Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

Pharmaceutical composition including dorzolamide and brimonidine

A technology of brimonidine and composition, applied in the field of pharmaceutical compositions containing dorzolamide and brimonidine, can solve problems such as corneal epithelial diseases

Inactive Publication Date: 2018-09-28
SANTEN PHARMA CO LTD
View PDF4 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, benzalkonium chloride is cytotoxic and may cause corneal epithelial disease when the exposure is increased (Non-Patent Document 1), so Cosopt (registered trademark) compound eye drops that do not contain benzalkonium chloride are also sold

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Pharmaceutical composition including dorzolamide and brimonidine
  • Pharmaceutical composition including dorzolamide and brimonidine
  • Pharmaceutical composition including dorzolamide and brimonidine

Examples

Experimental program
Comparison scheme
Effect test

Embodiment

[0106] Although the formulation example and the result of the antiseptic efficacy test are shown below, it is for better understanding of this invention, and does not limit the scope of this invention.

[0107] Preparation example

[0108] Representative formulation examples of the present invention are shown below. In addition, the compounding quantity of each component in the following formulation example is the content in 1 mL of formulations.

preparation example 1

[0109] Formulation example 1 (in multi-dose container)

[0110]

preparation example 2

[0111] Formulation example 2 (in multi-dose container)

[0112]

[0113] It should be noted that the desired composition can be obtained by appropriately adjusting the types and amounts of dorzolamide, brimonidine, and additives in the aforementioned formulation examples 1 and 2.

[0114] Anti-corrosion efficacy test (1)

[0115] 1. Preparation of test preparations

[0116] Dorzolamide hydrochloride (1g), brimonidine tartrate (0.1g), sodium citrate hydrate (0.294g), boric acid (0.7g), D-mannitol (2.0g), ethylene glycol Dissodium amine tetraacetate dihydrate (0.05 g) was dissolved in water and sterilized by filtration. After adjusting the resulting solution to pH 6.5 with a pH regulator, water was added to make the total amount 100 mL, thereby preparing the preparation of Example 1 . The preparation of Comparative Example 1 was prepared in the same manner as that of Example 1 except for changing the pH value.

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

No PUM Login to View More

Abstract

The present invention addresses the problem of providing a novel pharmaceutical composition that contains dorzolamide or a salt thereof and brimonidine or a salt thereof and exhibits a sufficient preservative effect. A pharmaceutical composition according to the present invention that contains dorzolamide or a salt thereof and brimonidine or a salt thereof has a pH of 6.0 or more. A pharmaceuticalcomposition according to the present invention preferably does not include a preservative or includes a prescribed amount thereof, wherein said prescribed amount is preferably such that the logarithmic value of the ratio (B / A) of the number (B) of bacteria at the time of inoculation to the number (A) of bacteria when the number of viable bacteria is measured after inoculating bacteria in a test sample that comprises the preservative and water and mixing homogeneously such that the concentration of Escherichia Coli ATCC 8739 in the bacterial suspension is within the range of 105-106 cfu / mL, and collecting 1 mL of the test sample using a micropipette after the test sample has been stored for seven days at 20-25 deg c while shielded from light, is 2.0 or less.

Description

technical field [0001] The present invention relates to a pharmaceutical composition containing dorzolamide or its salt and brimonidine or its salt. Background technique [0002] Dorzolamide, which is a carbonic anhydrase inhibitor, is useful in the treatment of glaucoma or ocular hypertension because of its ocular hypotension-lowering effect, and a preparation containing dorzolamide has been sold as Trusopt (registered trademark) ophthalmic solution. In addition, a preparation containing dorzolamide and timolol has been sold as Cosopt (registered trademark) compound eye drops. [0003] Furthermore, as α 2 Brimonidine, which is a receptor agonist, is also useful in the treatment of glaucoma or ocular hypertension because it exhibits an intraocular hypotensive effect, and a formulation containing brimonidine has been sold as Aiphagan (registered trademark) ophthalmic solution. [0004] In addition, for eye drops, in order to prevent the reproduction of fungi and the like ca...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/382A61K31/498A61K47/04A61K47/18A61K9/08A61P27/06
CPCA61K31/498A61K31/382A61K9/08A61K9/0048A61K47/183A61K47/02A61P27/06A61K2300/00A61K47/18Y02A50/30A61P27/02A61K31/497
Inventor 梅崎慎也
Owner SANTEN PHARMA CO LTD
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com