Quercetin eye drops and preparation method thereof

A technology of quercetin and eye drops, which is applied in the direction of medical formulas, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., which can solve the problems of poor patient compliance, increased dosage, and increased toxic and side effects and other issues, to achieve the effects of small toxic and side effects, good biocompatibility, and good social and economic benefits

Active Publication Date: 2018-05-29
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In order to achieve the therapeutic dose of the drug across the cornea, it is usually necessary to increase the dose, which will lead to increased toxicity and poor patient compliance

Method used

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  • Quercetin eye drops and preparation method thereof
  • Quercetin eye drops and preparation method thereof
  • Quercetin eye drops and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] Example 1 Screening of the preparation method of quercetin hydroxypropyl-β-cyclodextrin inclusion compound

[0030] Taking the quercetin drug loading as an index, the process of screening the quercetin hydroxypropyl-β-cyclodextrin inclusion compound preparation process is as follows:

[0031] Preparation of quercetin hydroxypropyl-β-cyclodextrin inclusion compound by solvent method: weigh 0.5% quercetin and 10% hydroxypropyl-β-cyclodextrin, quercetin Fully dissolve with methanol at 65°C, fully dissolve hydroxypropyl-β-cyclodextrin and water for injection at 65°C, add quercetin methanol solution dropwise to hydroxypropyl-β-cyclodextrin at a speed of 2ml / min -In the cyclodextrin aqueous solution, heat and reflux at 65°C for 10h, then stir at room temperature for 10h, use a rotary evaporator, control the temperature at 50°C, and control the pressure at 11-21KPa, evaporate for 30min to completely remove the solvent, dilute with water for injection to volume According to th...

Embodiment 2

[0035] Example 2 Prescription of Quercetin Eye Drops with Different Proportions of Hydroxypropyl-β-cyclodextrin

[0036] Raw materials

Dosage

%w / v

quercetin

3g

0.3％

Hydroxypropyl-β-cyclodextrin

70g

7％

Thiolated Chitosan

1g

0.1％

Benzalkonium Bromide

0.05g

0.005％

Sodium chloride

Appropriate amount

Borate Buffer Saline

Appropriate amount

Water for Injection

Add water for injection to 1000ml

[0037]crafting process:

[0038] (1) take quercetin and hydroxypropyl-β-cyclodextrin of prescription quantity by weighing;

[0039] (2) Fully dissolve quercetin and methanol at 65°C, fully dissolve hydroxypropyl-β-cyclodextrin and water for injection at 65°C, add quercetin methanol solution dropwise at a rate of 2ml / min Into the hydroxypropyl-β-cyclodextrin aqueous solution, heated to reflux at 65°C for 10h, and stirred at room temperature for 10h.

[0040] (3) Use a rotar...

Embodiment 3

[0043] Example 3 Prescription of Quercetin Eye Drops with Different Proportions of Hydroxypropyl-β-cyclodextrin

[0044]

[0045]

[0046] crafting process:

[0047] (1) take quercetin and hydroxypropyl-β-cyclodextrin of prescription quantity by weighing;

[0048] (2) Fully dissolve quercetin and methanol at 65°C, fully dissolve hydroxypropyl-β-cyclodextrin and water for injection at 65°C, add quercetin methanol solution dropwise at a rate of 2ml / min Into the hydroxypropyl-β-cyclodextrin aqueous solution, heated to reflux at 65°C for 10h, and stirred at room temperature for 10h.

[0049] (3) Use a rotary evaporator, control the temperature at 50°C and the pressure at 20KPa, evaporate for 15 minutes to completely remove the solvent, dilute with water for injection to 1000ml, add thiolated chitosan, and continue stirring for 30 minutes.

[0050] (4) Add the benzalkonium bromide of prescription quantity, add appropriate amount of sodium chloride to adjust osmotic pressure...

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Abstract

The invention belongs to the technical field of the medicine, relates to quercetin eye drops and a preparation method thereof, and specifically relates to quercetin hydroxypropyl-beta-cyclodextrin inclusion compound eye drops. The quercetin eye drops is prepared from the following components in weight volume percent: 0.1%-0.8% of quercetin, 0.025%-0.3% of penetration enhancer, 7%-30% of hydroxypropyl-beta-cyclodextrin, 0.005%-0.02% of bacteriostatic agent, 0.6%-1.5% of isoosmotic adjusting agent, 0.001%-0.05% of pH regulator, and the balance of water for injection. The penetration enhancer isone of the thiolated chitosan, chitosan or cell-permeable peptide (R8). The penetration enhancer is combined with the inclusion compound of the hydroxypropyl-beta-cyclodextrin of the quercetin to prepare the eye drops with good effect of preventing and treating cataract; the eye drops has the advantages of being good in cornea permeability, high in bioavailability, good in biocompatibility, and small in eye irritation, and has extensive development prospect.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and relates to a quercetin eye drop and a preparation method thereof, in particular to an eye drop containing quercetin in hydroxypropyl-β-cyclodextrin. The eye drop is suitable for For ophthalmic applications, especially for the prevention and treatment of cataracts. Background technique [0002] The structural formula of quercetin is as follows [0003] [0004] Quercetin belongs to flavonoids. In addition to antibacterial, anti-inflammatory, and cardiovascular disease prevention effects, quercetin can also maintain lens transparency, resist oxidation, inhibit lens aldose reductase activity, resist apoptosis, and regulate lens epithelial cell genes. Expression and other aspects also have significant effects, and have the effect of delaying the occurrence and development of cataract. Quercetin has very poor water solubility and has been prepared into eye drops such as li...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/08A61K31/352A61K47/36A61K47/42A61K47/69A61P27/12A61P27/02
CPCA61K9/0048A61K9/08A61K31/352A61K47/36A61K47/42
Inventor 姜同英王思玲兰琪
Owner SHENYANG PHARMA UNIVERSITY
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