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Difluprednate ophthalmic emulsion and preparation method thereof

A technology for difluprednate and ophthalmic use, which is applied in the field of difluprednate-containing ophthalmic emulsion and its preparation, and can solve the problems of epithelial cell shedding and the like

Inactive Publication Date: 2016-04-20
BEIJING LANDAN PHARMA TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Currently commonly used preservatives for ophthalmic preparations are mainly divided into quaternary ammonium salts, mercury agents, alcohols, carboxylic acids, phenols, and ethylenediaminetetraacetic acid salts according to their chemical structures, among which benzalkonium chloride (BAC) is The most commonly used quaternary ammonium salt broad-spectrum fungicide, but as early as 1941, Swan confirmed that 0.04% BAC can cause punctate inflammation of the corneal epithelium, and 0.1% BAC can cause corneal edema and epithelial cell shedding

Method used

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  • Difluprednate ophthalmic emulsion and preparation method thereof
  • Difluprednate ophthalmic emulsion and preparation method thereof
  • Difluprednate ophthalmic emulsion and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] prescription:

[0036] Raw materials

Dosage

%w / v

difluprednate

0.5g

0.05

castor oil

50g

5

Tween 80

40g

4

Glycerin

22g

2.2

Sodium acetate

0.5g

0.05

boric acid

1g

0.1

Polyquaternium-1

0.01g

0.001

sodium hydroxide

Appropriate amount

water

Add water to 1000ml

[0037] crafting process:

[0038] (1) Oil phase preparation: heat castor oil to about 70°C, add difluprednate, stir to dissolve, and use it as the oil phase.

[0039] (2) Water phase preparation: heat water to about 70° C., add Tween-80, glycerin, sodium acetate, boric acid, polyquaternium-1, stir to dissolve, and use as the water phase.

[0040] (3) Preparation of colostrum: add the oil phase obtained in the step (1) into the water phase obtained in the step (2), disperse at high speed for 10 minutes, and the shear rate is 10000 rpm to form colostrum a...

Embodiment 2

[0052] prescription:

[0053] Raw materials

Dosage

%w / v

difluprednate

0.5g

0.05

castor oil

50g

5

Tween 80

40g

4

Glycerin

22g

2.2

Sodium acetate

0.5g

0.05

boric acid

1g

0.1

Edetate Disodium

0.2g

0.02

Polyquaternium-1

0.01g

0.001

sodium hydroxide

Appropriate amount

4 -->

water

Add water to 1000ml

[0054] crafting process:

[0055] (5) Oil phase preparation: heat castor oil to about 70° C., add difluprednate, stir to dissolve, and use it as the oil phase.

[0056] (6) Preparation of water phase: Heat water to about 70°C, add Tween-80, glycerin, sodium acetate, boric acid, disodium edetate, polyquaternium-1, stir to dissolve, and use as water phase.

[0057] (7) Preparation of colostrum: add the oil phase obtained in the step (1) into the water phase obtained in the step (2), disperse at high speed for 1...

Embodiment 3

[0060] prescription:

[0061] Raw materials

Dosage

%w / v

difluprednate

0.5g

0.05

castor oil

50g

5

Tween 80

40g

4

Glycerin

22g

2.2

Sodium acetate

0.5g

0.05

boric acid

1g

0.1

Edetate Disodium

0.2g

0.01

Polyquaternium-1

0.01g

0.0005

sodium hydroxide

Appropriate amount

water

Add water to 1000ml

[0062] crafting process:

[0063] (1) Oil phase preparation: heat castor oil to about 70°C, add difluprednate, stir to dissolve, and use it as the oil phase.

[0064] (2) Preparation of water phase: Heat water to about 70°C, add Tween-80, glycerin, sodium acetate, boric acid, disodium edetate, polyquaternium-1, stir to dissolve, and use as water phase.

[0065] (3) Preparation of colostrum: add the oil phase obtained in the step (1) into the water phase obtained in the step (2), disperse at high speed for 10 mi...

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Abstract

The invention relates to a difluprednate ophthalmic emulsion. The difluprednate ophthalmic emulsion is prepared from difluprednate, oil, an emulsifier and a preservative, wherein the preservative contains polyquaternium-1, and the dosage of the polyquaternium-1 is 0.0005 to 0.01 percent w / v. According to the difluprednate ophthalmic emulsion disclosed by the invention, the novel preservative, namely the polyquaternium-1, basically has no damage effect on cornea and ocular surface tissues, and secondary injury on a patient cannot be caused while the pharmacological effect is achieved.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to an ophthalmic emulsion containing difluprednate and a preparation method thereof. Background technique [0002] Difluprednate, also known as difluprednate or defluprednate, belongs to adrenocortical hormone drugs and is a difluoro derivative of prednisolone, which has strong anti-inflammatory and analgesic effects. Inflammatory responses triggered by a variety of stimuli can delay wound healing, and corticosteroids can reduce inflammation-related edema, fibrin deposition, capillary dilatation, leukocyte migration, capillary hyperplasia, fibroblast proliferation, collagen deposition, and scarring Form etc. At present, the mechanism of action on ophthalmic topical is not clear, it is generally believed that it is through the inhibition of phosphatase A 2 And play an anti-inflammatory effect. Inhibits phosphatase A 2 It can inhibit the release of arachidonic acid, the ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/107A61K31/573A61K47/34A61P29/00A61P27/02
CPCA61K9/0048A61K9/107A61K31/573A61K47/34
Inventor 不公告发明人
Owner BEIJING LANDAN PHARMA TECH
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