Antifungal imidazole medicament controlled-release gel and preparation method thereof

A slow-release gel, fungal imidazole technology, applied in antifungal, drug delivery, pharmaceutical formulations and other directions, can solve the problems of short action time, poor adhesion, easy to fall off, etc., achieve less irritation, reduce the number of medication , the effect of not easy to fall off

Inactive Publication Date: 2013-05-01
SHENYANG WANJIA INST OF BIOLOGICAL TECH RES
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The imidazole topical vaginal drug preparations currently on the market include vaginal suppositories, vaginal effervescent tablets, vaginal ointments, vaginal gels, soft capsules and other dosage forms. These preparations all have the following technical problems: poor adhesion in the vagina, easy to fall off , short duration of action, requiring multiple doses
None of the above patents, documents and products already on the market involve the technical content of imidazole vaginal sustained-release gel

Method used

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  • Antifungal imidazole medicament controlled-release gel and preparation method thereof

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Effect test

Embodiment 1

[0019] The antifungal imidazole slow-release gel of the present invention is prepared from the following raw materials in parts by weight: 0.5 part of miconazole nitrate, 0.5 part of polycarbophil, 0.5 part of carbomer, liquid paraffin 0.2 parts, 1 part of mixed glycerides, 5 parts of glycerin, 100 parts of water.

[0020] The preparation method of antifungal imidazoles slow-release gel is as follows: a, get Carbomer and polycarbophil by said weight ratio, add the water of said weight ratio, stir at normal temperature for 2.5 hours, get hydration gel, add The miconazole nitrate in the weight ratio is stirred evenly, and the pH is adjusted to 3.0-3.5 with an aqueous sodium hydroxide solution with a mass percentage concentration of 20%, to obtain a gel for subsequent use; b, take mixed glycerides, Liquid paraffin and glycerin are mixed and melted at 80°C, mixed evenly, the temperature is lowered to 60°C, and the oil phase is obtained for later use; c, the gel obtained in a is he...

Embodiment 2

[0023] The antifungal imidazole slow-release gel of the present invention is prepared from the following raw materials in parts by weight: 3 parts of miconazole nitrate, 2 parts of polycarbophil, 2 parts of carbomer, liquid paraffin 1 part, 2 parts of mixed glycerides, 15 parts of glycerin, 80 parts of water.

[0024] The preparation method of antifungal imidazoles slow-release gel is as follows: a, get carbomer and polycarbophil according to the weight ratio, add the water of the weight ratio, and stir at room temperature for 2 hours to obtain a hydration gel, add The miconazole nitrate in the weight ratio is stirred evenly, and the pH is adjusted to 3.0-3.5 with an aqueous sodium hydroxide solution with a mass percentage concentration of 20%, to obtain a gel for subsequent use; b, take mixed glycerides, Liquid paraffin and glycerin are mixed and melted at 80°C, mixed evenly, and the temperature is lowered to 60°C to obtain the oil phase for later use; c. Heat the gel obtaine...

Embodiment 3

[0027] The antifungal imidazole slow-release gel of the present invention is prepared from the following raw materials in parts by weight: 2 parts of miconazole nitrate, 1 part of polycarbophil, 2 parts of carbomer 934P, liquid 0.5 parts of paraffin, 1 part of hydrogenated coconut oil glyceride, 12 parts of glycerin, and 90 parts of water.

[0028]The preparation method of antifungal imidazoles slow-release gel is as follows: a, get Carbomer 934P and polycarbophil AA-1 by said weight ratio, add the water of said weight ratio, stir at normal temperature for 3 hours, obtain hydration Gel, add miconazole nitrate in the weight ratio, stir evenly, adjust the pH to 3.0-3.5 with an aqueous solution of sodium hydroxide with a concentration of 20% by mass percentage, and obtain the gel for subsequent use; b, take hydrogenation according to the weight ratio Coconut oil glyceride, liquid paraffin, and glycerin are mixed and melted at 80°C, mixed evenly, and the temperature is lowered to ...

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Abstract

The invention discloses a preparation method of an antifungal imidazole medicament controlled-release gel. The preparation is mainly used for vaginal administration and treatment on colpomycosis and other diseases and belongs to the technical field of medicaments. The antifungal imidazole medicament controlled-release gel is prepared from the following raw materials in parts by weight: 0.5-3 parts of imidazole medicaments, 0.5-2 parts of polycarbophil, 0.5-2 parts of carbomer, 0.2-1.0 part of lipid component, 1-2 parts of emulsifying agent, 5-15 parts of wetting agent and 80-100 parts of water. The preparation method has the advantages that the medicament is slowly released, local durable concentration of the medicament is kept, the sterilizing effect is enhanced, the medicament application frequency is reduced, and the stimulation to the medicament is reduced.

Description

technical field [0001] The invention relates to an antifungal imidazole slow-release gel and a preparation method thereof. The preparation is mainly used for vaginal administration and local treatment of diseases such as candida vulvovaginosis and double infection caused by Gram-positive bacteria, and belongs to field of pharmaceutical technology. Background technique [0002] Imidazole drugs are currently the most widely used antifungal drugs in the world, mainly including miconazole nitrate, econazole nitrate, butoconazole nitrate, ketoconazole and clotrimazole, which are synthetic imidazole broad-spectrum antifungal drugs. Drugs have almost all effects on pathogenic fungi. Its mechanism is to inhibit the synthesis of sterols in the fungal cell membrane, affect the permeability of the cell membrane, inhibit the growth of fungi, and lead to their death. The concentration below 4mg / L can inhibit most clinically isolated fungi. In addition, miconazole is also effective agai...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/00A61K47/32A61K47/44A61P31/10
Inventor 董英杰艾莉王会芳张乃先刘茁韩亚男邹晓峰
Owner SHENYANG WANJIA INST OF BIOLOGICAL TECH RES
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