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Rapamycin microemulsion injection for eyes and preparation method and application thereof

A technology of rapamycin and injection, applied in the field of rapamycin ophthalmic microemulsion injection and its preparation, can solve the problems of lack of theoretical knowledge of age-related macular degeneration and other types of retinal degenerative diseases

Inactive Publication Date: 2011-04-13
赵晨
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, there is no Rapamycin ophthalmic microemulsion injection in the world, nor any theoretical knowledge, reports or attempts about Rapamycin in the treatment of age-related macular degeneration and other types of retinal degenerative diseases

Method used

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  • Rapamycin microemulsion injection for eyes and preparation method and application thereof
  • Rapamycin microemulsion injection for eyes and preparation method and application thereof
  • Rapamycin microemulsion injection for eyes and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0048] Rapamycin original drug provided by Tianjin Xinmei Technology Co., Ltd.

[0049] Prescription: Rapamycin (rapamycin) 1.00g;

[0050] 10.0ml soybean oil;

[0051] Tween-80 80.0ml;

[0052] Polyethylene glycol-400 64.0ml;

[0053] Appropriate amount of sterile water for injection;

[0054] The total amount prepared: 1000ml, the measured pH value is 7, the osmotic pressure: the osmotic pressure of 0.9% sodium chloride solution.

[0055] Process:

[0056] Precisely weigh Rapamycin, put it in a mortar, add soybean oil and Tween-80, grind it thoroughly until the powder is dissolved, and mix well; take another amount of PEG-400 and add it to 800ml sterile water for injection, boil to dissolve, stir to mix After uniformity, pour it into the above mixed solution, stir rapidly, adjust the volume to 1000ml with sterilized water for injection, filter through a 0.45 μm microporous membrane after mixing, and pack aseptically to obtain the product.

Embodiment 2

[0058] Rapamycin original drug provided by Tianjin Xinmei Technology Co., Ltd.

[0059] Prescription: Rapamycin (rapamycin) 1.15g;

[0060] 8.0ml soybean oil;

[0061] Tween-80 90.0ml;

[0062] Polyethylene glycol-400 70.0ml;

[0063] Appropriate amount of sterile water for injection;

[0064] The total amount prepared: 1000ml, the measured pH value is 6.5, the osmotic pressure: the osmotic pressure of 0.8% sodium chloride solution.

[0065] Process:

[0066] Precisely weigh Rapamycin, put it in a mortar, add soybean oil and Tween-80, grind it thoroughly until the powder is dissolved, and mix well; take another amount of PEG-400 and add it to 700ml sterile water for injection, boil to dissolve, stir to mix After uniformity, pour it into the above mixed solution, stir rapidly, adjust the volume to 1000ml with sterilized water for injection, filter through a 0.45 μm microporous membrane after mixing, and pack aseptically to obtain the product.

Embodiment 3

[0068] Rapamycin original drug provided by Tianjin Xinmei Technology Co., Ltd.

[0069] Prescription: Rapamycin (rapamycin) 0.85g;

[0070] 12.0ml soybean oil;

[0071] Tween-80 70.0ml;

[0072] Polyethylene glycol-400 58.0ml;

[0073] Appropriate amount of sterile water for injection;

[0074] Preparation volume: 1000ml, measured pH value is 7.5, osmotic pressure: 1.0% sodium chloride solution osmotic pressure.

[0075] Process:

[0076] Precisely weigh Rapamycin, put it in a mortar, add soybean oil and Tween-80, grind it thoroughly until the powder is dissolved, and mix well; take another amount of PEG-400 and add it to 800ml sterile water for injection, boil to dissolve, stir to mix After uniformity, pour it into the above mixed solution, stir rapidly, adjust the volume to 1000ml with sterilized water for injection, filter through a 0.45 μm microporous membrane after mixing, and pack aseptically to obtain the product.

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Abstract

The invention discloses rapamycin microemulsion injection for eyes and a preparation method and application thereof. In the injection, rapamycin is taken as an active ingredient and is added with a pharmaceutically acceptable carrier, and each 1,000ml of preparation contains 0.05 to 20g of rapamycin. The microemulsion injection for eyes has low cost and high stability, does not have obvious irritation and toxic or side effect on the eyes, can be used for treating retinal degenerative diseases, and particularly has obvious effect of treating age-related macular degeneration disease. The treatment effect of the injection is provided on the basis of breakthrough and discovery of a pathogenic mechanism, and the rapamycin microemulsion injection has profound significance for treating the diseases.

Description

technical field [0001] The invention belongs to the field of pharmacy, and in particular relates to a rapamycin ophthalmic microemulsion injection and a preparation method and application thereof. Background technique [0002] Blinding eye disease is the third most affecting human disease assessed by WHO, and the most important one is retinal degenerative disease. Retinal degeneration is a large group of diseases characterized by progressive loss of photoreceptor cells, which can be divided into hereditary retinal degeneration caused by obvious genetic defects and complex retinal degeneration caused by multiple factors. Age-related macular degeneration (AMD) is the most common complex retinal degenerative disease, especially as the population ages, its incidence is increasing, and there are more than 10 million patients in the United States alone. AMD can be caused by age-related factors such as genetic factors, smoking, oxidative damage, and mitochondrial defects. Patients...

Claims

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Application Information

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IPC IPC(8): A61K9/107A61K31/436A61P9/10A61P27/02
Inventor 赵晨赵堪兴刘美欣
Owner 赵晨
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