutically acceptable solvent, b) a first compound comprising diclofenac or a pharmaceutically acceptable salt or solvate thereof, c) a second compound comprising metamizole or tramadol or a pharmaceutically acceptable salt or solvate thereof, and d) a third compound selected as at least one benzodiazepine or a pharmaceutically acceptable salt or solvate thereof, the pharmaceutical composition further comprising a cortisone derivative or a pharmaceutically acceptable salt or solvate thereof. ### Claim 2 (depends on 1) The pharmaceutical composition according to claim 1, wherein the at least one benzodiazepine or pharmaceutically acceptable salt or solvate thereof comprises at least one of diazepam, delorazepam and chlonazepam or a pharmaceutically acceptable salt or solvate thereof. ### Claim 3 (depends on 1) The pharmaceutical composition according to claim 1, wherein the third compound comprises from 0.00001 wt.-% to 0.00004 wt.-% of the least one benzodiazepine or pharmaceutically acceptable salt or solvate thereof, preferably from 0.000016 wt.-% to 0.00003 wt.-%, more preferably from 0.000016 wt.-% to 0.000025 wt.-%, and most preferably 0.00002 wt.-%. ### Claim 4 (depends on 1) The pharmaceutical composition according to claim 1, wherein the pharmaceutical composition comprises from 0.00012 wt.-% to 0.0012 wt.-% of diclofenac or a pharmaceutically acceptable salt or solvate thereof, preferably from 0.0002 wt.-% to 0.008 wt.-%, and most preferably 0.0003 wt.-% or 0.0006 wt.-%. ### Claim 5 (depends on 1) The pharmaceutical composition according to claim 1, wherein the pharmaceutical composition further comprising paracetamol or a pharmaceutically acceptable salt or solvate thereof, preferably from 0.001 wt.-% to 0.008 wt.-% of paracetamol or a pharmaceutically acceptable salt or solvate thereof, more preferably from 0.0025 wt.-% to 0.008 wt.-%, and most preferably 0.004 wt.-% or 0.008 wt.-%. ### Claim 6 (depends on 1) The pharmaceutical composition according to claim 1, wherein the pharmaceutical composition comprises from 0.002 wt.-% to 0.01 wt.-% of metamizole or a pharmaceutically acceptable salt or solvate thereof, preferably from 0.003 wt.-% to 0.007 wt.-%, and most preferably 0.005 wt.-%. ### Claim 7 (depends on 1) The pharmaceutical composition according to claim 1, wherein the pharmaceutical composition comprises from 0.0002 wt.-% to 0.0008 wt.-% of tramadol or a pharmaceutically acceptable salt or solvate thereof, preferably from 0.0003 wt.-% to 0.0006 wt.-%, and most preferably 0.0004 wt.-%. ### Claim 8 (depends on 1) The pharmaceutical composition according to claim 1, the pharmaceutical composition further comprising a vitamin B additive composition, wherein the vitamin B additive composition preferably comprises at least one of thiamine, riboflavin, nicotinamide, cobalamin, dexapanthenol and pyridoxin or a pharmaceutically acceptable salt or solvate thereof. ### Claim 9 (depends on 1) The pharmaceutical composition according to claim 1, wherein the cortisone derivative or pharmaceutically acceptable salt or solvate thereof comprises dexamethasone, betamethasone, methylprednisolone, prednisolone, triamcinolone acetonide or a pharmaceutically acceptable salt or solvate thereof. ### Claim 10 A pharmaceutical composition, wherein the pharmaceutical composition is an injectable or infusable pharmaceutical composition, the pharmaceutical composition comprising: a) a pharmaceutically acceptable solvent, b) a first compound comprising diclofenac and lornoxicam, or a pharmaceutically acceptable salt or solvate thereof, c) a second compound comprising metamizole or tramadol or a pharmaceutically acceptable salt or solvate thereof, and d) a third compound selected as at least one benzodiazepine or a pharmaceutically acceptable salt or solvate thereof, the pharmaceutical composition further comprising a cortisone derivative or a pharmaceutically acceptable salt or solvate thereof. ### Claim 11 (depends on 10) The pharmaceutical composition according to claim 10, wherein the at least one benzodiazepine or pharmaceutically acceptable salt or solvate thereof comprises at least one of diazepam, delorazepam and chlonazepam or a pharmaceutically acceptable salt or solvate thereof. ### Claim 12 (depends on 10) The pharmaceutical composition according to claim 10, wherein the third compound comprises from 0.00001 wt.-% to 0.00004 wt.-% of the least one benzodiazepine or pharmaceutically acceptable salt or solvate thereof, preferably from 0.000016 wt.-% to 0.00003 wt.-%, more preferably from 0.000016 wt.-% to 0.000025 wt.-%, and most preferably 0.00002 wt.-%. ### Claim 13 (depends on 10) The pharmaceutical composition according to claim 10, wherein the pharmaceutical composition comprises from 0.00012 wt.-% to 0.0012 wt.-% of diclofenac or a pharmaceutically acceptable salt or solvate thereof, preferably from 0.0002 wt.-% to 0.008 wt.-%, and most preferably 0.0003 wt.-% or 0.0006 wt.-%. ### Claim 14 (depends on 10) The pharmaceutical composition according to claim 10, wherein the pharmaceutical composition comprises from 0.000008 wt.-% to 0.000128 wt.-% of lornoxicam or a pharmaceutically acceptable salt or solvate thereof, preferably from 0.000032 wt.-% to 0.000096 wt.-%, and most preferably 0.000032 wt.-% or 0.000064 wt.-%. ### Claim 15 (depends on 10) The pharmaceutical composition according to claim 10, wherein the pharmaceutical composition further comprising paracetamol or a pharmaceutically acceptable salt or solvate thereof, preferably from 0.001 wt.-% to 0.008 wt.-% of paracetamol or a pharmaceutically acceptable salt or solvate thereof, more preferably from 0.0025 wt.-% to 0.008 wt.-%, and most preferably 0.004 wt.-% or 0.008 wt.-%. ### Claim 16 (depends on 10) The pharmaceutical composition according to claim 10, wherein the pharmaceutical composition comprises from 0.002 wt.-% to 0.01 wt.-% of metamizole or a pharmaceutically acceptable salt or solvate thereof, preferably from 0.003 wt.-% to 0.007 wt.-%, and most preferably 0.005 wt.-%. ### Claim 17 (depends on 10) The pharmaceutical composition according to claim 10, wherein the pharmaceutical composition comprises from 0.0002 wt.-% to 0.0008 wt.-% of tramadol or a pharmaceutically acceptable salt or solvate thereof, preferably from 0.0003 wt.-% to 0.0006 wt.-%, and most preferably 0.0004 wt.-%. ### Claim 18 (depends on 10) The pharmaceutical composition according to claim 10, the pharmaceutical composition further comprising a vitamin B additive composition, wherein the vitamin B additive composition preferably comprises at least one of thiamine, riboflavin, nicotinamide, cobalamin, dexapanthenol and pyridoxin or a pharmaceutically acceptable salt or solvate thereof. ### Claim 19 (depends on 10) The pharmaceutical composition according to claim 10, wherein the cortisone derivative or pharmaceutically acceptable salt or solvate thereof comprises dexamethasone, betamethasone, methylprednisolone, prednisolone, triamcinolone acetonide or a pharmaceutically acceptable salt or solvate thereof. ### Claim 20 A pharmaceutical composition for use in the preemptive or palliative treatment of pain in a mammal, preferably in an human, wherein preferably pain is selected from the group consisting of chronic pain, inflammatory pain, neuropathic pain, acute pain, surgical pain, cancer-related pain, disc prolapse-related pain, low-back pain, neck ache, back pain, rheumatic pain, tension-type pain, tension-type headache, migraine pain, radicular pain, tooth pain, joint pain, and pain of the locomotor apparatus, wherein the pharmaceutical composition is administered to the mammal, preferably human, until a visual analog scale (VAS) rating of pain of 3 or less is reached, and wherein the pharmaceutical composition is an injectable or infusable pharmaceutical composition, the pharmaceutical composition comprising: a) a pharmaceutically acceptable solvent, b) a first compound comprising diclofenac or a pharmaceutically acceptable salt or solvate thereof, c) a second compound comprising metamizole or tramadol or a pharmaceutically acceptable salt or solvate thereof, and d) a third compound selected as at least one benzodiazepine or a pharmaceutically acceptable salt or solvate thereof. ### Claim 21 A method of preparing a pharmaceutical composition, comprising admixing a therapeutically effective amount of a first, second and third compound or a pharmaceutically acceptable salt or solvate thereof with a pharmaceutically acceptable solvent and with a cortisone derivative or a pharmaceutically acceptable salt or solvate thereof, wherein the first compound comprises diclofenac or a pharmaceutically acceptable salt or solvate thereof, wherein the second compound comprises metamizole or tramadol or a pharmaceutically acceptable salt or solvate thereof, and wherein the third compound is selected as at least one benzodiazepine or a pharmaceutically acceptable salt or solvate thereof.