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Brinzolamide brimonidine eye drop and preparation method thereof

A technology of brimonidine and eye drops, which is applied in the field of brimonidine brimonidine eye drops and its preparation, can solve the problems of low concentration of N-deethyl-brinzolamide, and promote Corneal epithelial repair, increased comfort, and good biocompatibility

Inactive Publication Date: 2018-07-10
SHANGHAI HAOHAI BIOLOGICAL TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Steady-state red blood cell concentrations similar to orally administered brinzolamide were found in studies of ophthalmic brinzolamide, but lower concentrations of N-deethyl-brinzolamide

Method used

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  • Brinzolamide brimonidine eye drop and preparation method thereof

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] 1. a brinzolamide brimonidine eye drop, by weight percentage, it comprises the following components: brinzolamide 2%, brimonidine 2%, sodium chloride 0.5%, potassium chloride 0.3%, 1% sodium hyaluronate and phosphate buffer solution, the balance is water for injection, and the addition amount of the pH regulator is such that the pH of the eye drop is 6.

[0024] 2. a preparation method of brinzolamide brimonidine eye drops, comprising the following steps:

[0025] (1) Take water for injection of 50wt% of the prescription amount, add it to the container together with brinzolamide, brimonidine, pH regulator and osmotic pressure regulator, stir and mix, and use a 0.2 μm filter membrane to filter and sterilize;

[0026] (2) Weigh the amino polysaccharide and add it to the filtrate, and stir at a stirring speed of 150 rpm for 5 hours at a temperature of 20° C. until the amino polysaccharide dissolves;

[0027] (3) Supplement the remaining water for injection, shake well, fi...

Embodiment 2

[0029] 1. a brinzolamide brimonidine eye drop, by weight percentage, it comprises the following components: brinzolamide 1.5%, brimonidine 1.5%, sodium chloride 0.3%, potassium chloride 0.1%, 0.1% chondroitin sulfate and an appropriate amount of sodium hydroxide, the balance is water for injection, and the amount of sodium hydroxide added is such that the pH of the eye drop is 5.5.

[0030] 2. a preparation method of brinzolamide brimonidine eye drops, comprising the following steps:

[0031] (1) Take water for injection of 40wt% of the prescribed amount, add it to the container together with brinzolamide, brimonidine, pH regulator and osmotic pressure regulator, stir and mix, and use a 0.2 μm filter membrane to filter and sterilize;

[0032] (2) Weigh the amino polysaccharide and add it to the filtrate, and stir at a stirring speed of 200 rpm for 6 hours at a temperature of 15°C until the amino polysaccharide dissolves;

[0033] (3) Supplement the remaining water for injecti...

Embodiment 3

[0035] 1. a brinzolamide brimonidine eye drop, by weight percentage, it comprises the following components: brinzolamide 1%, brimonidine 5%, magnesium chloride 0.8%, chitosan 0.5% , 0.5% chondroitin sulfate and an appropriate amount of boric acid, the balance is water for injection, and the amount of boric acid added is such that the pH of the eye drop is 7.5.

[0036] 2. a preparation method of brinzolamide brimonidine eye drops, comprising the following steps:

[0037] (1) Take water for injection of 40wt% of the prescribed amount, add it to the container together with brinzolamide, brimonidine, pH regulator and osmotic pressure regulator, stir and mix, and use a 0.2 μm filter membrane to filter and sterilize;

[0038] (2) Weigh the amino polysaccharide and add it to the filtrate, and stir at a stirring speed of 100 rpm, a stirring time of 3 hours, and a temperature of 25° C. until the amino polysaccharide dissolves;

[0039] (3) Supplement the remaining water for injection...

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Abstract

The invention belongs to the technical field of drugs, and particularly relates to a brinzolamide brimonidine eye drop and a preparation method thereof. The brinzolamide brimonidine eye drop is prepared from, by weight, 1-3% of brinzolamide, 1-5% of brimonidine, 0.3-0.8% of osmotic pressure conditioning agent, 0.1-1% of glycosaminoglycan, pH conditioning agent and balance water for injection, wherein the addition amount of the pH conditioning agent enables pH of the eye drop to be 5.5-7.5. The prepared eye drop containing the brinzolamide brimonidine and iso-osmia with tears have the advantages of not containing preservative, being capable of effectively reducing intraocular pressure and having no secondary damage to eyes caused by the preservative.

Description

technical field [0001] The invention belongs to the technical field of medicines, and in particular relates to a brinzolamide brimonidine eye drop and a preparation method thereof. Background technique [0002] Glaucoma is an eye disease in which the pressure in the eyeball increases intermittently or continuously. In addition to the increase in intraocular pressure, there are also changes in the optic nerve and visual field. According to the latest statistics from WHO, the number of glaucoma patients worldwide has reached 67 million. This disease has become the second largest disease leading to human blindness after cataract. Upward trend. [0003] Glaucoma is currently treated in three ways: drugs, lasers, and surgery. Laser and surgery have low clinical popularity due to their limited therapeutic effect and potential damage. Generally, patients will choose drug therapy, a relatively safe way to lower intraocular pressure. With the emergence and update of glaucoma drugs...

Claims

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Application Information

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IPC IPC(8): A61K9/08A61K47/36A61K31/542A61K31/498A61P27/06
CPCA61K9/0048A61K9/08A61K31/498A61K31/542A61K47/36A61K2300/00
Inventor 周晓惠陈晚华张军东廉云飞吴剑英
Owner SHANGHAI HAOHAI BIOLOGICAL TECH
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