Paclitaxel composition for injection and preparation method thereof

A technology for paclitaxel and injection, which is applied in the field of paclitaxel composition for injection and its preparation, which can solve the problems of inability to withstand high pressure sterilization, risk of drug safety, high production cost, etc., and achieve reduced drug risk, low lipid content, The effect of high encapsulation rate

Active Publication Date: 2017-10-20
HUIYU HEALTH HANGZHOU PHARM TECH CO LTD
View PDF5 Cites 0 Cited by
  • 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

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Paclitaxel composition for injection and preparation method thereof
  • Paclitaxel composition for injection and preparation method thereof
  • Paclitaxel composition for injection and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

preparation example Construction

[0075] [Preparation of paclitaxel composition for injection]

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

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

[0078] Hereinafter, the case where the paclitaxel composition for injection of the present invention is a paclitaxel microemul...

Embodiment 1

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

[0101] prescription

[0102]

[0103] Preparation:

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

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

[0106] (3) Colostrum: firstly preheat the hot 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 shearing and stirring at 5000 to 20000 rpm. , Continuously 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-pressure homogenizer, and homoge...

Embodiment 2

[0132] Example 2 (Paclitaxel Microemulsion for Injection)

[0133] prescription

[0134]

[0135] Preparation:

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

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

[0138] (3) Colostrum: first preheat the hot water phase and the oil phase to 50-70°C, then slowly add the water phase to the oil phase using a high-speed disperser under shearing and stirring at 5000 to 20000 rpm. Stir continuously 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 homogenize 6 times at 25~45℃ under 1000bar co...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more

PUM

PropertyMeasurementUnit
particle sizeaaaaaaaaaa
particle sizeaaaaaaaaaa
particle diameteraaaaaaaaaa
Login to view more

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 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 United States at the end of the 20th century. It belongs to the class of cytostatic drugs. It has a unique mechanism of action and is effective for many drug-resistant patients. Specifically, paclitaxel can promote the assembly of tubulin into microtubules, but inhibits the depolymerization of microtubules, stabilizes the microtubules, resulting in abnormal arrangement of the microtubule bundles, causing the spun pituitary to lose normal functions and leading to cell death. , Ovarian cancer has outstanding curative effect, and it is mainly used clinically for first-line and second-line treatment of ovarian cancer, breast cancer and non-small cell lung cancer. [0003] Paclitaxel is almost insoluble in water and the gastrointestinal barrier is poorly per...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more

Application Information

Patent Timeline
no application Login to view more
Patent Type & Authority Patents(China)
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 HUIYU HEALTH HANGZHOU PHARM TECH CO LTD
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Try Eureka
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap