A kind of Cabazitaxel injection and preparation method thereof

Abstract

The invention provides a Cabazitaxel injection, comprising the following components by mass: 10 parts of Cabazitaxel, 200-270 parts of polysorbate 80, 400-500 parts of polyethylene glycol and distilled to 1000 parts of ethanol share. The product has good stability, is easy to filter and fill, and is convenient to use in clinical practice.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a cabazitaxel injection. Background technique [0002] Cabazitaxel is a second-line chemotherapy drug for the treatment of prostate cancer recommended by the NCCN guidelines in the United States, and it is a chemical semi-synthetic taxane-like small molecule compound. The currently marketed Cabazitaxel injection is a liquid injection. According to the FDA Orange Book, the original manufacturer is Sanofi-aventis U.S. LLC. This product is packaged in combination, one bottle is 60mg / 1.5mL cabazitaxel-polysorbate 80 solution; one bottle is diluent, 13% ethanol-water. Before clinical use, dilute the cabazitaxel solution with 13% ethanol-water. After dilution, the drug solution needs to be diluted in the second step within 30 minutes, otherwise precipitation will occur. There are the following defects: [0003] 1) The solvent polysorbate 80 is a viscous liquid. If the raw material ...

AI Technical Summary

Problems solved by technology

[0003] 1) The solvent polysorbate 80 is a viscous liquid. If the raw material of cabazitaxel is directly added to polysorbate 80, the raw material is not easy to disperse and dissolve, and the filtration and filling process is difficult, which will easily cause loss of raw material

[0004] 2) Two-step dilution is required before clinical use, the use steps are cumbersome, and there is a time limit for medication, which poses a safety hazard

However, the product prescriptions involved in the above-mentioned patents all introduce H + The stabilizer citric acid, which promotes the risk of ring-opening degradation of the ester group and epoxy group in the cabazitaxel molecule, and the product formulation design itself has a stability risk; the application of freeze-drying technology, the product production cycle is long and the cost is high

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