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Application of artemisinin and derivatives thereof in preparation of ophthalmic vascular disease prevention and treatment medicines, and medicinal composition

A technology of artemisinin and its derivatives, applied in the field of ophthalmic vascular diseases, can solve the problems of peripheral visual field damage, decreased treatment effect, drug tolerance, etc. The effect of reducing complications

Inactive Publication Date: 2015-09-16
ZHONGSHAN OPHTHALMIC CENT SUN YAT SEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] 2. There are still 10-20% of patients who are ineffective in treatment, and some patients develop drug tolerance after repeated treatment, and the treatment effect declines;
[0007] 3. The price is expensive, which limits its application to a certain extent
However, as a traumatic treatment, laser therapy can cause irreversible damage to peripheral vision, and some patients can relapse

Method used

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  • Application of artemisinin and derivatives thereof in preparation of ophthalmic vascular disease prevention and treatment medicines, and medicinal composition
  • Application of artemisinin and derivatives thereof in preparation of ophthalmic vascular disease prevention and treatment medicines, and medicinal composition
  • Application of artemisinin and derivatives thereof in preparation of ophthalmic vascular disease prevention and treatment medicines, and medicinal composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] The application of artesunate in the preparation of drugs for the treatment of retinal choroidal neovascularization specifically includes the following:

[0029] (1) Dosing: mix artesunate and 0.05% sodium bicarbonate solution to make a 0.1-6mg / ml gradient solution;

[0030] (2) Dose: 0.1-0.5ml;

[0031] (3) Operation steps:

[0032] A. Disinfection of the surgical area: Disinfect the eyelids and skin around the eyes with 10% povidone-iodine, put 3 drops of 0.5% povidone-iodine in the conjunctival sac for a few minutes, rinse the conjunctival sac with tobramycin solution, and use antibiotic drops Eye drops to prevent dryness and abrasion of the cornea.

[0033] B. Local anesthesia: Put 3 to 4 drops of Alcaine eye drops into the conjunctival sac for local anesthesia.

[0034] C. Vitreous intravitreal injection: The injection site should be located 3.5-4 mm behind the limbus. The syringe uses a 30-gauge needle to pass through the surface of the sclera obliquely, and th...

Embodiment 2

[0036] (1) In vitro test

[0037] 1. Purpose of the experiment

[0038]Through in vitro experiments, the effects of artemisinin (Q) and its derivatives (artesunate (ART), dihydroartemisinin (DI) and artemether (J)) on HUVEC and RF / 6A were analyzed, namely Analyze the inhibition of HUVEC and RF / 6A proliferation and induction of HUVEC and RF / 6A apoptosis by artemisinin and its derivatives, so as to further screen the most effective artemisinin derivative monomers, calculate IC50, and find the appropriate concentration.

[0039] 2. Experimental method

[0040] (1) Human umbilical vein endothelial cells (human umbilical vein endothelial cells, HUVEC) were extracted for primary culture, and the 2nd-4th passage cells were used.

[0041] (2) Artemisinin and its derivative monomers induce HUVEC apoptosis experiment

[0042] Subjects: HUVEC, rhesus monkey retinal choroidal vascular endothelial cells (RF / 6A);

[0043] The experimental method is as follows, apoptosis test (MTT), repe...

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PUM

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Abstract

Disclosed are uses of artemisinin and derivatives thereof in the manufacture of medicaments for inhibition of ocular vascular endothelial cell proliferation, or the prevention and treatment of related diseases of ocular vascular system exudation, edema, new blood vessels formation and proliferation, and pharmaceutical compositions comprising artemisinin and derivatives thereof. Artemisinin and derivatives thereof of the present invention can be used for the prevention and treatment of ocular vascular related diseases, such as age-related macular degeneration, diabetic retinopathy, retinal central vein occlusion and retinal branch vein occlusion etc.

Description

technical field [0001] The invention relates to the field of ophthalmic vascular diseases, in particular to the application and pharmaceutical composition of artemisinin and its derivatives in the preparation of medicines for preventing and treating ophthalmic vascular-related diseases. Background technique [0002] Artemisinin (artemisinin, Q), also known as artemisinin, chrysanthemum, and artemisinin, is a sesquiterpene lactone drug with peroxy groups extracted from the plant Artemisia annua. Its common derivatives are: Hydrogen artemisinin (Dihydroartemisinin, DI), artesunate (Artesunate, ART), artemether (artemether, J), arteether (Arteether), artemisone (Artemisone), etc. Due to the existence of peroxide bridges in its molecular structure, free radicals are mediated by the free iron produced after the decomposition of hemoglobin. In the prior art, artemisinin and its derivatives are mainly used to kill malaria parasites. It is used for the treatment of various types of...

Claims

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Application Information

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IPC IPC(8): A61K31/357A61K31/541A61P27/02A61P27/06A61P35/00A61P29/00
CPCA61K9/0048A61K31/357A61K31/366A61P27/02A61P27/06A61P29/00A61P35/00
Inventor 高前应宗瑶
Owner ZHONGSHAN OPHTHALMIC CENT SUN YAT SEN UNIV
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