Paclitaxel composition for injection and preparation method thereof

Abstract

The invention provides a paclitaxel composition for injection. The composition comprises the following components in percentage by weight: 0.200-1.087% of paclitaxel, 95.000-99.200% of polyoxyethylenated castor oil and ethanol as well as 0.200-1.500% of organic acid. The paclitaxel composition for injection, provided by the invention, can be directly administrated after being diluted by an infusion solution. By using the paclitaxel composition for injection, provided by the invention, the damage caused by terminal sterilization of the product to the main component is avoided because a sterile production process is adopted in the preparation process; meanwhile, the sterile level of the product is more preferably guaranteed because an polyoxyethylenated castor oil sterilizing process is additionally increased in the process. Compared with the prior art, the paclitaxel composition for injection, provided by the invention, has the advantages of reducing the content of the preparation related substances, improving the product stability, reducing the occurring rate of the adverse reaction and improving the safety in clinical use.

Description

technical field [0001] The invention relates to the field of medicine preparation, in particular to the field of medicine preparation of compositions. Background technique [0002] The chemical name of paclitaxel is: (2S, 5R, 7S, 10R, 13S)-10,20-bis(acetoxy)-2-benzoyloxy-1,7-dihydroxy-9-oxo-5, 20-Epoxytaxane-11-en-13-yl(3S)-3-benzamido-3-phenyl-D-lactate. [0003] Its structural formula is: [0004] [0005] Molecular formula: C 47 h 51 NO 14 [0006] Molecular weight: 853.92 [0007] Paclitaxel is a new type of anti-microtubule drug, which can act on the microtubule / tubulin system of cells, promote the assembly of tubulin into microtubules, but inhibit the depolymerization of microtubules, resulting in abnormal arrangement of microtubule bundles and the formation of stars. The spindle loses its normal function, leading to the death of microcells. The drug also induces the formation of nonfunctional microtubules in the absence of guanosine triphosphate (GTP) a...

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Problems solved by technology

[0011] Experimental studies have found that paclitaxel will be degraded to varying degrees under conditions of light, alkali, acid, and high temperature, especially in high alkalinity and high heat, which will increase the content of related substances. Therefore, after the injection preparation and filling are completed The advanced terminal sterilization process (generally adopting 115°C, 30 minutes) may affect the product quality, increase the degradation products (related substances) of the main drug, and bring the risk of clinical use

[0012] A paclitaxel injectable composition is mentioned in CN1248680C. In this technology, the quality evaluation and stability expression of the paclitaxel injectable composition are mainly described from the aspects of paclitaxel content, particle size after dilution, and product toxicity. There is no detailed description of degradation products (related substances), clinical compatibility stability, and the preparation process of the injectable composition, and the clinical allergic reaction of the paclitaxel injectable composition, which is the most important adverse reaction, has an advantage in this composition not reflected

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