Voriconazole eye drops and preparation method thereof

A technology of voriconazole and eye drops, which is applied in the direction of medical formulas, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., can solve the problems of increased test costs, impact of antibacterial activity, high eye drops, etc., to achieve Effects of increasing corneal permeability, increasing comfort, and improving solubility

Inactive Publication Date: 2010-10-06
河南省眼科研究所
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

If the drug is insoluble in water, its antibacterial activity will be greatly affected
Because voriconazole is insoluble in water, some studies have used the method of preparing salts, adding acid to prepare salts. Since voriconazole itself is not alkaline, after adding acid, although the solubility can be improved, its pH value will decrease, while eye drops The pH requirement is relatively high, not suitable for the preparation of eye drops
Another reason is that from the perspective of new drug declaration requirements, after the salt is made, the raw material becomes another entity, which is required to be declared as a new drug, and the required various pharmaceutical materials and test costs are greatly increased.
Voriconazole eye drops are also prepared using voriconazole powder injection, but the excipients of the powder injection are not completely suitable for the requirements of eye drops
There are also studies using hydroxypropyl-β-cyclodextrin to increase the solubility of voriconazole. The main problems are: the preparation process requires heating and ultrasonic equipment, which will affect the stability of the drug; cost etc.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] a. Add 5 to 100 ml of ethanol to 3 to 50 grams of voriconazole powder, stir and dissolve at room temperature to obtain a clear solution A;

[0027] b. Add 100 to 400 ml of water for injection to 20 to 300 grams of hydroxypropyl-β-cyclodextrin, stir and dissolve at room temperature to obtain a transparent solution B;

[0028] c. Add solution A to solution B under stirring, and evaporate the ethanol under vacuum or normal pressure to obtain solution C;

[0029] d. Add 0.1-0.3 grams of antibacterial agent, 0.5-2.5 grams of sodium hyaluronate, and 1-5 grams of osmotic pressure regulator to solution C under stirring, so that the osmotic pressure can be adjusted to be equivalent to 0.8%-1.2% NaCl solution. Osmotic pressure, add water for injection to make up to 1000 ml, continue to stir until dissolved into a solution. The antibacterial agent is benzalkonium chloride, benzalkonium bromide or ethylparaben, and the osmotic pressure regulator is sodium chloride or glycerin.

...

Embodiment 2

[0032] Weigh 20 grams of voriconazole powder, add 50 ml of absolute ethanol to it, stir and dissolve at room temperature to obtain a clear solution A; weigh 200 grams of hydroxypropyl-β-cyclodextrin, add 300 ml of water for injection to it, stir and dissolve at room temperature to obtain Transparent solution B; under stirring, add solution A to solution B, evaporate the ethanol under normal pressure to obtain solution C; add 0.1 g of bacteriostatic agent benzalkonium chloride and sodium hyaluronate 1.5 g to solution C under stirring gram, 5 grams of sodium chloride, add water for injection and make it to 1000 milliliters, continue to stir until dissolving into a solution. Filter, sterilize with circulating steam at 100°C, and dispense into eye drops bottles under aseptic conditions.

Embodiment 3

[0034] Weigh 20 grams of voriconazole powder, add 50 ml of absolute ethanol to it, stir and dissolve at room temperature to obtain a clear solution A; weigh 140 grams of hydroxypropyl-β-cyclodextrin, add 300 ml of water for injection to it, stir and dissolve at room temperature to obtain Transparent solution B; under stirring, add solution A to solution B, evaporate the ethanol under normal pressure to obtain solution C; add 0.1 g of bacteriostatic agent benzalkonium chloride and sodium hyaluronate 1.5 g to solution C under stirring gram, add water for injection to make up to 1000 milliliters, and continue to stir until dissolved into a solution. Filter, sterilize with circulating steam at 100°C, and dispense into eye drops bottles under aseptic conditions.

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PUM

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Abstract

The invention discloses voriconazole eye drops. Every 1000 milliliters of eye drops contain 3-50g of voriconazole powder, 20-500g of hydroxypropyl-beta-cyclodextrin, 0.1-0.3g of bacteriostat, 0.5-2.5g of sodium hyaluronate and the balance of water for injection, wherein the bacteriostat is benzalkonium chloride, benzalkonium bromine or ethylparaben. The invention also discloses a preparation method of the voriconazole eye drops. The invention greatly increases the solubility of voriconazole in water to 0.3-5%, so that the medicine can exist in water solution in the form of molecules, thereby providing convenience for exerting the antifungal action of the medicine. Meanwhile, when being applied to eyes, the invention provides convenience for exerting the antifungal action of the medicine through cornea. The preparation method can be carried out at room temperature without affecting the medicine stability, and has the advantages of simple and easy realization and low cost.

Description

technical field [0001] The invention belongs to medical preparations, and in particular relates to an eye drop with voriconazole as the main component, and also relates to a manufacturing method of the eye drop. Background technique [0002] Voriconazole 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. 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. Because voriconazole is insoluble in water, some studies have used the method of preparing salts, adding acid to prepare salts. Since voriconazole itself is not alkaline, after adding acid, although the solubility can be improved, its pH value will decrease, wh...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/08A61K31/506A61P31/10A61P27/02A61K47/40A61K47/36A61K47/14A61K47/18
Inventor 张俊杰王丽娅
Owner 河南省眼科研究所
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