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Brinzolamide eye drop preparation and preparation method thereof

A technology of brinzolamide and eye drops, which is applied in the direction of pharmaceutical formulas, medical preparations with non-active ingredients, oil/fat/wax non-active ingredients, etc., to achieve simple equipment, easy control of process parameters, and strong operability Effect

Inactive Publication Date: 2018-01-16
合肥远志医药科技开发有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, none of the above-mentioned patent reports involves the direct preparation of brinzolamide mixed type eye drops from the micronized brinzolamide bulk drug, and the application proposes a micronized brinzolamide eye drop preparation and its Preparation

Method used

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  • Brinzolamide eye drop preparation and preparation method thereof
  • Brinzolamide eye drop preparation and preparation method thereof
  • Brinzolamide eye drop preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027]

[0028]

[0029] 【Preparation Process】

[0030] Put Tyloxapol and 5% of the total amount of purified water in a beaker according to the above table, dissolve, filter through a 0.22 μm filter membrane, add the raw material of brinzolamide to the filtrate, seal it, and prepare the suspension of the main drug; purify 30% of the total amount Put water in a beaker, sprinkle carbomer into it, stir while adding, heat to 60°C, after it swells completely, filter through a 10μm filter membrane, seal, add mannitol, sodium chloride, edetate disodium, benzalkonium chloride Ammonium and 30% of the total amount of purified water are placed in a beaker, heated to 60°C and stirred to dissolve, filtered through a 0.22 μm filter membrane, added to the above carbomer solution, stirred evenly, and adjusted to pH 7.5 with dilute hydrochloric acid or 10% sodium hydroxide solution ±0.2, stir evenly, add the above-mentioned main drug suspension, make up to volume with purified water, ful...

Embodiment 2

[0032]

[0033]

[0034] 【Preparation Process】

[0035] According to the above table, put poloxamer and 5% of the total amount of purified water in a beaker, dissolve, filter through a 0.22 μm filter membrane, add the raw material of brinzolamide to the filtrate, seal it, and prepare the main drug suspension; purify 30% of the total amount Put water in a beaker, sprinkle hydroxypropyl cellulose, stir while adding, heat to 60°C, after completely swelling, filter through a 10μm filter membrane, seal, add sorbitol, potassium chloride, disodium edetate, hydroxyl Benzyl ester and 30% of the total amount of purified water are placed in a beaker, heated to 60°C and stirred to dissolve, filtered through a 0.22 μm filter membrane, added to the above-mentioned hydroxypropyl cellulose solution, stirred evenly, adjusted with dilute hydrochloric acid or 10% sodium hydroxide solution When the pH value reaches 7.5±0.2, stir evenly, add the above main drug suspension, use purified water...

Embodiment 3

100%

[0038] 【Preparation Process】

[0039] Put polysorbate and 5% of the total amount of purified water in a beaker according to the above table, dissolve them, filter through a 0.22 μm filter membrane, add the raw material of brinzolamide to the filtrate, seal it, and prepare the suspension of the main drug; add 30% of the total amount of purified water Put it in a beaker, sprinkle sodium carboxymethyl cellulose, stir while adding, heat to 60°C, after it is completely swollen, filter through a 10μm filter membrane, seal it, add mannitol, boric acid, disodium edetate, ethyl hydroxybenzoate Put the ester and 30% purified water in a beaker, heat to 60°C and stir to dissolve, filter through a 0.22 μm filter membrane, add the above sodium carboxymethyl cellulose solution, stir well, adjust the pH with dilute hydrochloric acid or 10% sodium hydroxide solution value to 7.5±0.2, stir evenly, add the above main drug suspension, use purified water to make up the volume, fully h...

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PUM

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Abstract

A preparation method of a brinzolamide eye drop is disclosed. The method is as follows: dispersing active ingredient brinzolamide in a wetting agent, meanwhile completely swelling a suspending aidingagent at 60 DEG C, placing for two hours, dissolving an osmotic pressure regulator, a metal ion complexing agent and a preservative conditioner completely at 60 DEG C, adding a brinzolamide-containingwetting agent solution to a suspending aiding agent solution under homogeneous stirring conditions, continuing homogenizing stirring for 5min, adding other solutions, continuing homogenizing for 5min, adjusting pH, sterilizing and filling. The prescription of the brinzolamide eye drop is simple, the preparation method has strong industrialized production operationability, after direct micronization treatment of raw material medicines, a sample is prepared, a large number of manpower, material and financial resources can be saved, and the preparation method has the advantages of simple equipment required for the preparation project and easy process parameter control.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations. Specifically, the present invention relates to a brinzolamide eye drop preparation and a preparation method thereof. Background technique [0002] Brinzolamide is a drug used to treat primary and secondary open-angle glaucoma and ocular hypertension, and can also be used to prevent and treat intraocular pressure after laser surgery. It can be used as a beta-blocker Ineffective, or in patients with contraindications to the use of the drug alone, or as a co-therapy with beta-blockers. [0003] Chinese alias: (R)-(+)-4-ethylamino-2-(3-methoxypropyl)-3,4-dihydro-2H-thieno[3,2-e]-1,2 -thiazine-6-sulfonamide-1,,1-dioxide; -4-(ethylamino)-3,4-dihydro-2-(3-methoxypropyl)-2H-thiophene[3, 2-E]-1,,2-thiazine-6-sulfamoyl 1,1-dioxide; parozolomide. [0004] Its structural formula is as follows: [0005] [0006] The substrate of carbonic anhydrase inhibitors (CAIs) is carbonic anhydrase (CA)...

Claims

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Application Information

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IPC IPC(8): A61K9/08A61K31/542A61K47/32A61K47/38A61K47/44A61P27/06
Inventor 白中稳薛娟
Owner 合肥远志医药科技开发有限公司
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