Cyclosporine compound eye drops and preparation method thereof

A technology of cyclosporine and eye drops, which is applied in the direction of cyclic peptide components, pharmaceutical formulas, emulsion delivery, etc., can solve the problems of poor interaction stability of nano-suspensions, and achieve good pharmacokinetic data and specific area Increases the effect of tear secretion

Active Publication Date: 2018-05-08
NKD PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, in terms of cyclosporine ophthalmic compound preparations, the nanosuspension obtained according to conventional preparation methods has problems such as two drug interactions and poor stability.

Method used

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  • Cyclosporine compound eye drops and preparation method thereof
  • Cyclosporine compound eye drops and preparation method thereof
  • Cyclosporine compound eye drops and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1、025

[0049] The preparation of embodiment 1,0.25% cyclosporine compound eye drops (nanosuspension)

[0050] prescription

[0051]

[0052]

[0053] Preparation:

[0054] (1) Weigh 65g of poloxamer and dissolve it in 500mL of water for injection, add 50g of cyclosporine, stir and suspend evenly, then transfer to a wet grinding machine, using 0.6-0.8mm zirconia balls as the grinding medium, 1500rpm Grind for 20 minutes to obtain a nano-suspension, the average particle size of which is 850nm through particle size testing;

[0055] (2) Weigh 100g of moxifloxacin hydrochloride, 110g of hydroxypropyl methylcellulose, 180g of sorbitol, 85g of boric acid, 55g of borax, add 4L of water for injection, stir, dissolve and mix evenly, and filter through a 0.22μm filter membrane to obtain Inflammatory or antibiotic drug aqueous solution;

[0056] (3) Mix the cyclosporin nanosuspension prepared in step (1) with the anti-inflammatory or antibiotic drug aqueous solution obtained in step (2...

Embodiment 2、1

[0058] The preparation of embodiment 2, 1% cyclosporine compound eye drops (nanosuspension)

[0059] prescription

[0060] Cyclosporine

200g

Dexamethasone Sodium Phosphate

4.0g

Span 80

145g

Polyvinylpyrrolidone K30

400g

Mannitol

350g

glycerin

240g

sodium hydroxide

Appropriate amount

Water for Injection

Add to 20L

[0061] Preparation:

[0062] (1) Weigh 145g of Span 80 and dissolve it in 1L of water for injection, add 200g of cyclosporine, stir and suspend evenly, transfer to a wet grinding machine, use 0.6-0.8mm zirconia balls as the grinding medium, and grind at 3000rpm After 60 minutes, the nanosuspension was obtained, and the average particle diameter was 450nm through the particle size test;

[0063] (2) Weigh 4.0g of dexamethasone sodium phosphate, 400g of polyvinylpyrrolidone K30, 350g of mannitol, 240g of glycerin, add 10L of water for injection, stir to dissolve and mix evenly, ...

Embodiment 3

[0066] The preparation of embodiment 3, 0.05% cyclosporine compound eye drops (nanosuspension)

[0067] prescription

[0068] Cyclosporine

10g

Indomethacin

100g

Tween 80

25g

polyethylene glycol 4000

90g

Sodium chloride

86g

citric acid

12g

sodium hyaluronate

100g

Water for Injection

Add to 20L

[0069] Preparation:

[0070] (1) Weigh 25g of Tween 80 and dissolve it in 200mL of water for injection, add 10g of cyclosporine, stir and suspend evenly, and homogenize under 1000bar high pressure 12 times to obtain a nanosuspension, the average particle diameter of which is 235nm through particle size testing; The distribution is narrower, 150-300nm, in contrast, the API particles are larger, and the particle size distribution range is wider, 1-30μm.

[0071] (2) Weigh 100g of indomethacin, 90g of polyethylene glycol 4000, 86g of sodium chloride, 12g of citric acid, add 5L of water for injection, ...

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Abstract

The invention relates to a cyclosporine-containing composition and a preparation method thereof. The compound eye drops are prepared from cyclosporine, anti-inflammatory or antibiotic drugs, a surfactant, a stabilizer, a thickener, an isoosmotic adjusting agent, a pH adjusting agentr and water or oil, the preparation is a mixed suspension agent or an emulsion, and one or two of a high pressure homogenization method and a wet grinding technique is/are combined for use in the preparation method. The cyclosporine compound eye drops have the advantages that the ophthalmic tolerance is excellent, the drug utilization degree is high, the tear secretion of people suffering from xerophthalmia can be effectively improved, the tear film is stabilized, the anti-inflammation function of the anti-inflammatory or antibiotic drugs and the immunoregulation function of cyclosporine can be synergistically exerted, xerophthalmia can be effectively treated, and the compound eye drops have a better treatment effect compared with the separate application of cyclosporine.

Description

technical field [0001] The invention relates to a compound pharmaceutical preparation and a preparation method thereof, in particular to a cyclosporin compound eye drop and a preparation method thereof, belonging to the field of pharmaceuticals. Background technique [0002] With the rapid development and popularization of video terminals such as mobile phones and computers, the incidence of dry eye disease, which is clinically manifested as eye discomfort, tear film instability, visual disturbance and ocular surface inflammation, is increasing year by year. According to reports, the global incidence of dry eye is 5.5%-33.7%, while the incidence in my country is 21%-30%. The incidence is relatively high, which has brought a great impact on the lives of patients. Studies have shown that dry eye syndrome is caused by the secretion of lacrimal glands in the aqueous layer, secretion of the oil layer, insufficient secretion of the mucin layer, excessive evaporation of tears, unev...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K45/06A61K9/107A61K38/12A61K31/4709A61K31/661A61K31/405A61K31/7052A61P27/02
CPCA61K9/0048A61K9/1075A61K31/405A61K31/4709A61K31/661A61K31/7052A61K38/12A61K45/06A61K47/10A61K47/26A61K47/38A61K2300/00
Inventor 张志兵陶秀梅陈鹏尚丽霞
Owner NKD PHARMA CO LTD
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