# US 10,500,185 B2 · Stabilized cabazitaxel formulations > Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt - Number: US 10,500,185 B2 - Document ID: US10500185B2 - Status: Granted - Kind: B2 - Application number: 15/824,557 - Filed: 2017-11-28 - Published: 2018-03-29 - Granted: 2019-12-10 - Earliest claimed: 2015-11-03 - Assignees: Cipla Limited - Applicants: Cipla Limited - Inventors: Geena Malhotra; Sarabjit Singh; Ravichandra Bhadravathi Vedamurthy; Anirban Mallik Thakur; Dhiraj Abhyankar - Web page: https://patentgrep.com/patent/US10500185B2 ## CPC - A61K 31/337: having four-membered rings, e.g. taxol - A61K 9/0019: {Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner (non-active ingredients are additionally classified in A61K47/00)} - A61K 47/10: Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers - A61K 47/12: Carboxylic acids; Salts or anhydrides thereof - A61K 47/14: Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters - A61K 47/42: Proteins; Polypeptides; Degradation products thereof; Derivatives thereof, e.g. albumin, gelatin or zein (oligopeptides having up to five amino acids {A61K47/183}; polyamino acids A61K47/34) - 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 Disclosed herein are improved formulations for the cabazitaxel. The formulations exhibit increased storage stability relative to other formulations, and are simpler for health care providers to prepare and administer to patients. ## Claims ### Claim 1 A sterilized pharmaceutical composition, comprising a compound having the formula: or a pharmaceutically acceptable salt thereof, in a concentration of about 5 mg/ml to about 200 mg/ml, and at least one solubilizer wherein: a) the solubilizer comprises a compound of the formula wherein x is an integer from 1-20; y1 is an integer from 2-20; z1 is an integer from 1-15; and Z1 is selected from hydrogen or the group OR, in which R is selected from hydrogen and a group having the formula: wherein y2 is an integer from 2-20; z2 is an integer from 1-15; and Z2 is selected from hydrogen or hydroxyl, or b) the solubilizer comprises compound of the formula wherein x2 is an integer from 1-20; wherein y3 is an integer from 1-20; z3 is an integer from 0-15; Z3 is selected from hydroxyl and hydrogen, and Z4 is selected from hydroxyl and the group having the formula: wherein y4 is an integer from 1-20; z4 is an integer from 0-15; and Z5 is selected from hydrogen or hydroxyl, wherein the composition is a solution and does not include Cremophor EL. ### Claim 2 (depends on 1) The pharmaceutical composition according to claim 1, wherein the solubilizer is present in an amount from 5-50% by weight of the total composition. ### Claim 3 (depends on 1) The pharmaceutical composition according to claim 1, wherein the solubilizer comprises a macrogol 18-hydroxystearate. ### Claim 4 (depends on 1) The pharmaceutical composition according to claim 1, wherein the solubilizer comprises a caprylocaproyl polyoxylglyceride. ### Claim 5 (depends on 1) The pharmaceutical composition according to claim 1, wherein the composition comprises a surfactant. ### Claim 6 (depends on 5) The pharmaceutical composition according to claim 5, wherein the surfactant is present in an amount from 5-45% by weight of the total composition. ### Claim 7 (depends on 5) The pharmaceutical composition according to claim 5, wherein the surfactant comprises a polyethylene oxide. ### Claim 8 (depends on 5) The pharmaceutical composition according to claim 5, wherein the surfactant comprises PEG 400. ### Claim 9 (depends on 1) The pharmaceutical composition according to claim 1, wherein the formulation further comprises at least one alcohol, at least one acid, or at least one solvent. ### Claim 10 (depends on 9) The pharmaceutical composition according to claim 9, wherein the alcohol comprises ethanol, benzyl alcohol, tertiary-butyl alcohol, isopropyl alcohol, or a mixture thereof. ### Claim 11 (depends on 9) The pharmaceutical composition according to claim 9, wherein the alcohol comprises ethanol. ### Claim 12 (depends on 9) The pharmaceutical composition according to claim 9, wherein the acid comprises citric acid, tartaric acid, acetic acid and mixtures thereof. ### Claim 13 (depends on 12) The pharmaceutical composition according to claim 12, wherein the acid is present in an amount from about 0.1-1.0% of the total weight of the composition. ### Claim 14 (depends on 12) The pharmaceutical composition according to claim 12, wherein the acid comprises citric acid. ### Claim 15 (depends on 9) The pharmaceutical composition according to claim 9, wherein the solvent comprises diethylene glycol monoethyl ether, dimethylacetamide, dimethylsulfoxide, propylene glycol and glycofurol. ### Claim 16 (depends on 9) The pharmaceutical composition according to claim 9, wherein the solvent is present in an amount of about 0.1-10% of the total weight of the composition. ### Claim 17 (depends on 1) The pharmaceutical composition according to claim 1, further comprising albumin and water. ### Claim 18 (depends on 17) The pharmaceutical composition according to claim 17, wherein the albumin concentration is at least 10% by weight.