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

Ketoconazole eye drops and fabricating method thereof

A manufacturing method and technology of eye drops, which are applied in the direction of pharmaceutical formulations, medical preparations containing active ingredients, drug delivery, etc., can solve the problems of long stirring time, increased manufacturing costs, complicated operation process, etc., and achieve the effect of improving solubility

Inactive Publication Date: 2008-09-17
河南省眼科研究所
View PDF1 Cites 1 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

A kind of method that adopts polysorbate 80 to increase the dissolubility of ketoconazole in water is disclosed in " the development of ketoconazole eye drops " of volume 33, the 4th phase of " Chinese pharmaceutical journal " in April, 1998, but because polysorbate 80 The amount of sorbate 80 in eye drops should not be too high, so the solubilization effect of this method on ketoconazole is limited
"Preparation of ketoconazole β-cyclodextrin inclusion compound" in the 10th issue of volume 36 of "Chinese Journal of Pharmaceutical Sciences" in October 2001 discloses a method to improve The method for the solubility of ketoconazole improves the solubility of ketoconazole in water from 3 parts per million at 37°C to 119 parts per million that is 0.0119%, but the method has the following problems: in the preparation process, organic solvents need to be added, Heating is required, the stirring time is long, the operation process is complicated, and low temperature drying is required, etc.
"Development of Ketoconazole-Hydroxypropyl-β-cyclodextrin Inclusion Compound Eye Drops" in "Northwest Pharmaceutical Journal" June 2001, Volume 16, No. 3, disclosed another solubilization method, using hydroxy Propyl-beta-cyclodextrin increases the solubility of ketoconazole, but because of the problem of preparation process, the solubility of ketoconazole can only reach about 0.1%, and there are also the following problems: the preparation process needs heating, which will affect the Stability impacts and requires freeze-drying, which increases manufacturing costs

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
  • Ketoconazole eye drops and fabricating method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0019] Example 1: Weigh 30 grams of hydroxypropyl-β-cyclodextrin, add 100 milliliters of water for injection to it, stir at room temperature to dissolve it, and obtain a transparent solution A; weigh 5 grams of ketoconazole powder, and then take A Solution 15 ml, ketoconazole powder was added to the solution, and then 10 ml of 1mol / L hydrochloric acid was added thereto, stirred and dissolved at room temperature to obtain a transparent solution B; while stirring, solution B was added to solution A, and gradually added 10 ml of 1 mol / L sodium hydroxide, and adjust the pH value to 5.5-8 to obtain solution C; under stirring, add 0.1 g of bacteriostatic agent benzalkonium chloride and 10 g of polyvinyl alcohol to solution C, and continue Stir and heat the solution to reach 80°C until the polyvinyl alcohol dissolves, add water for injection to make up to 1000ml, then filter, sterilize with circulating steam at 100°C, and distribute it in 5ml or 8ml eye drops bottles under aseptic con...

Embodiment 2

[0022] Example 2: Weigh 500 grams of hydroxypropyl-β-cyclodextrin, add 400 milliliters of water for injection into it, and stir to dissolve it at a temperature of 30° C. to obtain a transparent solution A; weigh 50 grams of ketoconazole powder , and then take 45 ml of solution A, add ketoconazole powder to the solution, then add 100 ml of 1mol / L hydrochloric acid to it, stir and dissolve at 30°C to obtain a transparent solution B; add solution B while stirring into solution A, and gradually add 90 ml of 1mol / L sodium hydroxide to adjust the pH value to 5.5-8 to obtain solution C; under stirring, add bacteriostatic agent ethylparaben 0.3 g and 10 grams of polyvinyl alcohol, continue to stir and heat to make the solution temperature reach 50°C until the polyvinyl alcohol dissolves, add water for injection to make up to 1000 ml, then filter, sterilize with circulating steam at 100°C, and divide under aseptic conditions Packed in 5ml or 8ml eye drops bottle.

Embodiment 3

[0023] Example 3: Weigh 300 grams of hydroxypropyl-β-cyclodextrin, add 300 milliliters of water for injection into it, stir and dissolve it at a temperature of 10°C to obtain a transparent solution A; weigh 40 grams of ketoconazole powder , and then take 25 ml of solution A, add ketoconazole powder to the solution, then add 50 ml of 1mol / L hydrochloric acid to it, stir and dissolve at a temperature of 10°C to obtain a transparent solution B; add solution B while stirring into solution A, and gradually add 60 ml of 1mol / L sodium hydroxide to adjust the pH value to 5.5-8 to obtain solution C; under stirring, add bacteriostatic agent ethylparaben 0.4 g and 15 grams of polyvinyl alcohol, continue to stir and heat to make the solution temperature reach 40°C until the polyvinyl alcohol dissolves, add water for injection to make up to 1000 ml, then filter, sterilize with circulating steam at 100°C, and divide under aseptic conditions Packed in 5ml or 8ml eye drops bottle.

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 invention discloses a ketoconazole eye drop, which is prepared from ketoconazole powder 5-50g, Hydroxypropyl-beta-cyclodextrin 30-500g, bacteria inhibitor 0.1-0.4g, polyvinyl alcohol 10-20g, 1mol / L hydrochloric acid 5-100ml, 1mol / L sodium-hydroxide 5-100ml, and balancing water.

Description

technical field [0001] The invention belongs to medical preparations, in particular to an eye drop with ketoconazole as the main component, and also relates to a manufacturing method of the eye drop. Background technique [0002] We know that the antibacterial or antifungal activity of a drug is mainly exerted in molecular form, the greater the concentration of the same drug in water, the better the antibacterial effect of the drug. If the drug is insoluble in water, its antibacterial activity will be greatly affected. Ketoconazole is a broad-spectrum antifungal drug with good antifungal activity, but because it is insoluble in water, it is greatly limited in ophthalmology and other clinical applications. For this reason, people constantly try to improve the concentration of ketoconazole in water with different methods. A kind of method that adopts polysorbate 80 to increase the dissolubility of ketoconazole in water is disclosed in " the development of ketoconazole eye dr...

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 Patents(China)
IPC IPC(8): A61K31/496A61K9/08A61P27/02A61P31/10
Inventor 张俊杰王丽娅高长凤
Owner 河南省眼科研究所
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