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

Pharmaceutical composition of VEGFR inhibitor and preparation method of pharmaceutical composition

A composition and drug technology, applied in the directions of drug combination, pharmaceutical formulation, pill delivery, etc., can solve the problem of individual differences of nano-preparation and no literature report.

Active Publication Date: 2019-03-01
JIANGSU HENGRUI MEDICINE CO LTD
View PDF9 Cites 3 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] However, the use of nano-formulations to improve the individual variability of a drug in different patients has not been reported in the literature.

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
  • Pharmaceutical composition of VEGFR inhibitor and preparation method of pharmaceutical composition
  • Pharmaceutical composition of VEGFR inhibitor and preparation method of pharmaceutical composition
  • Pharmaceutical composition of VEGFR inhibitor and preparation method of pharmaceutical composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0050] Embodiment 1: Preparation and characterization of nanosuspension

[0051] Weigh about 2.5g of HPMC, add 100ml of purified water, stir to disperse and gradually dissolve, add 0.25g of SDS, stir to dissolve for later use;

[0052] Weigh about 1.0g of N-[4-(1-cyanocyclopentyl)phenyl]-2-(4-pyridylmethyl)amino-3-pyridinecarboxamide (Compound A) and add it to 10ml of the aforementioned solution, stir Mix for 30 minutes, the approximate concentration of compound A is 100mg / ml;

[0053]Use a 50ml ball mill tank, add small balls with a volume of 20ml, grind at a speed of 150rpm, grind for 60s, stop for 30s, before grinding (0h), after grinding 10min, 30min, 1h, 90min, 90min+10min (300rpm) , take a proper amount of samples with a syringe, and investigate the particle size (take the nanosuspension before grinding (0h) and grind for different times to directly detect the particle size), see Table 1.

[0054] Table 1: Particle size results before grinding and after grinding for di...

experiment example 1

[0056] Experimental Example 1: Physical Stability of Nanosuspension

[0057] Test 1: Take an appropriate amount of nano-suspension, seal it, place it at room temperature for 17 hours, and place it in a stability test chamber at 40°C for 6 hours to investigate the change in particle size of the suspension. It was found that after being placed at 40 degrees, D90 increased, D10 and D50 did not change significantly, and the stability at room temperature was better. The data are shown in Table 2.

[0058] Table 2:

[0059]

Embodiment 2

[0060] Embodiment 2: Nanoparticle tablet preparation

[0061]

[0062] 1) Preparation of nanosuspension

[0063] Weigh about 2.5g of HPMC (hydroxypropyl methylcellulose), 0.25g of SDS (sodium dodecyl sulfate), add 120ml of purified water, stir and dissolve for later use;

[0064] Weigh about 16.4mg of N-[4-(1-cyanocyclopentyl)phenyl]-2-(4-pyridylmethyl)amino-3-pyridinecarboxamide (compound A) and add it to 82ml of the aforementioned solution, Stir and mix well, the approximate concentration of compound A is 200mg / ml;

[0065] Using a 500ml ball mill tank, add 120ml volume of small balls and grind (grinding speed about 250rpm) to the target particle size. The particle size after grinding is shown in Table 3

[0066] table 3

[0067] sample

D10

D50

D90

D[4,3]

Compound A

45.5μm

108μm

207μm

77.5μm

Compound A after milling

0.025μm

0.105μm

1.64μm

3.26μm

[0068] 2) Granulation

[0069] Take 25g of MCC P...

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 diameteraaaaaaaaaa
particle diameteraaaaaaaaaa
particle diameteraaaaaaaaaa
Login to View More

Abstract

The invention relates to pharmaceutical composition of a VEGFR inhibitor and a preparation method of the pharmaceutical composition. Specifically, the invention relates to composition comprising N-[4-(1-cyanocyclopentyl)phenyl]-2-(4-pyridylmethyl)amino-3-pyridinecarboxamide with the particle size D90 smaller than about 10 mu m and a preparation method of the pharmaceutical composition. Compared with a commercial preparation, the pharmaceutical composition has improved individual difference.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, in particular to a N-[4-(1-cyanocyclopentyl)phenyl]-2-(4-pyridylmethyl)amino-3- A pharmaceutical composition of picolinamide and a preparation method thereof. Background technique [0002] In recent years, small molecule inhibitors of VEGFR have gradually become a new type of non-cytotoxic antitumor drugs with great application prospects. Compared with traditional cytotoxic drugs that inhibit tumor growth, therapeutic drugs targeting neovascularization have higher specificity, lower toxicity, and help overcome tumor drug resistance, and can be used for the treatment of various tumors . N-[4-(1-cyanocyclopentyl)phenyl]-2-(4-pyridylmethyl)amino-3-pyridinecarboxamide (compound A) is a new generation of small molecule inhibitors of VEGFR, with the following structure: [0003] [0004] N-[4-(1-cyanocyclopentyl) phenyl]-2-(4-pyridylmethyl) amino-3-pyridinecarboxamide methanesulfonate ...

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): A61K9/10A61K9/20A61K9/14A61K47/38A61K47/20A61K31/444A61P35/00
CPCA61K9/10A61K9/145A61K9/146A61K9/2013A61K9/2054A61K31/444A61P35/00
Inventor 李俊明杨俊然王立坤杜振兴
Owner JIANGSU HENGRUI MEDICINE 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