Ketoconazole vaginal suppository as well as preparation method and detection method thereof

A vaginal expansive suppository and detection method technology, which is applied in suppository delivery, pharmaceutical formula, material inspection products, etc., can solve the problems of low bioavailability, low effective utilization of ketoconazole, and less absorption, and achieve low bioavailability , avoid secondary infection, prevent the effect of outflow

Active Publication Date: 2014-05-07
哈尔滨田美药业股份有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although this suppository reduces the risk of systemic absorption and use of ketoconazole, because ketoconazole is almost insoluble in water, the effective utilization of ketoconazole caused by the use of a hydrophilic suppository base is low, and it cannot solve the problem of poor absorption. , low bioavailability and other issues

Method used

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  • Ketoconazole vaginal suppository as well as preparation method and detection method thereof
  • Ketoconazole vaginal suppository as well as preparation method and detection method thereof
  • Ketoconazole vaginal suppository as well as preparation method and detection method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0095]

[0096] Preparation:

[0097] 1) Preparation of drug-containing matrix:

[0098] a. placing propylene glycol stearate and poloxamer in a water bath for heating and melting to obtain a melt;

[0099] b. mixing ketoconazole and the melt of step a evenly to obtain a drug-containing matrix;

[0100] 2) Pour the drug-containing matrix into a suppository mold, insert a tampon, cool and shape, and prepare 100 cylindrical suppositories, each 4g.

Embodiment 2

[0102]

[0103] Preparation:

[0104] 1) Preparation of drug-containing matrix:

[0105] a. Semi-synthetic coconut oil ester, Polyethylene Glycol 400 are placed in a water bath and heated and melted to obtain a melt;

[0106] b. Take sorbitan monostearate, add 2 times the amount of water, fully grind to a paste with a moisture content of less than 5%, add ketoconazole under grinding, and mix well to obtain a mixture;

[0107] c. mixing the mixture of step b and the melt of step a evenly to obtain a drug-containing matrix;

[0108] 2) Pour the drug-containing matrix into a suppository mold, insert a tampon, cool and shape, and prepare 100 spherical suppositories, each 4.7g.

Embodiment 3

[0110]

[0111] Preparation method: make 100 egg suppositories according to the method in Example 2, each weighing about 4.9g.

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Abstract

The invention relates to a ketoconazole vaginal suppository as well as a preparation method and a detection method thereof. The suppository comprises a drug-containing base formed of ketoconazole and a base, a drug-containing mucous layer formed of ketoconazole and a mucous layer, and a swelling carrier. The oleaginous base and water soluble base are added, thereby ensuring that the whole body absorption and application risk of ketoconazole are reduced and the concentration and bioavailability of ketoconazole are effectively improved, so as to take full play of the efficacy of ketoconazole; an absorption promoting agent and chitosan are added, the absorption of a human body to ketoconazole is promoted; the solid disperse carrier can be used for improving the dissolution of ketoconazole, and further promoting absorption of the human body; the drug-containing mucous layer can be adsorbed on vaginal skin to promote skin absorption and can be used for further improving the bioavailability of ketoconazole. The ketoconazole vaginal suppository provided by the invention adopts six original advanced techniques, and has the beneficial effects of drug liquid outflow prevention, good human body absorption, high bioavailability, lasting curative effect, secondary infection prevention, and the like.

Description

technical field [0001] The invention belongs to the field of vaginal suppositories, in particular to a ketoconazole vaginal expansion suppository and a preparation method and detection method thereof. Background technique [0002] Ketoconazole is off-white crystalline powder; odorless, tasteless, easily soluble in chloroform, soluble in methanol, slightly soluble in ethanol, almost insoluble in water; prone to oxidative degradation in air. Ketoconazole is an imidazole antifungal drug, which has bacteriostatic and bactericidal effects on dermatophytes, yeasts (Candida, Pityrosporum, Torulopsis, Cryptococcus), biphasic fungi and mycoses; Mainly used for the treatment of vulvovaginal candidiasis. There are not many studies on ketoconazole suppositories in the prior art, and because ketoconazole itself is not easily soluble in water, after making suppositories, the amount absorbed by vaginal administration is small and the bioavailability is low; and common ketoconazole supposi...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/02A61K31/496A61K47/14A61K47/34A61K47/46A61P31/10A61P15/02G01N33/15G01N5/04
Inventor 邱学良邱明世
Owner 哈尔滨田美药业股份有限公司
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