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Taxol composition for injection and preparation method thereof

A technology for paclitaxel and injection, applied in the field of paclitaxel composition for injection and preparation thereof, can solve the problems of drug safety risk, inability to withstand high pressure sterilization, unfavorable industrialization, etc., and achieves reduction of drug risk and low lipid content. , the effect of high drug loading

Active Publication Date: 2016-05-04
慧禹康成(浙江)医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0013] As mentioned above, the existing paclitaxel preparations for injection have the following problems: poor stability (such as easy delamination, low encapsulation efficiency, easy leakage, inability to withstand high-pressure sterilization, etc.), low drug loading, and poor drug safety. There are risks (such as the safety of polysorbate 80, the nephrotoxicity of cyclodextrin, etc.), in addition, the production cost is high, which is not conducive to industrialization

Method used

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  • Taxol composition for injection and preparation method thereof
  • Taxol composition for injection and preparation method thereof
  • Taxol composition for injection and preparation method thereof

Examples

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preparation example Construction

[0075] [Preparation of paclitaxel composition for injection]

[0076] The invention provides a preparation method of a paclitaxel composition for injection, which is characterized in that, when preparing an oil phase, paclitaxel, an emulsifier and anhydrous ethanol are mixed and stirred until clear, then an injection oil and a stabilizer are added, and further stirring When it is clear, the ethanol is evaporated in vacuo to obtain an oil phase.

[0077] Specifically, when preparing the paclitaxel composition for injection of the present invention, the amount of anhydrous ethanol used is far lower than the prescription amount recorded in the prior art, and it is finally removed under vacuum conditions. Thereby, the risk of ethanol irritation can be reduced, and the drug safety is better compared with the case of using other organic solvents such as acetone.

[0078] In the following, the case where the paclitaxel composition for injection according to the present invention is ...

Embodiment 1

[0100] Example 1 (freeze-dried microemulsion of paclitaxel for injection)

[0101] prescription

[0102]

[0103] Preparation:

[0104] (1) Oil phase: at 40-70°C, mix paclitaxel, egg yolk lecithin, soybean lecithin and absolute ethanol and stir until clarification, then add vitamin E and oleic acid, further stir until clarification, and evaporate ethanol in vacuum , the oil phase is obtained;

[0105] (2) Water phase: add arginine and sucrose to water for injection, stir until completely dissolved, and filter with 0.22 μm microporous membrane to obtain water phase;

[0106] (3) Colostrum: First preheat the water phase and the oil phase to 50-70°C, then use a high-speed disperser to slowly add the water phase to the oil phase under shear stirring at 5000-20,000 rpm, and after the addition is complete , continue shearing and stirring at 10000rpm for 30 minutes to obtain colostrum;

[0107] (4) Final milk: Cool the colostrum to room temperature, then transfer it to a high-pr...

Embodiment 2

[0132] Example 2 (paclitaxel microemulsion for injection)

[0133] prescription

[0134]

[0135] Preparation:

[0136] (1) Oil phase: at 40-70°C, mix paclitaxel, egg yolk lecithin and absolute ethanol and stir until clear, then add vitamin E, dl-α-tocopherol and oleic acid, and further stir until clear, The ethanol was evaporated in a vacuum to obtain an oil phase;

[0137] (2) Water phase: add lysine and sucrose to water for injection, stir until completely dissolved, and filter with a 0.22 μm microporous membrane to obtain the water phase;

[0138] (3) Colostrum: first preheat the water phase and the oil phase to 50-70°C, then use a high-speed disperser to slowly add the water phase to the oil phase under shear stirring at 5000-20,000 rpm, and after complete addition, Continue stirring at 8000rpm for 20 minutes to obtain colostrum;

[0139] (4) Final milk: Cool the colostrum to room temperature, then transfer the colostrum to a high-pressure homogenizer, and homogeni...

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Abstract

The invention provides a taxol composition for injection, which comprises taxol, oil for injection, an emulsifying agent and a stabilizing agent, wherein the oil for injection is selected from at least one of soybean oil, olive oil, coix seed oil, medium chain triglyceride as well as vitamin E and derivatives thereof, and the emulsifying agent is selected from at least one of egg yolk lecithin, soybean lecithin and synthetic lipid as well as amino acid. The invention also provides a preparation method of the taxol composition for injection, wherein an oil phase is prepared by the following steps: mixing and stirring taxol, the emulsifying agent and absolute ethyl alcohol until the solution is clear, then adding the oil for injection and the stabilizing agent, further stirring until the solution is clear, and volatilizing ethyl alcohol in vacuum so as to obtain the oil phase. The taxol composition for injection, provided by the invention, is high in drug loading capacity, low in lipid content and good in stability and is capable of reducing the medication risk of taxol for injection and increasing the compliance of patients.

Description

technical field [0001] The present invention relates to a paclitaxel composition for injection and a preparation method thereof. technical background [0002] Paclitaxel is a natural anticancer drug developed by Bristol-Myers Squibb in the late 20th century. Specifically, paclitaxel can promote the assembly of tubulin into microtubules, but inhibit the depolymerization of microtubules and stabilize the microtubules, which leads to the abnormal arrangement of microtubule bundles, which makes the spinning pituitary lose its normal function and leads to cell death. , Ovarian cancer has outstanding curative effect, and it is mainly used in the first-line and second-line treatment of ovarian cancer, breast cancer and non-small cell lung cancer. [0003] Paclitaxel is not bioavailable orally because it is hardly soluble in water and has poor permeability to the gastrointestinal barrier. At present, the paclitaxel preparations used in clinics are all intravenous injections. prep...

Claims

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Application Information

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IPC IPC(8): A61K9/107A61K31/337A61K47/14A61K47/18A61K47/22A61K47/24A61K47/44A61P35/00
CPCA61K9/0019A61K9/1075A61K31/337A61K47/14A61K47/183A61K47/22A61K47/24A61K47/44
Inventor 游剑姜新东李青坡
Owner 慧禹康成(浙江)医药科技有限公司
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