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A kind of azithromycin gel eye drop and its preparation process

Azithromycin and its preparation technology are applied in medical preparations containing non-active ingredients, medical preparations containing active ingredients, organic active ingredients, etc., and can solve the problems of low bioavailability, short residence time, and poor drug absorption, etc. , to achieve the effects of reducing drug loss, increasing residence time, and delaying drug release

Active Publication Date: 2011-12-21
北京乐维生物技术有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] The invention discloses azithromycin gel-type eye drops and a preparation process thereof, aiming at providing clinically practical, convenient and reliable ophthalmic preparations for treating bacterial conjunctivitis, and solving the problem of eye drop-type drugs in the eyes. Short residence time, poor drug absorption, low bioavailability, etc.

Method used

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  • A kind of azithromycin gel eye drop and its preparation process
  • A kind of azithromycin gel eye drop and its preparation process
  • A kind of azithromycin gel eye drop and its preparation process

Examples

Experimental program
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Effect test

Embodiment 1

[0032] Example 1: Weigh 0.15 g of azithromycin and dissolve it with an appropriate amount of citric acid-sodium citrate buffer, then add 4.0 g of sodium chloride, 0.1 g of disodium edetate, and 0.05 g of thimerosal solution to the above-mentioned drug solution, and then add Add an appropriate amount of water for injection to dissolve by ultrasonic; add 0.01g of polycarbophil, and shear with high shear equipment at 10,000 r / min for 1 minute to fully swell and disperse the polycarbophil; after the polycarbophil is completely swollen and dispersed, cool it down To room temperature, adjust the pH to 6.0-6.5 with 1M sodium hydroxide solution; add 0.1 g of poloxamer 407 to the solution, and then transfer the solution to 4°C, so that the poloxamer 407 is completely dissolved and clear After the solution, add the full amount of water for injection, filter, and divide into packaging; store at 2-8°C.

Embodiment 2

[0033]Example 2: Weigh 1.06 g of azithromycin, 8.0 g of mannitol, 0.1 g of disodium EDTA, and 0.05 g of benzalkonium chloride solution, and dissolve them with an appropriate amount of citric acid-sodium citrate buffer and water for injection ultrasonically; add 0.05g of polycarbophil was sheared for 1 minute with high shear equipment at 10000r / min, so that polycarbophil was fully swollen and dispersed; A mixed solution of sodium and potassium hydroxide (molar ratio of 1:1) was adjusted to pH 6.0-6.5; 15g of carbomer was added to the solution, and then the solution was transferred to 4°C to completely dissolve the carbomer and obtain a clear After the solution, add water for injection to the full amount, filter, and divide into packaging; store at 2-8°C.

Embodiment 3

[0034] Example 3: Weigh the mixture of azithromycin 5.0g, glycerin 2.4g, disodium EDTA 6.0g, paraben A, B, propyl and butyl ester (mass ratio is 70:10:10:10) 2.0 g, dissolve with an appropriate amount of citric acid-sodium citrate buffer and water for injection ultrasonically; add 2.5g of polycarbophil, and shear for 2 minutes with a high-shear equipment at 10,000 r / min to make polycarbophil fully swollen and dispersed; After the polycarbophil was completely swollen and dispersed, it was cooled to room temperature, and the pH was adjusted to 6.0-6.5 with 1M sodium hydroxide solution; The poloxamer 407 was completely dissolved, and after a clear solution was obtained, water for injection was added to the full amount, filtered, and packaged separately; stored at 2-8°C.

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PUM

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Abstract

The invention discloses azithromycin gel eye drops and a preparation process thereof. The eye drops are prepared from a main medicine, namely azithromycin and excipients such as an adhesive, a gel matrix, an isotonic regulator, a preservative, an antioxidant, a buffering agent and the like. The adhesive, namely polycarbophil in the eye drops can increase the biological adhesion of the eye drops, so that the detention time of medicines in eyes is further prolonged. The invention provides a practical, convenient and reliable ophthalmic preparation for treating bacterial conjunctivitis, and solves the problems that the detention time of medicines in an eye drop formulation in the eyes is short, the medicines are not easy to absorb, the bioavailability is low and the like.

Description

technical field [0001] The invention relates to an eye drop and a preparation process thereof, in particular to a gel-type eye drop containing azithromycin and a preparation process thereof, and belongs to the technical field of production of ophthalmic pharmaceutical preparations. Background technique [0002] Bacterial conjunctivitis is the most frequently encountered eye disease in daily ophthalmology first visits. Although bacterial conjunctivitis is considered a self-limiting disease, it is usually treated with antibiotic water-soluble eye drops. As an outstanding representative of a new generation of antibiotics, azithromycin is the only 15-membered ring macrolide antibiotic that has been marketed in the world. Its antibacterial spectrum is similar to that of erythromycin but its antibacterial effect is stronger. It has been widely used in China in recent years. [0003] [0004] Azithromycin structural formula [0005] Its mechanism of action is to interfere with...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K31/7052A61K47/32A61K47/34A61K47/36A61K47/38A61P31/04A61P27/02
Inventor 薛泉
Owner 北京乐维生物技术有限公司
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