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Docetaxel medical composition for injection and preparation method thereof

A technology of docetaxel and composition, which is applied in the direction of drug combination, pharmaceutical formulation, drug delivery, etc., can solve problems such as allergic reactions, achieve the effects of improving solubility, solving production difficulties, and avoiding allergic reactions

Active Publication Date: 2013-03-20
HAINAN SIMCERE PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although the formula can encapsulate docetaxel, due to the use of a certain amount of surfactants such as Tween and polyoxyethylene castor oil, there are still unavoidable toxic and side effects such as allergic reactions

Method used

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  • Docetaxel medical composition for injection and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] Dissolve 500 mg of docetaxel, 10 g of soybean lecithin (purity > 95%), 20 mg of a-tocopherol, and 100 mg of glycerol in 50 ml of ethanol, pass the resulting transparent solution through a 0.22 μm microporous filter membrane, and fill it with sterile nitrogen into 20 mg or 80mg / bottle, stopper and cap. Add a tube of the composition solution to 20 times the volume of 5% glucose injection for hydration, shake evenly, and measure the average particle diameter of the obtained particles to be 279nm, and the particle diameter distribution range is 122-825nm. The encapsulation efficiency of the obtained particles was measured by the Sephadex column chromatography method, and it was 92%.

Embodiment 2

[0041] Docetaxel 500mg, soybean lecithin (purity > 95%) 8g, dipalmitoylphosphatidylglycerol 800mg, cholesterol 1g, glycerol 500mg are dissolved in 15ml ethanol, the transparent solution of gained is passed through 0.22 μm microporous membrane, sterile filled Nitrogen packaged in 20mg or 80mg / bottle, stoppered and capped. Take a tube of the composition solution and add 15 times the volume of water for injection to hydrate, shake evenly, and the average particle diameter of the obtained particles is measured to be 445nm, and the particle diameter distribution range is 214-914nm. The encapsulation efficiency of the obtained particles was measured by the Sephadex column chromatography method, and it was 88%.

Embodiment 3

[0043] Dissolve 500 mg of docetaxel, 20 g of egg yolk lecithin (purity > 95%), and 100 g of soybean phosphatidylglycerol in 40 ml of tert-butanol, pass the resulting transparent solution through a 0.22 μm microporous membrane, and pack 20 mg aseptically filled with nitrogen Or 80mg / support, stopper and cap. Take a tube of the composition solution and add 80 times the volume of physiological saline to hydrate, shake evenly, and the average particle diameter of the obtained particles is measured to be 420nm, and the particle diameter distribution range is 198-824nm. The encapsulation efficiency of the obtained particles was measured by the Sephadex column chromatography method, and it was 92%.

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Abstract

The invention discloses a docetaxel pharmaceutical combination used for injection and a preparation method thereof. The combination is composed of docetaxel, phospholipid and organic solvent. When the docetaxel pharmaceutical combination is used for clinical treatment, hydration media with proper amount is directly added and shaken evenly, so as to disperse sub-particle suspension for medicine delivery. The docetaxel pharmaceutical combination has the advantages of simple preparation process, good industrialization production feasibility, greatly improving the solubility of medicine in water, good stability and reducing the allergic reaction caused by tween and improving the compliance of patients.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and relates to a composition for injection containing an insoluble anticancer drug docetaxel and a preparation method thereof. Background technique [0002] Docetaxel is a precursor extracted from the needles of the berry yew, and then semi-synthesized. The benzoic acid group in paclitaxel is replaced by t-butoxycarbonyl, so its water solubility is slightly greater than that of paclitaxel (paclitaxel in water Solubility<0.004g·L -1 ). Its anti-cancer mechanism is to stimulate the polymerization of cathelicidin, promote the assembly of microtubule dimers into microtubules, and cause cell proliferation to stop at the stage of mitotic quiescence (G2 / M). Docetaxel is effective for advanced breast cancer, non-small cell lung cancer, ovarian cancer, pancreatic cancer, liver cancer, head and neck tumors and other tumors. [0003] Docetaxel has poor water solubility and good fat solubilit...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/08A61K31/337A61K47/24A61P35/00
Inventor 王青松林巧平张翠霞沈洁刘春晖许向阳
Owner HAINAN SIMCERE PHARMA CO LTD