Amphiphilic block copolymer micelle composition containing taxane and manufacturing process of the same

An amphiphilic block and composition technology, which is applied in the directions of drug combination, medical preparations containing active ingredients, drug delivery, etc., can solve the problems of reduced pharmacological effect, degradation of active pharmaceutical ingredients, etc., so as to reduce the preparation time and prevent rapid The best effect of release, pharmacological effect

Active Publication Date: 2010-12-08
SAMYANG HLDG CORP
View PDF0 Cites 10 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Further, the solvent evaporation process basically includes a step of exposing the reagent to high temperature for a long time, so it may cause problems such as degradation of pharmaceutically active ingredients or reduction of pharmacological effects

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
  • Amphiphilic block copolymer micelle composition containing taxane and manufacturing process of the same
  • Amphiphilic block copolymer micelle composition containing taxane and manufacturing process of the same
  • Amphiphilic block copolymer micelle composition containing taxane and manufacturing process of the same

Examples

Experimental program
Comparison scheme
Effect test

preparation example 1

[0052] Preparation Example 1: Monomethoxy polyethylene glycol-polylactide (mPEG-PLA) block copolymer (A-B type) synthesis

[0053] First, 5.0 g of monomethoxypolyethylene glycol (number average molecular weight: 2,000 Dalton) was introduced into a 100 mL two-necked round bottom flask, and heated at 130° C. for 3-4 hours under reduced pressure (1 mmHg) to remove water from it. Next, the flask was purged with nitrogen, and 0.1 wt% (10.13 mg, 25 mmol) of stannous octoate (Sn(Oct) 2 ) based on the weight of D-lactide and L-lactide was added thereto using a syringe. as a reaction catalyst. The reaction mixture was stirred for 30 minutes, then allowed to depressurize (1 mmHg) at 130° C. for 1 hour to remove the solvent (toluene) which dissolved the catalyst. Then, 10.13 g of purified lactide was added thereto, and the resulting mixture was heated at 130° C. for 18 hours. After heating, the resulting polymer was dissolved in dichloromethane, and this was added to diethyl ether...

preparation example 2

[0055] Preparation Example 2: Monomethoxy polyethylene glycol-polylactic acid-glycolic acid copolymer (mPEG-PLGA) block Synthesis of Copolymer (Type A-B)

[0056] In the same manner as in Preparation Example 1, by making monomethoxypolyethylene glycol (number average molecular weight: 5,000 Daltons), lactide and glycolide in the presence of stannous octoate as a catalyst, The reaction was carried out at 120° C. for 12 hours to obtain a block copolymer.

[0057] The block copolymer monomethoxy polyethylene glycol-polylactic acid-glycolic acid copolymer (mPEG-PLGA) has a number average molecular weight of 5,000-4,000 Daltons and is an A-B type copolymer. pass 1 Analysis of the copolymer by H-NMR revealed that the copolymer is an A-B type diblock copolymer (see figure 2 ).

Embodiment 1

[0058] Example 1: mPEG-PLA block copolymer micelles containing sodium chloride and docetaxel compound preparation

[0059] First, 760 mg of the amphiphilic block copolymer mPEG-PLA (number average molecular weight: 2,000-1,765 Daltons) obtained in Preparation Example 1 was completely dissolved in 0.2 mL of ethanol at 60°C to provide clear ethanol solution. The ethanol solution was cooled to 25°C, and 20 mg of docetaxel was added thereto, and the resulting solution was stirred until docetaxel was completely dissolved.

[0060] Next, aqueous solutions each containing 0.9 wt % and 1.8 wt % of sodium chloride and having an osmolality of 300 mOsm / kg and 600 mOsm / kg were prepared in separate containers. The osmolarity was measured by using a commercially available osmometer (Gonotech GmbH, OSMOMAT030). 4 mL of each aqueous solution was added to the ethanol solution containing the copolymer, and the resulting mixture was stirred at 40° C. for 10 minutes to form an aqueous solut...

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
molecular weightaaaaaaaaaa
molecular weightaaaaaaaaaa
number average molecular weightaaaaaaaaaa
Login to view more

Abstract

A taxane-containing amphiphilic block copolymer micelle composition, including taxane, an amphiphilic block copolymer containing a hydrophilic block and a hydrophobic block, and an osmolality adjusting agent, is discribed. Also described are a method for preparing the same composition. The composition has excellent stability so that it can prevent rapid release of a drug and can improve a desired pharmacological effect. Additionally, the method enables highly efficient preparation of the composition.

Description

technical field [0001] Exemplary embodiments of the present invention relate to taxane-containing amphiphilic block copolymer micelle compositions and methods for their preparation. Background technique [0002] In order to implement intravenous administration of drugs, submicronic particulate drug delivery systems using biodegradable polymers have been studied. Recently, nanoparticle systems and polymeric micelle systems using biodegradable polymers have been reported to be useful technical systems that can alter the in vivo distribution of drugs to reduce adverse side effects and can provide improved efficacy. Furthermore, because such systems enable targeted drug delivery, they can achieve controlled drug release to target organs, target tissues, or target cells. In fact, such systems are known to have excellent compatibility with body fluids, and improve the solubility of poorly soluble drugs and the bioavailability of the drugs. [0003] Recently, a method for prepari...

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 Applications(China)
IPC IPC(8): C08K5/04A61K31/785A61K9/127C08L39/04
CPCC08L2203/02C08G63/664A61K9/1075A61K31/337C08L2205/05C08G65/3324A61K31/7048C08K5/1525C08L71/02C08L67/04A61K9/0019C08G65/3322A61P35/00C08L2666/18C08K5/04C08L71/00C08L67/00C08K5/00
Inventor 李思元徐敏孝
Owner SAMYANG HLDG CORP
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