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Brinzolamide liposome eye preparation and preparation method thereof

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

Inactive Publication Date: 2015-08-05
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 liposome eye preparation and preparation method thereof
  • Brinzolamide liposome eye preparation and preparation method thereof
  • Brinzolamide liposome eye preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1～3

[0181]

[0182] Note: " / " means not added.

[0183] Embodiments 1 to 3 are Brinzolamide or Brinzolamide salt temperature-sensitive gel formulations. The preparation method is as follows. Weigh the thickening agent macromolecular matrix in proportion, add distilled water, stir fully, and place until all dissolved; then press Proportionally weigh poloxamer, add it to distilled water, stir to partially dissolve, and place it in the refrigerator until it is completely dissolved; dissolve brinzolamide or brinzolamide, solubilizer, osmotic pressure regulator, and preservative. Dissolve in distilled water, stir to dissolve, 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 adjuster, stir evenly, that is, .

Embodiment 4～6

[0185]

[0186]

[0187] Embodiments 4 to 6 are brinzolamide or brinzolamide salt pH-sensitive gel formulations. The preparation method is as follows: Hypromellose and carbopol are dispersed in 30ml water for injection and soaked overnight, stirred to obtain a solution, For subsequent use, add brinzolamide or brinzolamide salt, osmotic pressure regulator, add 30 ml of water for injection, dissolve under stirring, filter through a 0.22 μm microporous membrane, and add the filtrate to the hypromellose prepared above and In the carbopol solution, add water for injection to 100ml, add an appropriate amount of pH adjuster solution to adjust the pH of the system to 5.5, and stir evenly to obtain brinzolamide ophthalmic gel.

Embodiment 7～9

[0189]

[0190] Note: " / " means not added.

[0191] Embodiments 7 to 9 are prescriptions for brinzolamide or brinzolamide salt ion-sensitive gels, and the preparation method is as follows: add the polymer material of the prescription amount into 20 to 30 ml of water for injection, stir magnetically, and disperse uniformly. Drug, osmotic pressure regulator, add 30 ml of water for injection, dissolve under stirring, filter with 0.22 μm microporous membrane, add the filtrate to the hypromellose and carbopol solution prepared above, adjust pH value and osmotic pressure , and add water for injection to 100ml, stir evenly, and obtain brinzolamide ophthalmic gel.

[0192] The applicant further studies and analyzes the above three in situ gels during 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 liposome 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, the nerve fibers can be damaged, causing 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 is unbalanced, 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 tissue, and catalyzes the hydration of carbon dioxide to carbonic acid, as well as the reversible reaction of carbonic acid dehydration. The ciliary body produces aqueous hum...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/06A61K9/127A61K31/542A61K47/36A61K47/34A61P27/06A61K47/10A61K47/32
Inventor 宋相容魏于全
Owner SICHUAN UNIV
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