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Submicron docetaxel emulsion for intravenous injection and its preparing process

A technology of docetaxel and submicroemulsion, which is applied in the field of intravenous injection of docetaxel submicroemulsion and its preparation, can solve the problems of easy decomposition of drugs, influence on drug stability, poor water solubility of docetaxel, etc., and achieve the preparation process Simple and easy to use, good organ targeting, and the effect of improving bioavailability

Inactive Publication Date: 2006-11-08
NAT INST OF PHARMA R & D CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
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Problems solved by technology

Due to the poor water solubility of docetaxel, the current clinical use mainly includes freeze-dried powder injection and water injection injection. Before intravenous injection, the preparation needs to be dissolved and diluted with normal saline or 5% glucose injection, which is cumbersome to use and brings great inconvenience to clinical medication. Inconvenient, the existing water injection (40g·L -1 ) uses Tween-80 as a solvent, and is also equipped with a solvent containing 13% ethanol. This kind of injection is extremely inconvenient for clinical use because Tween-80 is prone to adverse reactions such as hemolysis and allergies, and is highly viscous. Therefore, it is necessary to develop new formulations
[0003] In the public document 200510084055.6, a docetaxel fat emulsion is disclosed, which is made by mixing docetaxel with vegetable oil for injection, phospholipid for injection and water for injection to make a fat emulsion. This emulsion can overcome some shortcomings of existing injections. And can supplement nutrition, but it still has some deficiencies: for example, the drug content is low, and its highest content is only 1mg / mL; its oil content is very high, and the oil content is all at 100mg / ml. Lead to the accumulation of fat in tissues and organs, and even affect the immune function of the body; the average particle size of the fat emulsion is about 500nm, which does not have good organ targeting; in addition, the placement emulsion also needs high temperature ( 110-121°C) sterilization, the drug is easy to decompose at this temperature, which affects the stability of the drug

Method used

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  • Submicron docetaxel emulsion for intravenous injection and its preparing process
  • Submicron docetaxel emulsion for intravenous injection and its preparing process

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preparation example Construction

[0045] The preparation method of docetaxel emulsion for intravenous injection of the present invention comprises the following steps:

[0046] Preparation of the oil phase: weigh docetaxel, oil for injection, emulsifier and stabilizer according to the formula, and heat at 20-80°C, preferably 20-60°C, to obtain the oil phase;

[0047] Preparation of the water phase: Weigh the water for injection according to the formula, add an isotonic regulator, and heat to obtain the water phase. The heating temperature should preferably not exceed 80°C;

[0048] Preparation of docetaxel emulsion: mix the oil phase and the water phase at 20-80°C, preferably 30-60°C, and emulsify with shearing or stirring for 3-200 minutes at a speed of 300-20000 rpm to obtain the initial milk;

[0049] The colostrum is further emulsified, and further emulsification can adopt any of these emulsification methods such as high-pressure homogeneous emulsification, mechanical stirring emulsification, ultrasonic e...

Embodiment 1

[0053] Embodiment 1: preparation drug content is the docetaxel intravenous injection submicroemulsion of 0.01% (being 0.1mg / mL)

[0054] Weigh 100 mg of docetaxel, 50 g of soybean oil, 5 g of phospholipid, and 5 g of polyethylene glycol-distearoylphosphatidylethanolamine (PEG-DSPE), heat in a water bath to 55° C., stir and dissolve to obtain an oil phase. Measure 920 ml of water for injection, add 22.5 g of sorbitol and heat to 55°C and stir to dissolve to obtain an aqueous phase. Mix the oil phase and the water phase at 60° C. and emulsify with a stirrer (10,000 rpm) for 10 minutes to mix the oil phase and the water phase evenly. Use sodium phosphate solution (1mol / L) to adjust its pH to 7.5 to obtain colostrum. The colostrum was homogenized and emulsified (pressure 10000psi, temperature 40°C) four times with a micro-jet high-pressure homogenizer, sterilized by filtration through a 0.22μm microporous membrane, subpackaged, and filled with nitrogen to obtain the product docet...

Embodiment 2

[0056] Embodiment 2: preparation content is 0.1% (being 1mg / mL) docetaxel intravenous injection submicroemulsion

[0057] Weigh 1 g of docetaxel, 20 g of evening primrose oil, 15 g of soybean lecithin, and 1 g of tocopherol, heat in a water bath to 55° C., stir and dissolve to obtain an oil phase. Measure 950 ml of water for injection, add 15 g of glycerin and heat to 45°C and stir to dissolve to obtain an aqueous phase. Mix the oil phase and the water phase at 45° C., and emulsify with a stirrer (15,000 rpm) for 10 minutes, so that the oil phase and the water phase are evenly mixed. Use phosphoric acid solution (1mol / L) to adjust its pH to 5.5 to obtain colostrum. The colostrum was emulsified with a colloid mill at a rotating speed of 25,000 rpm and the emulsification time was 3 minutes, filtered through a 0.22 μm microporous membrane to sterilize, subpackaged, and filled with nitrogen to obtain 1000 ml of the product docetaxel submicroemulsion.

[0058] The emulsion was te...

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Abstract

The present invention provides submicron docetaxel emulsion for intravenous injection and its preparation process, and docetaxel is prepared into submicron docetaxel emulsion for intravenous injection with proper emulsifier and other pharmaceutical supplementary material. Docetaxel, injection oil, emulsifier, stabilizer, injection water and isoosmotic regulator are stirred separately to obtain both oil phase and water phase, the oil phase and the water phase are mixed and emulsified to obtain initial emulsion, and the initial emulsion is further emulsified and high pressure homogenized to prepare the required docetaxel emulsion for intravenous injection. The submicron docetaxel emulsion has stable property, long preservation period, convenient use and simple preparation process, and is suitable for industrial production.

Description

Field of invention: [0001] The invention relates to the technical field of medicine, in particular to an intravenous injection docetaxel submicroemulsion prepared by preparing the anticancer drug docetaxel with appropriate pharmaceutical auxiliary materials and a preparation method thereof. Background of the invention: [0002] Docetaxel (docetaxel) is a semi-synthetic new anti-tumor drug. It is an inactive precursor extracted from the needles of the European yew tree. The active drug obtained after chemical treatment can effectively inhibit the replication of tumor cells. , acting on cells in the G2~M growth phase. Clinical studies have shown that docetaxel has good anticancer activity against various tumor diseases, and it is used for the treatment of breast cancer, non-small cell lung cancer, pancreatic cancer, soft tissue sarcoma, head and neck cancer, gastric cancer, ovarian cancer and prostate cancer. Efficacy. Due to the poor water solubility of docetaxel, the curre...

Claims

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Application Information

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IPC IPC(8): A61K9/107A61K31/337A61K47/30A61P35/00
Inventor 郑少辉王明新
Owner NAT INST OF PHARMA R & D CO LTD
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