Ocular surface applied medicament for treating eyes immunological disease and inhibiting proliferation and neovascularization

A technology for immune diseases and new blood vessels, applied in the field of ophthalmic pharmaceutical preparations, can solve problems such as inability to treat ophthalmic diseases

Active Publication Date: 2007-05-23
洪晶 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In the application documents of the patent, the applicant specifically pointed out that when the concentration of immunosuppressant drugs in the eye is very low, it cannot treat ophthalmic immune-related diseases.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0015] Embodiment 1 eye drops

[0016] Prescription: Rapamycin 0.01, 0.02, 0.05, 0.1, 0.2, 0.5, 0.9, 2g

[0017] Ethylparaben 0.03g

[0018] Add vitamin E, vitamin A or evening primrose oil to 100ml

[0019] Process: Dissolve ethylparaben with vitamin E, vitamin A or evening primrose oil, and let it cool. Take another rapamycin plus vitamin E, vitamin A or evening primrose oil to dissolve. Combine the two solutions, add vitamin E, vitamin A or evening primrose oil to a sufficient amount.

[0020] Stability test of rapamycin eye drops:

[0021] in CH 3 COOK.1.5H 2 O saturated solution, adjust relative humidity 22.5%, temperature 25 ℃, carry out 2% rapamycin eye drop stability investigation, HPLC measures rapamycin content, the result is as follows: 2% rapamycin eye drop stores 6 Monthly inspection results

[0022] Time 1 month 2 months 3 months 6 months

[0023] Rapamycin content 2.04% 2.04% 2.04% 2.02%

[0024] PH 6.4 6.4 6.4 6.6

[0025] Appearance inspection Compl...

Embodiment 2

[0027] Example 2 Gel

[0028] Prescription: Rapamycin 0.5, 1g respectively

[0029] Ethylparaben 0.03g

[0030] Carbomer 2g

[0031] Distilled water to 100ml

[0032] Process: heat ethyl paraben with sterilized distilled water and let it cool; take carbomer, add appropriate amount of distilled water, wait until the swelling is complete, and set aside; take rapamycin and add a small amount of absolute ethanol to dissolve. Combine the above solutions, stir until uniform, and add distilled water to a sufficient amount.

Embodiment 3

[0033] Embodiment 3 eye ointment

[0034] Prescription: Rapamycin 2g

[0035] Ethylparaben 0.03g

[0036] Liquid paraffin 3g

[0037] Anhydrous lanolin 10g

[0038] Yellow Vaseline 85g

[0039] Process: Add ethylparaben and rapamycin to liquid paraffin that has been sterilized, filtered and cooled, stir evenly, and then add to vaseline that has been dry-heat sterilized, filtered and cooled to about 50°C Stir well with lanolin and solidify.

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PUM

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Abstract

The invention relates to a drug used to treat eye immunity disease and restrain increment and new blood vessel, wherein it uses rapamycin as active component at 0.01-2% mass. And the invention can be used to treat Sj gren disease, Mooren ulcer, etc.

Description

Technical field: [0001] The present invention relates to ophthalmic pharmaceutical preparations, and in particular provides an ocular surface drug that uses rapamycin as the main active ingredient to treat ocular immune diseases, treat ocular immune diseases, and inhibit proliferation and neovascularization. medicine. Background technique: [0002] Ocular immune disease is a refractory eye disease in ophthalmology. At present, the topical ophthalmic drugs mainly include corticosteroids and cyclosporine A. On the one hand, some diseases cannot be effectively controlled. On the other hand, long-term application of corticosteroids can cause glaucoma and cataracts. , secondary infection and other serious hazards to eye health. Immune rejection after keratoplasty is also an immune disease in a broad sense. Corneal transplantation is an important sight restoration operation for corneal blindness, and it is also the main measure for treating some stubborn corneal lesions. Of all ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/436A61K9/00A61K9/06A61K9/107A61P27/02
Inventor 洪晶李兵
Owner 洪晶
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