Medicine composition containing docetaxel matter and its preparation process

Abstract

The present invention relates to medicine composition containing docetaxel matter suitable for injection and its preparation process. The medicine composition has docetaxel or its salt or hydrate as the active component, and cyclodextrin and amino acid as complex solubilizing agent. The injection of the medicine composition of the present invention has high stability, less toxic side effect and other advantages.

Description

A pharmaceutical composition containing docetaxel and its preparation method technical field The invention relates to a pharmaceutical composition containing docetaxel substances, more specifically an injection pharmaceutical composition with docetaxel or its salt or hydrate as an active ingredient. The invention also relates to a process for the preparation of the composition. Background technique Docetaxel is a known class of compounds with significant anticancer activity, belonging to mitosis inhibitors, which stabilize microtubules by promoting the assembly of microtubule dimers into microtubules and by preventing the process of depolymerization, Block cells in G2 and M phases, thereby inhibiting the mitosis and proliferation of cancer cells. These drugs are effective for advanced breast cancer, non-small cell lung cancer, ovarian cancer, prostate cancer, pancreatic cancer, liver cancer, head and neck cancer, gastric cancer, etc. Because docetaxel is insoluble in wa...

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Problems solved by technology

Many researchers have conducted research on reducing the adverse reactions caused by docetaxel substances in clinical application and their own toxic and side effects. For example, Chinese patent application 02155476.5 discloses the use of hyaluronic acid, glucose or mannitol, ethanol, propylene glycol, Ionic surfactant prepares the injection of docetaxel substance; U.S. Patent 97 / 196,934 discloses the composition of docetaxel substance prepared with dimethylacetamide and polyethylene glycol as a solvent for parenteral administration ;Australian patent 35544 / 93 discloses that the use of unsaturated cyclodextrin and enzyme-modified branched cyclodextrin can moderately increase the solubility of docetaxel substances; Chinese patent ZL98811010.5 uses acetylated cyclodextrin and hydroxypropyl-β -Cyclodextrin and other water-soluble adjuvants to prepare injection preparations of docetaxel substances; The injection preparation of substance, the stability of the injection that obtains improves to some extent, but the content of docetaxel substance declines close to 10% in 6 hours, and because containing adding organic acid and organic acid salt, the pH value of preparation is too high Low (pH value 3-5), easy to produce obvious vascular irritation when used intravenously

Most of the injections of docetaxel substances obtained by the prior art have the defect that the stability is not ideal enough

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