Docetaxel injection and preparation method thereof

Abstract

The invention discloses docetaxel injection. The docetaxel injection is prepared from the following components in parts by weight: 1-2 parts of docetaxel, 18-25 parts of a solvent, 20-30 parts of a surfactant, 0.3-0.6 part of a stabilizer, and 40-60 parts of a solubilizer, wherein the solvent is one or more of absolute ethyl alcohol, glycerol and propylene glycol, the surfactant is polyoxyethylenated castor oil, the stabilizer is one or more of citric acid, tartaric acid, fumaric acid and maleic acid, and the solubilizer is polyethylene glycol 300 and / or polyethylene glycol 400. The docetaxel injection provided by the invention is free of hemolysis, good in safety, good in stability, stable in content of active ingredients, and low in contents of related substances and impurities, and can be stored under the condition with the temperature being 20-40 DEG C.

Description

technical field [0001] The invention relates to docetaxel injection and a preparation method thereof, belonging to the field of pharmaceutical preparations. Background technique [0002] Docetaxel (Docetaxel or Docetaxel) is a taxane anticancer drug developed by the French company Rhone-Planck Le'an and has been widely marketed. It is a white or nearly white powder with a molecular formula of C 43 h 53 NO 4 , with a relative molecular mass of 861.9, is a product obtained by semi-synthesis of the extract from the needles of Yew berry. Since docetaxel replaces the benzoic acid group in paclitaxel with t-butoxycarbonyl, its water solubility is slightly greater than that of paclitaxel (the solubility of paclitaxel in water is less than 0.004g / L). Its mechanism of action is to promote tubulin polymerization and inhibit microtubule depolymerization, "freeze" the synthesis of intracellular skeleton, a component of microtubules, resulting in the formation of stable non-functiona...

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Problems solved by technology

[0004] Docetaxel injection is sensitive to temperature. The storage temperature of domestic docetaxel injection is 2-8°C, and the storage temperature of imported docetaxel injection is 2-25°C. The marketed docetaxel injection cannot Store in an environment above 25°C for long-term storage; in addition, the docetaxel injections that have been marketed all use the surfactant Tween 80, which has a hemolytic effect and is likely to cause serious adverse reactions of acute intravascular hemolysis, even It can lead to the death of patients. Tween 80 can interfere with the expression of P-glycoprotein and interact with certain drugs. Therefore, glucocorticoids, such as dexamethasone, should be used before medication

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