Composition of docetaxel polymer micelle freeze-dried preparation and special solvent

A technology of docetaxel and polymer glue, which is applied in the field of medicine and chemical industry, can solve the problems of short validity period of drugs, difficult application, increased substance content, etc., and achieve the effect of solving physical stability problems and chemical stability problems

Active Publication Date: 2018-01-16
XINAN PHARMA
View PDF3 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But the contriver finds in further research, although above-mentioned method can improve the physical stability of docetaxel polymer micelle to a certain extent, but this arginine-docetaxel polymer micelle is accelerating (temperature 25 ±2°C) and long-term (6±2°C) stability studies, the content of related substances increased rapidly, resulting in a drug with a short validity period and difficult to be used in clinical practice
Therefore, it is necessary to study a docetaxel polymer micelle system that can solve both the physical stability of the docetaxel polymer micelle and the chemical stability of the docetaxel polymer micelle during long-term storage. Stability issues

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
  • Composition of docetaxel polymer micelle freeze-dried preparation and special solvent
  • Composition of docetaxel polymer micelle freeze-dried preparation and special solvent
  • Composition of docetaxel polymer micelle freeze-dried preparation and special solvent

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0019] Embodiment 1, the preparation of docetaxel polymer micelle lyophilized preparation

[0020] Weigh 5g of polyethylene glycol monomethyl ether-polylactic acid amphiphilic block copolymer (mPEG to PDLLA mass ratio is 40:60) and dissolve it in an appropriate amount of acetonitrile to prepare mPEG-PDLLA acetonitrile solution, and take another 1g of docetaxel Dissolve docetaxel in an appropriate amount of acetonitrile to prepare a docetaxel acetonitrile solution, mix the mPEG-PDLLA acetonitrile solution with the docetaxel acetonitrile solution, and remove the acetonitrile by rotary evaporation, so that the docetaxel and mPEG-PDLLA form a polymer gel, Then add 100ml of water for injection, rotate to hydrate to form a polymer micelle solution, add a freeze-drying protective agent, add water to volume, filter with a 0.22 μm microporous membrane, and freeze-dry the filtrate to prepare a docetaxel polymer gel A bundle of lyophilized preparations (the mass ratio of docetaxel to mPE...

Embodiment 2

[0022] Embodiment 2, the preparation of docetaxel polymer micelle lyophilized preparation

[0023] Weigh 5g of polyethylene glycol monomethyl ether-polylactic acid amphiphilic block copolymer (mPEG to PDLLA mass ratio is 50:50) and dissolve it in an appropriate amount of acetonitrile to prepare mPEG-PDLLA acetonitrile solution, and take another 1g of docetaxel Dissolve docetaxel in an appropriate amount of acetonitrile to prepare a docetaxel acetonitrile solution, mix the mPEG-PDLLA acetonitrile solution with the docetaxel acetonitrile solution, and remove the acetonitrile by rotary evaporation, so that the docetaxel and mPEG-PDLLA form a polymer gel, Then add 100ml of water for injection, rotate to hydrate to form a polymer micelle solution, add a freeze-drying protective agent, add water to volume, filter with a 0.22 μm microporous membrane, and freeze-dry the filtrate to prepare a docetaxel polymer gel A bundle of lyophilized preparations (the mass ratio of docetaxel to mPE...

Embodiment 3

[0025] Example 3, preparation of arginine aqueous solution, a special solvent for docetaxel polymer micelle freeze-dried preparation

[0026] Dissolve 4g of arginine in 1000ml of water for injection, add 0.2g of activated carbon, adjust the volume to 2000ml with water, mix well, let it stand for 20 minutes, first filter it with a microporous membrane with a pore size of 0.45μm, and then filter it with a pore size of 0.22μm The microporous membrane is filtered, and the filtrate is divided into vials, plugged, capped, inspected by light, and packaged, that is, the special solvent for docetaxel polymer micellar freeze-dried preparation-arginine aqueous solution.

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
concentrationaaaaaaaaaa
concentrationaaaaaaaaaa
pore sizeaaaaaaaaaa
Login to view more

Abstract

The invention discloses a composition of a docetaxel polymer micelle freeze-dried preparation and a special solvent. The docetaxel polymer micelle freeze-dried preparation is composed of docetaxel, polyethylene glycol monomethyl ether-poly Composed of lactic acid amphiphilic block copolymer and freeze-drying protective agent, the special solvent is arginine aqueous solution; the clinical application of the composition is to inject the special solvent into the docetaxel polymer micelle freeze-dried preparation before use, After reconstitution, a stable polymer micelle solution is formed and used; the present invention can not only solve the physical stability problem of the docetaxel polymer micelle freeze-dried preparation, but also solve the problem of docetaxel polymer micelle freeze-dried preparation. Chemical stability issues of dry formulations during long-term storage.

Description

technical field [0001] The invention belongs to the technical field of medicine and chemical industry, and relates to a composition composed of a polymer micelle freeze-dried preparation and a special solvent. Background technique [0002] Polymer micelle is a drug-loading system for insoluble drugs developed in recent years. It has a core-shell structure, in which the core is a hydrophobic part and the shell is a hydrophilic part. The purpose of solubilizing poorly soluble drugs. Compared with commonly used solubilizers and latent solvents such as Tween 80, polyoxyethylene castor oil, etc., since the polymers used are all biodegradable materials, their safety is greatly improved. However, the stability of the existing drug-loaded polymer micelles is poor, and drugs are easily leaked from the polymer micelles, which affects the popularization and application of drug-loaded polymer micelles. [0003] Chinese patent application CN 101972480 A discloses a docetaxel polymer mi...

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): A61K9/19A61K31/337A61K47/34A61P35/00
Inventor 蒲道俊冯燕丽邹意琼余春梅陈兰杨秀丽李慧慧郑小锋
Owner XINAN PHARMA
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