Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

Method for purifying carbetocin

A technology of carbetocin and pure product, which is applied to the preparation method of peptide, chemical instrument and method, organic chemistry and other directions, can solve the problem that the yield of carbetocin product is not high and carbetocin cannot be effective. Separation, low purity of carbetocin finished products, etc.

Active Publication Date: 2013-12-11
ADLAI NORTYE BIOPHARMA CO LTD
View PDF3 Cites 12 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The technical problem that the present invention needs to solve is: select a kind of purification method of carbetocin, solve (1) carbetocin finished product purity is not high, (2) carbetocin finished product yield is not high, ( 3) The problem that carbetocin cannot be effectively separated from the impurity D-Cys5- carbetocin

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
  • Method for purifying carbetocin
  • Method for purifying carbetocin
  • Method for purifying carbetocin

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0095] Solid phase synthesis of carbetocin:

[0096] Scale: 1.0 mmol carbetocin Synthesis:

[0097] Step (1) Peptide Resin Reaction: Weigh 1.38g (1.1mmol) Wang Resin (the degree of substitution is 0.80mmol / g) into the reaction kettle, add 15ml DCM, stir and swell at 15-35°C for 30min, and remove by suction filtration liquid. Weigh 1.17g (3.3mmol) Fmoc-Leu-OH and 0.45g (3.3mmol) HOBt into a dissolution tank. Measure 6ml of DMF solvent into the tank, stir to dissolve, cool down to about 0-15°C in an ice bath after complete dissolution, add 510μl (3.3mmol) of DIC, stir well, control the temperature at 10-25°C for 5min, add 0.04g (0.3mmol) DMAP, then added to the reaction kettle, reacted at 25-35°C for 5h, took a sample to detect that the degree of substitution was 0.73mmol / g, and pumped out the reaction solution. Measure 10ml of DMF into the reaction kettle, stir and wash for 3 minutes, and repeat the washing 3 times. Measure 525 μl (5.5 mmol) of acetic anhydride, 445 μl (5.5...

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
Wavelengthaaaaaaaaaa
Login to View More

Abstract

The invention relates to a method for purifying carbetocin. The method is characterized by comprising the following steps of: 1, dissolving a carbetocin crude product by using water, and regulating pH to be acidic; 2, arranging gradients according to volume fraction, and flushing a polymer reverse-phase filled column by using a mobile phase A; 3, loading a solution obtained from the step 1 into a polymer reverse-phase filler; 4, arranging the gradients according to the volume fraction, wherein a mobile phase B is 5% in the initial state of the eluted gradients and is kept for 2 minutes, then the proportion of the mobile phase B is increased to 25% within 5 minutes, and then the proportion of the mobile phase B is increased to 40% within 30 minutes; collecting all eluted distillates; 5, drying the eluted distillates to obtain the pure product carbetocin.

Description

Technical field: [0001] The invention relates to a purification method of polypeptide drugs, which is a purification method of a synthetic long-acting oxytocin nonapeptide analogue with agonist properties. Background technique: [0002] Carbetocin is a cyclic polypeptide with the following structural formula: [0003] [0004] The chemical formula is as follows: [0005] [0006] The clinical and pharmacological properties of carbetocin are similar to those of naturally occurring oxytocin. Like oxytocin, carbetocin binds to the oxytocin receptors of uterine smooth muscle, causing rhythmic contractions of the uterus, increasing its frequency and increasing uterine tension on the basis of the original contractions. Oxytocin receptor levels in the uterus are low in the non-pregnant state, increase during pregnancy, and peak at parturition. Carbetocin therefore has no effect on the non-pregnant uterus, but has potent uterotonic effects on the pregnant and newborn uterus...

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
IPC IPC(8): C07K7/16C07K1/20
Inventor 路杨杨东晖周亮张阳萍
Owner ADLAI NORTYE BIOPHARMA CO LTD
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products

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

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com