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Composition containing ursodeoxycholic acid for prevention or treatment of visual impairment

一种熊去氧胆酸、视力障碍的技术,应用在药物组合物,预防或治疗视力障碍的组合物领域,达到促进恢复、消除疼痛和恐惧、抑制发展的效果

Inactive Publication Date: 2019-08-27
LIUS BIOPHARMACEUTICALS
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

So far, no one has attempted to deliver UDCA / tUDCA across the blood-retinal barrier to the inner eyeball by oral administration or intravitreal injection to protect the retina and prevent or treat visual impairment

Method used

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  • Composition containing ursodeoxycholic acid for prevention or treatment of visual impairment
  • Composition containing ursodeoxycholic acid for prevention or treatment of visual impairment
  • Composition containing ursodeoxycholic acid for prevention or treatment of visual impairment

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0215] (Example 1) The weight ratio of UDCA and maltodextrin is the clarified aqueous solution of 1:6

[0216] A clear aqueous stock solution of water-soluble UDCA containing native UDCA and low dextrose equivalent water-soluble starch was prepared.

[0217] Specifically, 6.7 g of sodium hydroxide granules were dissolved in 400 ml of purified water. 60 g of UDCA were dissolved in sodium hydroxide solution at room temperature while stirring. 360 g of maltodextrin were slowly added to the clear solution while stirring. Preservatives were then added to the clear solution obtained by sonication at high throughput (750 W, 20 kHz) in an amount suitable for pharmaceutical formulations, and the pH was adjusted by the dropwise addition of HCl. Add purified water and adjust to a total of 1000ml. Filter the clear solution through a suitable filter unit if necessary. This filtration is important to remove impurities from the raw material or to sterilize it, but since the solution is a...

Embodiment 2

[0218] (Example 2) The weight ratio of UDCA and maltodextrin is the clarified aqueous solution of 1:12

[0219] A clear aqueous stock solution of water-soluble UDCA containing native UDCA and low dextrose equivalent water-soluble starch was prepared.

[0220]Specifically, it was prepared according to the same procedure as in Example 1, except that 720 g of maltodextrin, which is a high molecular weight water-soluble starch conversion product, was used per 60 g of ursodeoxycholic acid. As shown in Table 3, the prepared ursodeoxycholic acid solutions formed clear aqueous solutions without any visually visible precipitate at pH 9.6, 7.3, 6.5 and 6.0, but formed a precipitate at pH 5.5.

Embodiment 3

[0221] (Example 3) The weight ratio of UDCA and maltodextrin is the clarified aqueous solution of 1:15

[0222] A clear aqueous stock solution of water-soluble UDCA containing native UDCA and low dextrose equivalent water-soluble starch was prepared.

[0223] Specifically, it was prepared according to the same procedure as in Example 1, except that 750 g of maltodextrin, which is a high molecular weight water-soluble starch conversion product, was used per 50 g of ursodeoxycholic acid. Dissolve 5.7 g of sodium hydroxide granules in 400 ml of purified water and use. As shown in Table 3, the prepared ursodeoxycholic acid solutions formed clear aqueous solutions with no visually visible precipitate at pH 9.5, 8.9, 7.9, 7.1 and 6.0, but formed a precipitate at pH 5.5. figure 1 is a graph showing whether a clear aqueous solution of ursodeoxycholic acid was formed at each pH value.

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PUM

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Abstract

The present invention relates to a composition containing ursodeoxycholic acid (UDCA) for prevention or treatment of visual impairment. More specifically, the present invention relates to a pharmaceutical composition, which allows oral administration, intraocular injection, or eye drop administration, by aqueous solubilized ursodeoxycholic acid, leading to excellent prevention or treatment effectsof visual impairment-causing diseases, such as macular degeneration, glaucoma, and diabetic retinopathy.

Description

technical field [0001] The present disclosure relates to a composition for preventing or treating visual impairment containing ursodeoxycholic acid (UDCA). More specifically, the present disclosure relates to a pharmaceutical composition, which can be administered orally, intravitreal injection, intravenous injection or eye drops through water-soluble ursodeoxycholic acid, and is effective for vision disorders such as macular degeneration, Prevention or treatment of glaucoma and diabetic retinopathy is excellent. Background technique [0002] Macular degeneration, glaucoma, and diabetic retinopathy are the three most common eye diseases that cause blindness. The leading cause of blindness is age-related eye disease associated with an aging society. According to a 2006 study in the United Kingdom, these three most common forms of blindness accounted for approximately 74% of all blindness. [0003] About 2 percent of adults age 40 and older have glaucoma. Glaucoma is an ey...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/575A61K31/718A61K45/06A61K9/00A61K9/08
CPCA61K31/575A61P27/02A61K9/0048A61K9/0019A61K47/36A61K9/00A61K9/08A61K31/718A61K45/06A61K47/26A61K2300/00A61P27/00A61K9/0053A61K39/3955
Inventor 宋永镐高煇进
Owner LIUS BIOPHARMACEUTICALS
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