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A kind of pharmaceutical composition of vegfr inhibitor and preparation method thereof

A composition and drug technology, which is applied in the direction of drug combination, pharmaceutical formula, antineoplastic drugs, etc., can solve the problems of individual differences in nano-preparations without literature reports, etc.

Active Publication Date: 2021-04-06
JIANGSU HENGRUI MEDICINE CO LTD
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  • 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

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  • A kind of pharmaceutical composition of vegfr inhibitor and preparation method thereof
  • A kind of pharmaceutical composition of vegfr inhibitor and preparation method thereof
  • A kind of pharmaceutical composition of vegfr inhibitor and preparation method thereof

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 PH101 in the granulator, turn...

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Abstract

The invention relates to a pharmaceutical composition of a VEGFR inhibitor and a preparation method thereof. Specifically, the present invention relates to a N-[4-(1-cyanocyclopentyl)phenyl]-2-(4-pyridylmethyl)amino-3-picolinylmethyl group comprising a particle size D90 of less than about 10 μm A pharmaceutical composition of amides and a method for preparing the same, the pharmaceutical composition has improved individual variability compared with commercially available preparations.

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

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Application Information

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Patent Type & Authority Patents(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
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