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Application of organic dicarboxylic acid salts in preparing medicaments for preventing and treating cataract

An organic dicarboxylate and cataract technology, which is applied in the application field of medicine, can solve the problems of reducing benzyl lysine eye drops, increasing patient compliance, influence, etc., and achieving enhanced antioxidant capacity and high effect intensity. , the effect of high efficiency

Active Publication Date: 2010-05-12
ZHEJIANG SHAPUAISI PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Over the past ten years, due to its unique and precise curative effect, more and more cataract patients welcome this drug, which makes the influence of this product in the anti-cataract market rise with a strong advantage; because 50% of users respond to a certain Transient burning sensation, some patients could not tolerate the treatment and gave up the treatment, which affected the advantages of its anti-cataract drugs; so reducing the irritation of benda-lysine eye drops and increasing the compliance of patients has become the problems urgently need to be solved,

Method used

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  • Application of organic dicarboxylic acid salts in preparing medicaments for preventing and treating cataract
  • Application of organic dicarboxylic acid salts in preparing medicaments for preventing and treating cataract
  • Application of organic dicarboxylic acid salts in preparing medicaments for preventing and treating cataract

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0013] One class of organic dicarboxylates is eight kinds of monomeric compounds derived from Bendalysine. Its chemical structural formula and number are as follows:

[0014]

[0015]

[0016] Bendalysine (BDL, No. 5) is provided by Zhejiang Shapuaisi Pharmaceutical Co., Ltd., with a purity greater than 98.5%. Compounds No. 1-9 are prepared by dissolving in different solutions according to different tests, such as: Acute intravenous injection test, chick embryo allantoic membrane irritation test, eye irritation blink test, use 0.9% NaCl (WT) solution, acute poison gavage test with 0.5% (WT) carboxymethyl cellulose solution to clean the lens Use pH 7.2 phosphate buffer solution, commercially available Bendalysine eye drop formula for allergy test, and DMEM cell culture medium for anti-oxidation test of lens, etc. Under the above conditions, No. 1-5 is easy to dissolve in water, No. 6-9 is not easy to dissolve in water, especially No. 8 is not easy to dissolve in water. T...

Embodiment 2

[0048] Example 2 Experimental Research on Resisting Oxidative Damage of Lens

[0049] 1. Materials

[0050] 1.1. Experimental animals: rats, guinea pigs, rabbits, both male and female.

[0051] 1.2. Main reagents and drugs:

[0052] DMEM / high glucose (high sugar) culture medium was purchased from Thermo Fisher Biochemical Co., Ltd. (Beijing), vitamin C, 30% (VT) H 2 o 2 , FeCl 3 , NaCl, Na 2 HPO 4 and NaH 2 PO 4 etc. are commercially available AR-grade reagents. Xylose (D+xylose) is commercially available HGB-grade reagents.

[0053] 1.3. Main equipment: ultra-clean bench, CO 2 Incubator, homogenizer, low-temperature high-speed centrifuge, visible spectrophotometer, 12-well culture plate.

[0054] 2. Method

[0055] 2.1. Lens culture: kill the rats and rabbits, take out the eyeball and rinse it with normal saline containing 500u / mL penicillin, carefully cut the eyeball from the posterior way to remove the bulb wall and vitreous body, peel off the zonule, take out th...

Embodiment 3

[0091] Embodiment 3 and commercially available Bendalysine eye drops (No. 5) comparative test on eye irritation

[0092] 1 Materials and methods

[0093] 1.1 Test samples and reagents

[0094] In vitro test: Compounds No. 1-9 of the test samples, including Bendalysine as the reference substance, were formulated with 0.9% wtNaCl to a concentration of 70mmol / L. A 0.9% wtNaCl solution was used as a control test, and all chemical reagents used were of analytical grade. Compound No. 1-5 in vivo test: all were prepared with 0.9% wtNaCl to prepare colorless and clear eye drops with a specification of 5 mL: 25 mg. No. 6-9 have not been tested in vivo.

[0095] 1.2 Animals and instruments

[0096] Chicken embryos aged 10 days were provided by Nanjing Nanjiao Breeding Chicken Factory. 21 New Zealand big-eared white rabbits, weighing 2.5±3.0kg, both male and female. Provided by the Experimental Animal Center of Nanjing Medical University. OLYMPUS inverted microscope, Queue carbon ...

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Abstract

The invention aims to provide application of organic dicarboxylic acid salts, namely new application in pharmacy, in particular application in preparing medicaments for preventing and treating cataract. New anti-cataract active components in No.1, No.2, No.3, No.4, No.6, NO.7, No.8 and No.9 compounds are discovered by screening rabbit and rat H2O2 induced cataract and rat xylose induced cataract models, and the medical application of the compounds in preparing the medicaments for resisting oxidative damage and sugar metabolism disorder induced cataract is discovered. The No.4 compound has strong and high effect of resisting phacoscotasmus, and has good medicinal prospect. The No.4 compound has obvious effects of improving rabbit lens water-soluble proteins (sol-pro) and total antioxidant capacity (T-AOC), and reducing malondialdehyde (MDA), so the effect of the No.4 compound of resisting H2O2 induced lens oxidative damage is related to the strong oxidation resistance of the No.4 compound.

Description

technical field [0001] The present invention relates to the use of a class of organic dicarboxylates, in particular to the application of a class of organic dicarboxylates in preparing medicines for preventing and treating cataracts. Background technique [0002] Benzyl lysine: chemical name: L-lysine [1-benzyl-1H-indazol-3-oxyl] acetate L-lysine-mono[[[(1-phenylmethyl)-1H- indazol-3-yl]oxy]acetat] English name Bendazac Lysine (BDL). After extensive animal experiments and clinical studies in foreign countries, BDL was first listed in Italy (1983) by Anglini Pharmaceutical Group as an effective drug for treating cataract. There are two kinds of 0.5g tablet and 0.5% eye drops. The drug has obtained production licenses in Italy, Argentina, Spain, Portugal, and the Philippines, and is registered or undergoing clinical research in Greece, Brazil, and South Korea. [0003] The drug's raw materials and eye drops (trade name: Shapuaisi) obtained the new drug certificate and produc...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/416A61P27/12
Inventor 张银娣苟少华沈建平朱延勤冯鲁中沈宏吴建伟胡正国陈德康
Owner ZHEJIANG SHAPUAISI PHARMA
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