Nitric acid butoconazole cyclodextrin or cyclodextrin derivant clathrate and preparation method as well as application thereof

A technology of butoconazole nitrate cyclodextrin and butoconazole nitrate, which is applied in the field of medicine, can solve the problems such as the lack of research on the water solubility of butoconazole nitrate, and achieve the effect of safe and effective clinical medication, clear and transparent appearance, and easy to accept

Inactive Publication Date: 2008-05-21
山东特瑞林医药科技发展有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there was no research on the water solubility of butoconazole nitrate at that time

Method used

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  • Nitric acid butoconazole cyclodextrin or cyclodextrin derivant clathrate and preparation method as well as application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038]Example 1: Preparation of liquid butoconazole nitrate hydroxypropyl-β-cyclodextrin inclusion compound

[0039] (1) Weigh 200g of hydroxypropyl-β-cyclodextrin, pour it into 200ml of water, and stir to dissolve;

[0040] (2) Take another 10g of butoconazole nitrate, pour it into the above-mentioned hydroxypropyl-β-cyclodextrin solution, and stir the mixture for 20 minutes with the method of Zili stirrer, and the stirring speed should be such that the liquid does not splash. Until it becomes clear and transparent, 210 g of butoconazole nitrate hydroxypropyl-β-cyclodextrin inclusion compound is obtained as a light yellow transparent liquid. It has been determined that the clathrate is easily soluble in water.

Embodiment 2

[0041] Example 2: Preparation of solid butoconazole nitrate hydroxypropyl-β-cyclodextrin inclusion compound

[0042] (1) Weigh 200g of hydroxypropyl-β-cyclodextrin, pour it into a mixture of 200ml of water and 40ml of absolute ethanol, and stir to dissolve;

[0043] (2) Take another 10g of butoconazole nitrate, pour it into the above mixed solution, and stir the mixed solution for 20 minutes with a stirrer method, the stirring speed should be such that the liquid does not splash outside, and observe the solution until it is clear and transparent, and liquid nitric acid is obtained. Hydroxypropyl-β-cyclodextrin inclusion complex of butoconazole.

[0044] (3) Concentrate the liquid butoconazole nitrate hydroxypropyl-β-cyclodextrin inclusion compound, and freeze-dry to obtain 210 g of off-white solid butoconazole nitrate hydroxypropyl-β-cyclodextrin inclusion compound. It has been determined that the clathrate is easily soluble in water.

Embodiment 3

[0045] Example 3: Preparation of gel with butoconazole nitrate hydroxypropyl-β-cyclodextrin inclusion compound

[0046] (1) Take butoconazole nitrate 4g;

[0047] (2) Dissolve 80g of hydroxypropyl-β-cyclodextrin in 150ml of water for injection;

[0048] (3) Butoconazole nitrate is added to the hydroxypropyl-β-cyclodextrin solution and stirred for clathrate;

[0049] (4) Add 6.0g of glycerin, 4.0g of ethanol, 6.0g of hypromellose, add water for injection to 200ml, disperse for 5 hours, fill, and obtain.

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PUM

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Abstract

The invention relates to a butoconazole nitrate cyclodextrin or a cyclodextrin derivative inclusion compound, the preparation method and the usage. The invention uses the cyclodextrin or the cyclodextrin derivative to carry out the inclusion of the butoconazole nitrate, and the weight ratio of the butoconazole nitrate and the cyclodextrin or the cyclodextrin derivative in the inclusion compound is 1: 1 to 300. The inclusion compound can be used in the preparation of transfusion, liquid acupuncture therapy, powder injection, oral liquor, syrup, tablets, pills, capsules, granules, gels, soft capsules, suppositories, aerosols, creams and other various formulations. The water solubility and the stability of the prepared preparations are improved significantly, moreover, the invention has long drug release time, no irritating smell and small side effects, and can be used for mycotic vaginitis and skin fungal infections, and the clinical usage is more safe and effective.

Description

technical field [0001] The invention relates to butoconazole nitrate cyclodextrin or a cyclodextrin derivative inclusion compound, a preparation method and application thereof, and belongs to the technical field of medicine. Background technique [0002] Fungal vaginitis (monilial or mycotic vaginitis) is caused by fungal infection, and its incidence rate is second only to trichomonal vaginitis. Mold (fungus) has many kinds, and the most important one in human body is Candida albicans. 80~90% of vaginal infections are caused by Candida albicans, so mycotic vaginitis is actually Candida vaginitis or vaginal candidiasis (vagmalcandidiansis). Candidal vaginitis is more common in young girls, pregnant women, diabetic patients, and postmenopausal patients who have been treated with higher doses of estrogen. This disease is easy to show effect repeatedly clinically, is extremely difficult to cure. [0003] Foreign long-term clinical trials have shown that butoconazole nitrate h...

Claims

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Application Information

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IPC IPC(8): A61K31/4164A61K9/00A61K9/02A61K9/12A61K9/48A61K47/40A61P31/10A61P15/02
Inventor 肖广常张颖张冰
Owner 山东特瑞林医药科技发展有限公司
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