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Application of haematopophyrin in treating ophthalmic disease

A technology of hematoporphyrin monomethyl ether and ophthalmic diseases, applied in the field of medicine, can solve the problems of unsatisfactory treatment effect and the like

Inactive Publication Date: 2005-03-09
上海复旦张江生物医药股份有限公司 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, its therapeutic effect is still unsatisfactory

Method used

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  • Application of haematopophyrin in treating ophthalmic disease
  • Application of haematopophyrin in treating ophthalmic disease
  • Application of haematopophyrin in treating ophthalmic disease

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0056] Embodiment 1: Preparation of hematoporphyrin monomethyl ether and therapeutic agent

[0057] A. Preparation of Hematoporphyrin Monomethyl Ether

[0058] By the method described in the Chinese patent application of CN 01131939, with 20 grams of 3,8-two (1-bromoethyl) hypoporphyrin IX hydrobromide and 3000 milliliters of methanol / water mixed solution stirring reaction 2 hours, The pH of the reaction solution was adjusted to 13 with 10 mol / L sodium hydroxide, stirred for 4 hours, and then the pH of the reaction solution was adjusted to 4-5 with glacial acetic acid to precipitate out. The separated precipitate was collected by Buchner funnel, washed with water and dried to obtain 19.5 g of crude product. Purify through silica gel column chromatography to obtain 3.9 grams of hematoporphyrin monomethyl ether ( figure 1 ).

[0059] Repeat the above steps to obtain about 20 grams of hematoporphyrin monomethyl ether.

[0060] B. Preparation of Therapeutic Agents

[0061] Ta...

Embodiment 2

[0062] Embodiment 2: CAM model is used for photodynamic therapy effect determination in vivo

[0063] The establishment of the CAM model adopts the following method: 37 ℃ incubator, the air chamber is upward, rotate 3 to 4 times a day, until the 9th day of hatching, disinfect the surface of the egg and make a small hole of 1 to 2 mm on the top of the air chamber, and place it at a distance from the fetal head. Mark a rectangular area of ​​1.0 cm × 1.5 cm on the projected part of the egg shell in the first 1 cm and between the two anterior yolk veins, grind and cut through the egg shell, and gently scratch a small hole with a diameter of about 1 mm on the egg shell membrane. A little sterile pure water was added dropwise to separate the eggshell membrane at the edge of the small hole, and a sterile microporous filter membrane carrier with a diameter of 6 mm was placed on the part of the CAM where the blood vessels were least.

[0064] Then 10 ul of hematoporphyrin monomethyl et...

Embodiment 3

[0066] Embodiment 3: the establishment of CNV mouse model

[0067] The CNV model was established as follows: randomly select 20 adult male C57BL-6J mice with a body weight of 25g-26g. Mice were anesthetized by intraperitoneal injection of 200 μL of 0.3% pentobarbital sodium, 2% tropicamide and 10% phenylephrine to dilate the pupils. Laser light (wavelength 810nm, diameter 75μm, irradiation time 0.1s, power 140mW) was introduced into the eyes of mice through a slit lamp and a contact lens. Fundus fluorescence angiography (FFA) was performed 1 week after laser irradiation, and the photocoagulation point was selected without fluorescence leakage, and the photocoagulation point was milky white (such as Figure 4 ) of 9 animals, the tissue section was observed to confirm the membrane formation or further photodynamic therapy test was carried out.

[0068] One of the above-mentioned animals was killed by excessive sodium pentobarbital, the eyeballs were removed, fixed in 2% glutar...

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Abstract

An application of hematopropyrin monomethylether as a photosensitizer in treating ophthalmopathy by photodynamic therapy is disclosed. Said diseases may be yellow spot degeneration, eye histoplasmosis, myopia, etc.

Description

technical field [0001] The invention relates to the field of medicine, and more specifically relates to the application of hematoporphyrin monomethyl ether to treat ophthalmic diseases by applying photodynamic therapy (PDT) to eyes. Background technique [0002] Vision loss is a common problem that accompanies aging and various eye diseases. Aging and other etiologies often lead to the development of harmful new blood vessels in the cornea, iris, retina, or choroid, resulting in decreased or even loss of vision. In many known eye diseases, including macular degeneration, ocular histoplasmosis syndrome, myopia, and inflammatory diseases, choroidal neovascularization leads to hemorrhage and fibrosis, ultimately with vision loss. [0003] Age-related macular degeneration (AMD) is the main cause of vision loss in the elderly, and 10% of AMD patients are accompanied by choroidal neovascularization, resulting in rapid vision loss. According to statistics, 80% of new blindness ca...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/40A61P27/02
CPCC07D487/22A61K31/40A61P27/02A61P27/10
Inventor 陈文辉陶纪宁熊乾斌许德余李军苏勇
Owner 上海复旦张江生物医药股份有限公司
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