Larotaxel water-soluble powder injection preparation and application

A technology of water-soluble powder and larotaxel, which can be applied to medical preparations with non-active ingredients, medical preparations containing active ingredients, powder delivery, etc., and can solve the problem of larotaxel nano-polymer micelles Relevant preparation research and other issues

Active Publication Date: 2016-10-05
SHANDONG HUBBLE KISEN BIOLOGICAL TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] After patent and literature search, there is no report related to the preparation of larotaxel nano-polymer micelles

Method used

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  • Larotaxel water-soluble powder injection preparation and application
  • Larotaxel water-soluble powder injection preparation and application
  • Larotaxel water-soluble powder injection preparation and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment example 1

[0031] Weigh 180mg carrier material (mPEG 2000 -PDLLA 1700 ) and 20 mg of larotaxel were placed in a round bottom flask, 10 mL of absolute ethanol was added, and the carrier material and the drug were fully dissolved by ultrasonication. The solution was placed in a rotary evaporator at 40° C. for 60 minutes to evaporate the organic solvent completely to obtain a dry and transparent mixed film matrix. Then add 10mL of water for injection preheated at 60°C, hydrate to form micelles under stirring conditions, add mannitol, first pass through a 0.45μm filter membrane for coarse filtration, and then pass through a 0.22μm sterile filter membrane for fine filtration to sterilize, the filtrate freeze-dried to obtain a sample.

Embodiment example 2

[0033] Weigh 150mg carrier material (mPEG 2000 -PCL 2000 ) and 50 mg of larotaxel were placed in a lyophilized bottle, 5 ml of tert-butanol was added, and the carrier material and the drug were fully dissolved by ultrasonication. The solution is lyophilized and the organic solvent is completely removed to obtain a mixed matrix of drug and carrier material. Then add 10mL of water for injection preheated at 60°C, hydrate to form micelles under the condition of stirring, add sucrose, first pass through a 0.45μm filter membrane for coarse filtration, and then pass through a 0.22μm sterile filter membrane for fine filtration to sterilize, and the filtrate is frozen Dry to get a sample.

Embodiment example 3

[0035] Weigh 180mg carrier material (mPEG 5000 -PGA 6000 ) and 20 mg of larrotaxel were placed in a round bottom flask, 5 ml of tetrahydrofuran was added, and the carrier material and the drug were fully dissolved by ultrasonication. The solvent was distilled under reduced pressure to completely remove the organic solvent to obtain a dry and transparent mixed film matrix. Then add 10 mL of water for injection preheated at 50°C, vortex for 3 minutes, add trehalose, pass the hydration solution through a 0.45 μm filter membrane for coarse filtration, and then pass through a 0.22 μm filter membrane for fine filtration to sterilize, and the filtrate is freeze-dried to obtain sample.

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Abstract

The invention relates to larotaxel which is a new-generation taxane medicine. The larotaxel is loaded in a carrier auxiliary material to form nanoscale particles which are lyophilized to form a powder injection. The carrier auxiliary material is an amphipathic segmented copolymer comprising a hydrophilic segment and a hydrophobic segment, the hydrophilic segment refers to methoxy polyethylene glycol, and the hydrophobic segment comprises polylactic acid, polycaprolactone, polyglutamic acid, polytrimethylene carbonate, polymethyl methacrylate and the like. Prepared drug loading micelles are high in drug loading capacity, encapsulation efficacy and stability, and water solubility of drugs is greatly improved; particle sizes of the prepared micelles range from 10nm to 100nm, and recognition and elimination of a reticuloendothelial system can be avoided by pegylation, in-vivo circulation is prolonged, passive targeting to tumor tissues is realized, and accordingly curative effect improvement and toxic and side effect reduction are realized.

Description

field of invention [0001] The invention relates to the preparation and application of larotaxel water-soluble powder injection, which belongs to the technical field of medicines, and in particular to a preparation method and application of a water-soluble preparation formed by encapsulating larotaxel in a biodegradable carrier material. Background technique [0002] Cancer is a serious threat to human health and the second killer after cardiovascular and cerebrovascular diseases. According to estimates from the American Cancer Society, cancer will become the number one cause of death in the next few years. According to the report of the World Health Organization (WHO), as a country with a large population, with the deterioration of environmental pollution and food safety, the incidence of cancer is extremely serious. [0003] At present, the most commonly used anti-tumor drugs in clinic are taxane compounds, which are widely used in the treatment of breast cancer, cervical c...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/19A61K31/337A61K47/34A61P35/00
CPCA61K9/0019A61K9/19A61K31/337A61K47/34
Inventor 王成张震刘宗银徐益杨爽
Owner SHANDONG HUBBLE KISEN BIOLOGICAL TECH CO LTD
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