Compound voriconazole eardrops and preparation method thereof

A technology of azole ear drops and voriconazole, which is applied in the field of compound voriconazole ear drops and its preparation, can solve the problems of slow effect and large ear canal irritation, and achieve relief of discomfort and pain, reasonable and scientific prescription, and anti-allergic keratin abnormal effect

Inactive Publication Date: 2013-06-19
孙国栋 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Due to the simple and convenient operation, ear drops are the most common treatment for otitis media. However, due to the variety of ear diseases, different types of ear drops are required. No ear drops can treat most otitis media. If you go to buy medicine, you may make a big mistake because you can’t prescribe the right medicine, and the current ear drops have the problems of slow effect and great irritation to the ear canal, which need to be corrected urgently. Voriconazole is a kind of antifungal drug, which has antibacterial Broad-spectrum, strong antibacterial efficacy, including acute invasive aspergillosis, fluconazole-resistant severe invasive candidiasis (including Candida krusei), and severe bacteriostasis caused by Mycetoma and Fusarium It has a good inhibitory effect on fungal infection and is the main force of antifungal treatment. It has not been used in ear drops so far

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0019] At 0°C, add 16g of hydroxypropyl-β-cyclodextrin, 0.5g of voriconazole, and 1g of nitrofurazone into 20ml of purified water, while stirring, add an appropriate amount of 1mol / L hydrochloric acid solution to dissolve it, then add 20ml of ethanol, Hydrocortisone 0.5g, Menthol 0.3g, Sodium Chloride 0.8g, Polyethylene Glycol 30ml, Boric Acid 30g, stir well, ultrasonic vibration for 5min, then add glycerin 40g, ethylparaben 0.6g ultrasonic vibration until uniformly dispersed , without air bubbles, add water to 100ml, shake well, adjust the pH to 6.0, pack into 10ml / bottle, and get ready.

[0020] The combination of voriconazole, nitrofurazone and boric acid in the ear drops of this implementation can really treat the infection of various bacteria and fungi, and treat the inflammation of multiple microbial infections in the ear canal. The effect is better, and it is easy to use. The prescription of this implementation is reasonable Science, choose voriconazole with the broades...

Embodiment 2

[0022] At 10°C, first add 5g of hydroxypropyl-β-cyclodextrin, 0.1g of voriconazole, and 0.1g of nitrofurazone into 10ml of purified water, while stirring, add an appropriate amount of 0.7mol / L hydrochloric acid solution to dissolve it, and then add ethanol in sequence 10ml, hydrocortisone 0.1g, menthol 0.1g, sodium chloride 0.1g, polyethylene glycol 10ml, boric acid 10g, stir evenly, ultrasonically oscillate for 5 minutes, then add 5g of glycerin, ultrasonically oscillate until the dispersion is uniform, no bubbles, add water to 120ml, shake well, adjust the pH to 6.0, pack into 10ml / bottle, and get ready.

[0023] The combination of voriconazole, nitrofurazone and boric acid in the ear drops of this implementation can really treat the infection of various bacteria and fungi, and treat the inflammation of multiple microbial infections in the ear canal. The effect is better, and it is easy to use. The prescription of this implementation is reasonable Science, choose voriconazol...

Embodiment 3

[0025] At 20°C, add 40g of hydroxypropyl-β-cyclodextrin, 2.0g of voriconazole, and 10g of nitrofurazone into 50ml of purified water, while stirring, add an appropriate amount of 1.3mol / L hydrochloric acid solution to dissolve it, and then add 100ml of ethanol in sequence , hydrocortisone 3.0g, menthol 3.0g, sodium chloride 2.0g, polyethylene glycol 80ml, boric acid 100g, stir evenly, ultrasonically oscillate for 5min, then add glycerin 60g, ultrasonically oscillate until uniformly dispersed without air bubbles, add water until 1000ml, shake well, adjust the pH to 6.0, pack into 10ml / bottle, and get ready.

[0026] The combination of voriconazole, nitrofurazone and boric acid in the ear drops of this implementation can really treat the infection of various bacteria and fungi, and treat the inflammation of multiple microbial infections in the ear canal. The effect is better, and it is easy to use. The prescription of this implementation is reasonable Science, choose voriconazole...

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PUM

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Abstract

The invention relates to eardrops, and in particular relates to compound voriconazole eardrops and a preparation method thereof. The compound voriconazole eardrops is characterized in that 0.1-2.0g of voriconazole, 0.1-3.0g of hydrocortisone, 5-40g of hydroxypropyl-beta-cyclodextrin, 10-80ml of polyethylene glycol, 0.1-3.0g of menthol, 0.1-2.0g of sodium chloride, 0.01-0.1g of ethylparaben, 5-60g of glycerin and 10-100ml of ethanol are contained in per 100-1000ml of the eardrops. The compound voriconazole eardrops disclosed by the invention has the beneficial effects that the composing prescription is reasonable and scientific and the voriconazole with the broadest antifungal spectrum is selected as the main medicine, so that the eardrops has antibacterial activity on all candida; the toxic and side effects of systemic administration can be reduced through local application and in the meantime, the eardrops is convenient for application, capable of increasing the curative effect and low in price when being directly used as the eardrops; and the eardrops is stable in quality and little in irritation and adverse reaction.

Description

(1) Technical field [0001] The invention relates to an ear drop, in particular to a compound voriconazole ear drop and a preparation method thereof. (2) Background technology [0002] Otitis media is an inflammatory lesion involving all or part of the structure of the middle ear (including the eustachian tube, tympanic cavity, and mastoid air cell). Most of it is non-specific inflammation, especially in children. Otitis media, also known as "ear base", causes pain in the head when it starts, and sometimes pus flows out of the ear. Although it is not a serious illness, it brings endless pain to people. Due to the simple and convenient operation, ear drops are the most common treatment for otitis media. However, due to the variety of ear diseases, different types of ear drops are required. No ear drops can treat most otitis media. If you go to buy medicine, you may make a big mistake because you can’t prescribe the right medicine, and the current ear drops have the problems ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/573A61K31/506A61K31/345A61K33/22A61K9/08A61P27/16A61P31/02A61P31/04A61P31/10
Inventor 孙国栋李军
Owner 孙国栋
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