Ophthalmic gel containing dorzolamide and timolol and preparation method thereof

A technology of ophthalmic gel and dorzolamide, applied in the field of pharmaceutical preparations, can solve the problems of reducing the dosage of active ingredients and strong ocular retention

Active Publication Date: 2017-03-08
SHENYANG XINGQI PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0011] The present inventor has made an ophthalmic gel containing dorzolamide and timolol through in-depth research and creative work, which uses a bioadhesive matrix as a carrier, has a clear and transparent appearance, and has high thixotropy. High drug permeability, strong ocular retention, overcome the influence of active ingredients on matrix carrier viscosity and thixotropy, and overcome the limitation of drug penetration rate from stroma to cornea, greatly reduce the dosage of active ingredients, reduce Increased the number of daily doses, improved the safety and compliance of drug use, and met the demand for once-daily doses

Method used

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  • Ophthalmic gel containing dorzolamide and timolol and preparation method thereof
  • Ophthalmic gel containing dorzolamide and timolol and preparation method thereof
  • Ophthalmic gel containing dorzolamide and timolol and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0096] Embodiment 1: Preparation of ophthalmic gel 1

[0097] Ophthalmic gel 1 was prepared according to the corresponding prescription ratio in Table 1 below.

[0098]Preparation method: (1) Swell the prescribed amount of carbomer, sodium hyaluronate, and polyvinyl alcohol with an appropriate amount of water for injection, and sterilize for later use; (2) Fully mix the carbomer base and polyvinyl alcohol base, and set aside; Dissolve sodium hydroxide in appropriate amount of water, sterilize with 0.22 μm filter and mix with the mixed matrix obtained in (2) for later use; (4) take 40ml of water for injection at 50-80°C, dissolve dorzolamide hydrochloride and timolol maleate in sequence Er, glycerin, ethylparaben, sterilized by 0.22 μm filtration, and set aside; (5) mix the sodium hyaluronate matrix obtained from (1) with the solution obtained from (4) evenly; (6) mix the material obtained from (5) with the material obtained from (3), and add water for injection to 100g, Sti...

Embodiment 2－4

[0099] Embodiment 2-4: Preparation of ophthalmic gel 2-4

[0100] Prepare ophthalmic gels 2-4 according to the corresponding prescription ratio in Table 1.

[0101] The preparation method refers to Example 1.

[0102] Table 1: Prescription ratio

[0103] Component Example 1 Example 2 Example 3 Example 4 Dorzolamide Hydrochloride 0.56g 0.56g 1.11g 2.22g timolol maleate 0.68g 0.34g 0.14g 0.068g Carbomer 980 0.5g 0.5g - - Carbomer 974 - - 0.6g 0.7g sodium hyaluronate 0.7g 0.5g 0.6g 0.6g polyvinyl alcohol 1.1g 0.7g 1.0g 1.2g

[0104] Propylene Glycol - - 1.4g 0.9g glycerin 1.8g 2.0g - - Benzalkonium chloride - 0.01 - 0.005 Ethylparaben 0.03 - 0.03 0.02 sodium hydroxide Appropriate amount Appropriate amount Appropriate amount Appropriate amount Add water for injection to 100g 100g 100g 100g

Embodiment 5－8

[0105] Embodiment 5-8: Preparation of ophthalmic gel 5-8

[0106] Prepare ophthalmic gels 5-8 according to the corresponding prescription ratio in Table 2.

[0107] Table 2: Prescription ratio

[0108]

[0109] Preparation method: (1) Swell the prescribed amount of carbomer, sodium hyaluronate, and polyvinyl alcohol with an appropriate amount of water for injection, and sterilize for later use; (2) Fully mix the carbomer base and polyvinyl alcohol base, and set aside; Dissolve sodium hydroxide in appropriate amount of water, sterilize with 0.22 μm filter and mix with the mixed matrix obtained in (2) for later use; (4) take 40ml of water for injection at 50-80°C, dissolve dorzolamide hydrochloride and timolol maleate in sequence Alcohol, glycerin, ethylparaben, HS15, sterilized by 0.22μm filtration, and set aside; (5) mix the sodium hyaluronate matrix obtained from (1) with the solution obtained from (4) evenly; (6) mix the material obtained from (5) with the material o...

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Abstract

The invention belongs to the field of pharmaceutical preparations, and relates to an ophthalmic gel containing dorzolamide and timolol and a preparation method thereof. Specifically, the present invention relates to an ophthalmic gel comprising an effective amount of dorzolamide or a pharmaceutically acceptable salt thereof, timolol or a pharmaceutically acceptable salt thereof, a gel base and water. The invention also relates to the use of said ophthalmic gel. The ophthalmic gel of the present invention realizes the administration method of once-a-day administration while reducing the dosage of active ingredients, combined with its high thixotropy and high clarity characteristics, it greatly improves the safety and safety of clinical medication. compliance.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and relates to an ophthalmic gel containing dorzolamide and timolol and a preparation method thereof. The invention also relates to the use of said ophthalmic gel. Background technique [0002] Glaucoma is generally defined as a group of clinical syndromes or eye diseases that threaten and impair optic nerve visual function, mainly related to pathological elevated intraocular pressure. Elevated intraocular pressure can lead to damage to optic nerve function, which may cause irreversible damage to the optic nerve head and visual function. If left untreated, visual field defects or total loss can result, leading to blindness. The main types of glaucoma include primary (including open-angle and angle-avoidance), secondary, congenital, and mixed glaucoma. [0003] Aiming at the possible etiological mechanism of glaucoma, the current effective clinical measures are to use different method...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/5377A61K31/382A61K9/06A61P27/02A61P27/06
Inventor 刘继东王宁利杨宇春唐海高坤孙洋
Owner SHENYANG XINGQI PHARM CO LTD
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