Taurine-containing ophthalmic in-vivo gel preparation and preparation method thereof

A taurine eye and body gel technology, applied in liquid delivery, aerosol delivery, anhydride/acid/halide active ingredients, etc., can solve the problems of difficult eye spreading, long retention time, inaccurate dosage, etc. , to achieve the effect of easy and accurate dose control, long residence time and good biocompatibility

Inactive Publication Date: 2014-04-16
INST OF CHINESE MATERIA MEDICA CHINA ACAD OF CHINESE MEDICAL SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, the domestically marketed variety is taurine eye drops. After the eye drops are instilled into the eyes, they are easily diluted by tears and need to be used frequently. Although eye ointments and ophthalmic gels have a certain slow-release effect, they exist Ophthalmic in-body gels, also known as in-situ gels, also known as instant gels, exist in the form of hydrophilic sols or macromolecular solutions in vitro. After being dripped into the medication site, it will quickly gel to form a gel when encountering gel factors (temperature, body fluid, etc.), which not only retains the advantages of convenient administration and accurate dosage of the solution, but also has the advantages of gel in the medication The site stays for a long time to achieve the purpose of long release and slow release
[0003] At present, there is no new drug variety of ophthalmic in-body gel on the market in China. The foreign FDA has approved one such product: Timolol Malaeate Ophthalmic Forming Solution (Timolol Malaeate Ophthalmic Forming Solution). The artificial tear ophthalmic in-body gel prepared by Sharm 407 has been launched in Australia and Japan

Method used

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  • Taurine-containing ophthalmic in-vivo gel preparation and preparation method thereof
  • Taurine-containing ophthalmic in-vivo gel preparation and preparation method thereof
  • Taurine-containing ophthalmic in-vivo gel preparation and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0024] Take 80kg of water for injection, add 2.5kg of taurine, and stir to dissolve. Weigh 0.1 kg of deacetylated gellan gum, disperse it into the above solution, let it stand overnight, then add 0.1 kg of potassium sorbate, 1 kg of calcium sodium edetate, add appropriate amount of boric acid and sodium borate to adjust the pH to 5.0-7.0, and then add Add sodium chloride, adjust the osmotic pressure to 250-350 mosmol / kg, filter the solution through a microporous membrane, add water for injection from the filter to 100kg, and sterilize with circulating steam. Put it in an eye drop bottle and pack it.

Embodiment 2

[0026] Take 80kg of water for injection, add 1kg of taurine, and stir to dissolve. Weigh 0.25 kg of deacetylated gellan gum, disperse it into the above solution, let it stand overnight, then add 0.03 kg of ethylparaben, 1 kg of disodium edetate, add appropriate amount of boric acid and sodium borate to adjust the pH to 5.0-7.0 , then add glucose, adjust the osmotic pressure to 250-350 mosmol / kg, filter the solution through a microporous membrane, add water for injection from the filter to 100kg, and sterilize with circulating steam. Put it in an eye drop bottle and pack it.

Embodiment 3

[0028] Get 80kg of water for injection, add 5kg of taurine, and stir to dissolve. Weigh 0.5 kg of deacetylated gellan gum, disperse it into the above solution, let stand overnight, then add 0.015 kg each of methylparaben and ethylparaben, 2 kg of disodium edetate, add appropriate amount of boric acid, boric acid Adjust the pH to 5.0-7.0 with sodium, then add mannitol, adjust the osmotic pressure to 250-350 mosmol / kg, filter the solution through a vertically fused glass filter, add water for injection to the total amount, add water for injection from the filter to 100kg, and circulate steam Sterilize, take a sample for quality identification, and after passing the test, subpackage it in an eye drop bottle under aseptic conditions, and pack it to get the product.

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Abstract

The invention relates to a taurine-containing ophthalmic in-vivo gel preparation and a preparation method thereof. The taurine-containing ophthalmic gel is an ophthalmic preparation which is in a liquid state in vitro and forms a gel state after dropped into eyes. The taurine-containing ophthalmic gel is prepared by taking taurine as an active substance and supplementing a gel adjuvant, a thickening agent, a preservative, an osmotic-pressure conditioning agent, a pH conditioning agent and water for injection. The taurine-containing ophthalmic gel is suitable for treatment of diseases such as retinopathy and the like; and the ophthalmic gel is in the liquid state in vitro, a dosage is easy and accurate to control, the use is convenient, the ophthalmic gel can be uniformly spread after dropped into the eyes, gelates, is retained in the eyes for longer time and is not prone to loss, effective drug concentration can be effectively maintained, the treatment effect is enhanced, further, the toxicity is low, the irritation is small, the biocompatibility is good, and the taurine-containing ophthalmic gel is effective, facilitates clinical application, and has a wide development prospect.

Description

technical field [0001] The invention relates to ophthalmic in-body gel preparation of taurine, which belongs to the field of pharmaceutical preparations. Background technique [0002] Studies have shown that taurine has a certain therapeutic effect on various types of retinopathy. At present, the domestically marketed variety is taurine eye drops. After the eye drops are instilled into the eyes, they are easily diluted by tears and need to be used frequently. Although eye ointments and eye gels have a certain slow-release effect, they still exist Ophthalmic in-body gels, also known as in-situ gels, also known as instant gels, exist in the form of hydrophilic sols or macromolecular solutions in vitro. After dripping into the medication site, it will quickly gel to form a gel when encountering gel factors (temperature, body fluid, etc.), which not only retains the advantages of convenient administration and accurate dosage of the solution, but also has The site stays for a l...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/06A61K31/185A61P9/10A61P27/02
Inventor 王国华张保献聂其霞臧琛赵小妹
Owner INST OF CHINESE MATERIA MEDICA CHINA ACAD OF CHINESE MEDICAL SCI
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