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Application of nintedanib to prevention and treatment of ocular diseases

A technology for nintedanib and eye diseases, which is applied in the field of medicine to achieve good prevention and treatment effects

Inactive Publication Date: 2018-07-20
REYOUNG SUZHOU BIOLOGY SCI & TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there are no products on the market for the treatment of three angiogenic receptors for VEGF, PDGF, and FGF, so it is still necessary to find better drugs to treat eye diseases such as AMD, and the pharmaceutical composition also needs to provide sufficient concentrations of active agent to achieve therapeutic effect, and the number of times of use should not exceed 5 times a day, and the fewer times the better

Method used

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  • Application of nintedanib to prevention and treatment of ocular diseases
  • Application of nintedanib to prevention and treatment of ocular diseases
  • Application of nintedanib to prevention and treatment of ocular diseases

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] Preparation of nintedanib ethanesulfonate eye ointment:

[0034]

[0035]

[0036] Preparation method: In a clean bench (aseptic cabinet) in a class-C clean area, add the prescribed amount of micronized nintedanib ethanesulfonate and benzalkonium chloride into a suitable container according to the aseptic method, and add the prescribed amount The liquid paraffin that has been sterilized, filtered and cooled is ground into a fine paste, passed through a No. 6 sieve, and then gradually added to the sterilized filtered lanolin and vaseline base, stirred evenly, and cooled.

Embodiment 2

[0038] Preparation of nintedanib ethanesulfonate liposome eye drops:

[0039]

[0040] Preparation method: in a clean bench (aseptic cabinet) in a class C clean area, dissolve the prescribed amount of micronized nintedanib ethanesulfonate, soybean lecithin, cholesterol and benzalkonium chloride in 10ml according to the aseptic method ether, as the oil phase. Prepare 10 ml of 0.9% sodium chloride solution, adjust the pH to 6.8 with hydrochloric acid or sodium hydroxide, and use it as the water phase. The above two solutions were mixed and ultrasonicated intermittently for 30 minutes until a stable water / oil (W / O) emulsion was formed. Evaporate the emulsion under reduced pressure on a rotary evaporator to remove the organic solvent (water bath temperature 30°C, rotating speed 75r / min). After the gel is formed on the bottle wall, continue rotary evaporation to make the gel fall off and hydrate to obtain uniform liposomes. The suspension was sterilized by filtration with a 0....

Embodiment 3

[0042] Preparation of nintedanib ethanesulfonate emulsion eye drops:

[0043]

[0044]

[0045] Adjust the pH to 7.5 with hydrochloric acid or sodium hydroxide, and add water for injection to 100 mL.

[0046] Preparation method: In a clean bench (aseptic cabinet) in a class-C clean area, heat and stir the prescribed amount of medium-chain triglycerides, soybean lecithin, glycerin and one-half of the prescribed amount of polyoxyethylene castor oil , and then add cholesterol to dissolve it, and filter it as the oil phase. Dissolve the prescribed amount of micronized nintedanib ethanesulfonate in the oil phase according to the aseptic method, add the prescribed amount of vitamin E, the prescribed amount of benzalkonium chloride and one-half of the prescribed amount of polyoxyethylene Add castor oil to the prescribed amount of water, filter and use it as the water phase, homogeneously emulsify the water phase at 1000 rpm for 10 minutes, then quickly add the oil phase to the...

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PUM

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Abstract

The invention discloses application of nintedanib to prevention and treatment of ocular diseases, specifically to application of nintedanib and a salt or polymorph thereof and a nintedanib hydrate orsolvate as active ingredients in drugs used for prevention and treatment of ocular diseases. The related pharmaceutical compositions of nintedanib in the invention can treat ocular diseases directed at three angiogenesis receptors including VEGF, PDGF and FGF; and the application frequency of the pharmaceutical compositions is no more than 5 times a day, and the pharmaceutical compositions can provide an effective drug concentration, so good prevention and treatment effects are obtained.

Description

technical field [0001] The invention belongs to the field of medicine, and in particular relates to the application of nintedanib and its salt or polymorph, nintedanib hydrate or solvate as active ingredients in medicines for preventing and treating eye diseases. Background technique [0002] Nintedanib, namely 3-Z-[1-(4-(N-((4-methyl-piperazin-1-yl)-methylcarbonyl)-N-methyl-amino)-anilino) -1-phenyl-methylene]-6-methoxycarbonyl-2-indolinone, the compound structure is shown in formula (I): [0003] Nintedanib is a novel angiogenesis inhibitor that can simultaneously act on three key receptor families involved in angiogenesis: vascular endothelial growth factor receptor (VEGFR), platelet-derived growth factor receptor (PDGFR) ) and fibroblast growth factor receptor (FGFR). Nintedanib has been approved by the FDA and EMA for the treatment of idiopathic pulmonary fibrosis (IPF), and has also been approved by the EMA for use in combination with docetaxel after first-line che...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/496A61K9/00A61K9/06A61K9/107A61K9/127A61K47/28A61K47/44A61P27/02A61P27/06A61P27/12A61P27/10A61P29/00
Inventor 郭树华张佳春
Owner REYOUNG SUZHOU BIOLOGY SCI & TECH CO LTD
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