Liquid formulation of cabazitaxel
Inventors
PATEL, Hiren Pravinbhai • PATEL, Haresh Ishwarbhai • CHUDASAMA, Arpan Suresh • PATEL, Neha Manubhai • GONDALIYA, Deepak Pragjibhai • Gurjar, Mukund Keshav • Mehta, Samit Satish
Assignees
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Publication Number
US-10278946-B2
Publication Date
2019-05-07
Expiration Date
Abstract
The present invention relates to a stable liquid formulation of cabazitaxel. The formulation comprises cabazitaxel and at least one solubilizer. Typically, formulations are in the form of ready-to-use solutions or concentrates.
Core Innovation
The invention relates to stable liquid cabazitaxel formulations comprising cabazitaxel or a pharmaceutically acceptable salt thereof. The formulations include a mixture of macrogol 15 hydroxy stearate and polyethylene glycol with a molecular weight range from 200 to 600, together with ethanol and citric acid. The disclosure provides single-vial injectable concentrates that are ready for only one dilution prior to IV infusion and are characterized by stability based on impurity content over time.
The invention further discloses optional nanodispersion forms in which cabazitaxel is present as nanoparticles in a water-miscible vehicle. The nanoparticles have a mean size less than 500 nm, preferably less than 300 nm. This nanodispersion aspect is presented alongside the stable liquid formulation framework using solubilizers and stabilizers/antioxidants.
Claims Coverage
The document provides two independent claims that cover a pharmaceutical composition containing cabazitaxel formulated with a specific excipient system, and a single-vial injection solution with quantitative cabazitaxel concentration limits and the same defined excipient system. Across these claims, four main inventive features are combined.
Cabazitaxel with a defined excipient system
A pharmaceutical composition consisting of cabazitaxel or a pharmaceutically acceptable salt thereof, a mixture of macrogol 15 hydroxy stearate and polyethylene glycol with a molecular weight range from 200 to 600, ethanol, and citric acid.
Single-vial injection concentration and defined PEG system
A single-vial injection solution consisting of about 10 mg/mL to about 100 mg/mL of cabazitaxel or a pharmaceutically acceptable salt thereof, macrogol 15 hydroxy stearate, polyethylene glycol with a molecular weight range from 200 to 600, ethanol, and citric acid.
The claim coverage centers on stable liquid cabazitaxel formulations in which cabazitaxel or a pharmaceutically acceptable salt thereof is combined with macrogol 15 hydroxy stearate and polyethylene glycol (MW 200 to 600) plus ethanol and citric acid, with the single-vial injection solution defining cabazitaxel concentration limits of about 10 mg/mL to about 100 mg/mL.
Stated Advantages
Stable liquid cabazitaxel formulations are provided with impurity content stability over time at 40°C/75% RH and at 25°C/60% RH.
Single-vial injectable concentrates are provided that are ready for only one dilution prior to IV infusion.
Documented Applications
Parenteral administration as IV infusion following only one dilution of a single-vial injectable concentrate.
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