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Nanocrystalline eye drop, and preparation method and application thereof

A technology of nanocrystals and eye drops, applied in the fields of nanotechnology, nanotechnology, nanomedicine, etc., can solve problems such as research on diseases related to angiogenesis in the retina, and achieve the effect of easy tissue permeability, small size, and improved therapeutic effect.

Active Publication Date: 2020-01-10
CHENGDU RUIMU BIO PHARM TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Ruan Tan et al. made eye drops of tinib drugs only for the treatment of ocular surface angiogenesis-related diseases, such as pterygium, which can inhibit the growth of ocular surface neovascularization in rabbit eye suture models, and have no effect on fundus angiogenesis. research on related diseases

Method used

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  • Nanocrystalline eye drop, and preparation method and application thereof
  • Nanocrystalline eye drop, and preparation method and application thereof
  • Nanocrystalline eye drop, and preparation method and application thereof

Examples

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Embodiment 1

[0059] This embodiment provides a nanocrystalline eye drop, which contains a double-soluble macromolecule, a single-soluble macromolecule, and a targeted drug that simultaneously acts on the vascular endothelial growth factor receptor and the platelet growth factor receptor;

[0060] Bi-soluble macromolecules and mono-soluble macromolecules interact to encapsulate targeted drugs. Among them, the double-soluble macromolecule is poloxamer 188, the mono-soluble macromolecule is HPC EF, the targeted drug is axitinib, the mass ratio of poloxamer 188 and HPC EF is 5:1, and poloxamer 188 The mass ratio with Axitinib is 10:1.

[0061] The present embodiment also provides a preparation method of nanocrystalline eye drops:

[0062] Disperse 0.5g of Poloxamer 188 and 0.1g of HPC EF in 50ml of purified water to obtain a mixed solution;

[0063] Disperse 50 mg of axitinib in the above mixed solution to obtain an initial suspension with a drug concentration of 1 mg / mL;

[0064] Then tran...

Embodiment 2-10

[0066] The structure of the drug in the nanocrystalline eye drops provided in Examples 2-10 is the same as the structure of the drug in the nanocrystalline eye drop provided in Example 1, except that the specific compounds used are different.

Embodiment 2

[0069] In the nanocrystalline eye drops: the double-soluble macromolecule is Poloxamer 188, the single-soluble macromolecule is HPC EF, and the targeted drug is axitinib. The mass ratio of the double-soluble macromolecule and the single-soluble macromolecule is 5:1, the mass ratio of poloxamer 188 and axitinib is 5:1.

[0070] When preparing the nanocrystalline eye drops, the grinding temperature is 0° C., the rotation speed is 350 rpm, and the grinding time is 2 hours.

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Abstract

The present invention relates to the field of eye drops and particularly relates to a nanocrystalline eye drop, and a preparation method and an application thereof. The nanocrystalline eye drop comprises double-soluble macromolecules, single-soluble macromolecules and targeted drugs acting on vascular endothelial growth factor receptors and / or platelet growth factor receptors. The double-soluble macromolecules and the single-soluble macromolecules interact to encapsulate the targeted drugs to form nanocrystallines and maintain stability of the nanocrystallines. The eye drop can quickly penetrate a blood-eye barrier and enter a vitreous body through a special intercellular space penetration and / or pinocytosis method, an effective therapeutic effect is achieved through passive targeting andattachment, and at the same time, the drug is convenient to use.

Description

technical field [0001] The invention relates to the field of eye drops, in particular to a nanocrystalline eye drop, its preparation method and application. Background technique [0002] Macular degeneration is usually divided into two categories, one is juvenile macular degeneration, also known as congenital macular degeneration, and the other is age-related macular degeneration (AMD). In AMD and other eye diseases, retinal pigment epithelium (RPE) and choroid tissue can secrete and regulate growth factors such as VEGF, PDGF and PlGF and their corresponding receptors to promote angiogenesis, while overexpression can lead to vascular permeability Increased, producing AMD, DME, DR, retinal vein occlusion macular edema (RVO), myopic choroidal neovascularization (mCNV), pathological myopia (PM), ocular surface neovascular disease and neovascular glaucoma (NVG) and other eye diseases. Experimental and clinical studies have proved that inhibiting / regulating these growth factors...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K9/10A61K31/404A61K31/44A61K31/4439A61K31/517A61K45/00A61K47/20A61K47/26A61K47/34A61K47/36A61K47/38A61P9/10A61P27/02A61P27/06A61P27/10A61P37/06B82Y5/00A61K31/496A61K31/506
CPCA61K9/1274A61K9/0048A61K45/00A61K9/10A61K47/26A61K47/38A61K31/4439A61K47/20A61K47/36A61K31/44A61K47/34A61K31/517B82Y5/00A61K31/404A61P27/02A61P9/10A61P27/10A61P27/06A61P37/06A61K31/506A61K31/496A61K47/10A61K45/06
Inventor 董庆
Owner CHENGDU RUIMU BIO PHARM TECH CO LTD
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