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Application of oleanolic acid derivative and pharmaceutically acceptable salts thereof in diabetic eye disease treatment

A technology for diabetic eye disease and zidonolic acid, applied in the field of long-acting polymer preparations, to avoid surgical trauma, improve bioavailability, and long-term effects

Active Publication Date: 2013-06-19
陈丽梅
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Although there are many methods for treating diabetic eye disease in the prior art, these methods only have a good effect on a single disease, for example, the effect is obvious only on retinopathy, but it is mediocre for other eye diseases caused by diabetes

Method used

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  • Application of oleanolic acid derivative and pharmaceutically acceptable salts thereof in diabetic eye disease treatment
  • Application of oleanolic acid derivative and pharmaceutically acceptable salts thereof in diabetic eye disease treatment

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0019] ①Mix 8ml acetone and 2ml ethanol;

[0020] ② Take 25mg of polysebacic anhydride (PSA) and add it to 1ml ① to prepare an organic phase;

[0021] ③Add 6mg of CDDO-ME to the organic phase prepared in ②;

[0022] ④ Take propylene glycol block polyether (i.e. F68) and Tween 80 (i.e. T80) (1:1) to make an aqueous solution containing 2% emulsifier, and add dextran-70 (i.e. Dextran-70) to it , adjust the pH of the solution to be 7.8;

[0023] 5. quickly drop the organic phase prepared in step 2 to the external aqueous phase prepared in 4;

[0024] ⑥ Removing the organic solvent to obtain a colloidal solution of nanoparticles.

Embodiment 2

[0026] ①Dissolve 40mg CDDO-IM and 150mg polylactide-glycolide (PLGA) with 1.8ml dichloromethane and 0.2ml DMSO in a 30°C water bath;

[0027] ②Add 1.5% polyvinyl alcohol to 7ml to ①, and ultrasonic;

[0028] ③ Pour ② into low-concentration polyethanol, stir at low speed at room temperature for 2 hours, and wait for the organic solvent to evaporate;

[0029] ④ Collect the obtained nanoparticles after centrifugation at 4°C for 60 minutes;

[0030] ⑤ Wash the product obtained in ④ three times with double distilled water to obtain the drug-loaded nanoparticles.

Embodiment 3

[0032] ①Mix 8ml of dichloromethane and 2ml of ethyl acetate;

[0033] ② Take 100mg PLGA and add it to 1ml ① to prepare an organic phase;

[0034] ③Add 20mg CDDO-MA to the organic phase prepared in ②;

[0035] ④ Take F68 and T80 (1:1) to make a 4% aqueous solution containing an emulsifier, and add Dextran-70 to it to adjust the pH of the solution to 8;

[0036] 5. quickly drop the organic phase prepared in step 2 to the external aqueous phase prepared in 4;

[0037] ⑥ Removing the organic solvent to obtain a colloidal solution of nanoparticles.

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PUM

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Abstract

The present invention discloses an application of an oleanolic acid derivative and pharmaceutically acceptable salts thereof in diabetic eye disease treatment. The oleanolic acid derivative is prepared into a nanometer preparation, a microsphere preparation and a hydrogel by using a polymer, such that toxicity of the oleanolic acid derivative is substantially reduced, an administered dose is increased, the obtained drug can provide an effect in eyes, and can provide stronger therapeutic effects compared to ordinary preparations and other long-acting preparations of the oleanolic acid derivative, the effect can be lasted for a plurality of months, and is uniform, and the drug can provide treatment effects for various or most of diabetic eye diseases, and can be taken at the diabetic eye disease initial stage so as to relieve patient pain, such that pathogenetic condition deterioration can be avoided, and surgeries and other surgical treatment methods with heavy traumas can be avoided.

Description

technical field [0001] The invention relates to a medicine for treating diabetic eye disease, in particular to the application of zidonolic acid derivatives and pharmaceutically acceptable salts thereof in the preparation of medicines for treating diabetic eye disease, the preparation of the zidonolic acid derivatives and pharmaceutically acceptable salts thereof Become a polymer long-acting preparation. Background technique [0002] Diabetes is a group of metabolic diseases characterized by elevated blood sugar levels. It is one of the three major diseases that threaten human health in the 21st century. Microvascular disease can cause many complications in patients, and eye disease is one of the important chronic complications. Almost all eye diseases may occur in diabetic patients, such as fundus hemangioma, fundus hemorrhage, dacryocystitis, glaucoma, cataract, vitreous opacity, optic atrophy, macular degeneration, retinal detachment. The prevalence of diabetes in my cou...

Claims

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Application Information

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IPC IPC(8): A61K31/56A61K9/16A61K9/10A61P3/10A61P27/02
Inventor 陈丽梅薛志花
Owner 陈丽梅
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