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Ciclopirox olamine gelling agent, method for preparing the same and pharmaceutical use thereof

A technology of ciclopirox olamine gel and ciclopirox olamine, which is applied in drug combination, drug delivery, pharmaceutical formulation, etc., can solve ciclopirox oxamine heat and metal ion instability, poor mucoadhesive effect, biological Problems such as low utilization, to avoid irritation and burning sensation, strong adhesion, and improve antibacterial efficacy

Inactive Publication Date: 2009-10-21
SHANGHAI HUILUN BIOLOGICAL TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, ointments and suppositories contain oily components, which have the disadvantages of slow drug release, greasy feeling, easy contamination of clothing, poor adhesion to mucous membranes, and low bioavailability; meanwhile, ciclopirox olamine is sensitive to light, heat and Metal ions are unstable, so appropriate excipients should be preferably added to the preparation to ensure its stability and give full play to its efficacy; in addition, according to the physiological characteristics of vaginal drug use, the pH range of the preparation should be adjusted appropriately to avoid damage to the mucous membranes. irritation and burning

Method used

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  • Ciclopirox olamine gelling agent, method for preparing the same and pharmaceutical use thereof
  • Ciclopirox olamine gelling agent, method for preparing the same and pharmaceutical use thereof
  • Ciclopirox olamine gelling agent, method for preparing the same and pharmaceutical use thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0053]Preparation: Add 10g of Carbomer 940 to 600g of purified water, let it swell naturally for 24 hours, stir well, adjust the pH to 5.0-6.0 with 0.5mol / L sodium hydroxide, add 100g of propylene glycol and stir well, set aside; take ciclopirox amine Add 20g to 100ml of ethanol to dissolve, set aside (the preparation and storage of ciclopirox amine should be placed in a brown bottle); take another 0.2g of edetate disodium, Tween 8020g, add appropriate amount of purified water to dissolve, slowly add to Carbomer for use In the solution, stir evenly, then add ciclopirox olamine solution, stir evenly; add purified water to 1000g, stir evenly, degas, potting, and pack.

Embodiment 2

[0055] Preparation: Add carbomer 94010g to 600g purified water, swell naturally for 24 hours, stir well, adjust pH to 5.0-6.0 with 0.5mol / L sodium hydroxide, add 150g propylene glycol and stir well, set aside; take 20g ciclopirox olamine Add 100ml of ethanol to dissolve, set aside (the preparation and storage of ciclopirox amine should be placed in a brown bottle); take another 0.2g of edetate disodium, Tween 8015g, add appropriate amount of purified water to dissolve, slowly add to the carbomer standby solution , stir evenly, then add ciclopirox olamine solution, stir evenly; add purified water to 1000g, stir evenly, degas, potting, and pack.

Embodiment 3

[0057] Preparation: Add carbomer 94015g to 650g purified water, swell naturally for 24 hours, stir well, adjust pH to 5.0-6.0 with 0.5mol / L sodium hydroxide, add 150g propylene glycol and stir well, set aside; take ciclopirox 20g Add 150ml of ethanol to dissolve, set aside (the preparation and storage of ciclopirox amine should be placed in a brown bottle); take another 0.2g of edetate disodium, Tween 8020g, add appropriate amount of purified water to dissolve, slowly add to the carbomer standby solution , stir evenly, then add ciclopirox olamine solution, stir evenly; add purified water to 1000g, stir evenly, degas, potting, and pack.

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PUM

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Abstract

The invention relates to a ciclopirox olamine gel preparation used to cure vagina candida albicans and mycotic infection, wherein the gel preparation takes ciclopirox olamine as active material and macromolecule polymer carbomer as hydrophilic gel ground substance; meanwhile, the gel preparation is made through adding appropriate amount of cosolvent, pH regulator, percutaneous absorption enhancer, stabilizer and purified water according to the physiologic characteristics of vaginal administration and physical and chemical characters of ciclopirox olamine. The gel preparation is characterized by exquisite and smooth texture, no greasy feeling and easy cleaning and also has the advantages of no stimulus, strong adhesion and good adhering effect on skin; meanwhile, the gel preparation can prolong stay time of ciclopirox olamine in vagina and promote percutaneous absorption of medicine to improve antibacterial efficacy, thereby possessing high safety and clinic practicability.

Description

Technical field: [0001] The invention relates to a ciclopirox amine gel preparation, and relates to its preparation method and medicinal use. Background technique: [0002] Ciclopirox olamine is a synthetic pyridone compound, which is a new generation of non-imidazole broad-spectrum antifungal drugs. Ciclopirox olamine mainly changes the integrity of the fungal cell membrane, causes the outflow of intracellular substances, and blocks the uptake of protein precursor substances, leading to its death. It has strong penetrating power, can directly reach the deep part of the infected skin, and can resist most pathogenic molds, including skin fungi, Candida albicans, and a variety of non-pathogenic molds, Gram-positive bacteria, Gram-negative bacteria, etc. . Because of its advantages of high efficiency, broad spectrum, safety, strong penetrating power and no effect on damaged skin, it is suitable for tinea pedis, tinea corporis and tinea versicolor, and can also be used for ski...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/4418A61K9/00A61K47/32A61K47/10A61P15/02A61P31/04A61P31/10A61K47/26
Inventor 秦继红
Owner SHANGHAI HUILUN BIOLOGICAL TECH CO LTD
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