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Brinzolamide eye preparations, and preparation method and use thereof

A technology of brinzolamide and preparations, which is applied in the field of brinzolamide ophthalmic preparations and its preparation, and can solve the problems of short retention time of brinzolamide eye drops, preservatives, etc.

Active Publication Date: 2013-06-12
SICHUAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In a word, none of the above-mentioned products and patents has simultaneously solved the short retention time of brinzolamide eye drops in the eyes and the irritating problems of long-term use of preservatives. It is very necessary in this field to make brinzolamide eye drops safe, efficient, stable, Controlled liquid formulation for easy ophthalmic application

Method used

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  • Brinzolamide eye preparations, and preparation method and use thereof
  • Brinzolamide eye preparations, and preparation method and use thereof
  • Brinzolamide eye preparations, and preparation method and use thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1～3

[0330]

[0331] Note: " / " means not added.

[0332] Examples 1 to 3 are brinzolamide or brinzolamide salt temperature-sensitive gel prescriptions. The preparation method is as follows: weigh the thickener polymer matrix in proportion, add distilled water, stir well, and place until completely dissolved; then press Proportionally weigh the poloxamer, add it to distilled water, stir to dissolve part of it, and place it in the refrigerator until it is completely dissolved; Stir to dissolve in distilled water, filter through a 0.22 μm microporous membrane, combine the filtrate with the above polymer solution, add distilled water to the full amount, adjust the pH of the solution to 5.0-9.0 with a pH regulator, and stir evenly to obtain .

Embodiment 4～6

[0334]

[0335] Embodiments 4 to 6 are brinzolamide or brinzolamide salt pH-sensitive gel prescriptions, and the preparation method is as follows: disperse hypromellose and carbopol in 30ml water for injection and soak overnight, stir to obtain a solution, Standby, add brinzolamide or brinzolamide salt, osmotic pressure regulator, add 30ml of water for injection, dissolve under stirring, filter through a 0.22 μm microporous membrane, add the filtrate to the hypromellose and hypromellose prepared above In the Carbopol solution, add water for injection to 100ml, add an appropriate amount of pH regulator solution to adjust the pH of the system to 5.5, and stir evenly to obtain brinzolamide ophthalmic gel.

Embodiment 7～9

[0337]

[0338] Note: " / " means not added.

[0339] Examples 7 to 9 are brinzolamide or brinzolamide salt ion-sensitive gel prescriptions, and the preparation method is as follows: add the polymer material of the prescription amount to 20 to 30 ml of water for injection, stir magnetically, and disperse evenly. Drug, osmotic pressure regulator, add 30ml of water for injection, dissolve under stirring, filter through a 0.22 μm microporous membrane, add the filtrate to the hypromellose and carbopol solution prepared above, adjust the pH value and osmotic pressure , and add water for injection to 100ml, stir evenly to obtain brinzolamide ophthalmic gel.

[0340] The applicant further researched and analyzed the above three in situ gels within the priority period.

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Abstract

The invention relates to the medicine field, and concretely relates to brinzolamide eye preparations, and preparation methods and uses thereof. Several brinzolamide eye preparations are provided to prolong the eye stay time or improve the bioavailability, and provide a new dose form choice for the reduction of the intraocular tension or the treatment of glaucoma. The concrete dose forms of the preparations comprise a temperature-sensitive eye in-situ gel, a pH-sensitive eye in-situ gel, an ion-sensitive eye in-situ gel, a brinzolamide lipidosome, a brinzolamide nanoparticle, a brinzolamide nano-suspension, and a brinzolamide composite gel preparation, the preparations can be used for treating diseases comprising intraocular hypertension, glaucoma and the like, and the gels can prolong the stay time of medicines in eyes and reduce the administration frequency and the administration dosage, so the patient compliance is improved, and the side effects of medicines are reduced. The no addition of any antiseptics and the adoption of single-dosage packaging reduce the irradiation of the use of eye drops for a long term to eyes and substantially improve the medicine safety.

Description

technical field [0001] The invention relates to the field of medicine, in particular to a brinzolamide ophthalmic preparation and a preparation method and application thereof. Background technique [0002] Glaucoma is a disease that causes damage to the optic nerve. The optic nerve is composed of many nerve fibers. When the intraocular pressure increases, it can cause damage to the nerve fibers and cause visual field defects. The key to controlling glaucoma is to reduce intraocular pressure, and the production and discharge of aqueous humor is the key to controlling intraocular pressure. If the production and discharge of aqueous humor are out of balance, causing too much pressure on the eyeball wall, it will lead to optic nerve damage. Carbonic anhydrase (CA) is present in many body tissues, including eye tissues, and catalyzes the reversible reaction of carbon dioxide hydration to carbonic acid and carbonic acid dehydration. The ciliary body produces aqueous humor throug...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/06A61K9/10A61K31/542A61K47/36A61K47/40A61K47/38A61K47/34A61P27/06A61K47/10A61K47/32
Inventor 宋相容魏于全
Owner SICHUAN UNIV
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