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Colon-targeted pellets containing vancomycin and preparation method thereof

A colon-targeted and pellet-oriented technology, which is applied in pharmaceutical formulation, powder delivery, glycopeptide components, etc.

Inactive Publication Date: 2011-12-28
ZHEJIANG MEDICINE CO LTD XINCHANG PHAMACEUTICAL FACTORY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, there is no oral vancomycin preparation available on the market, so if oral administration is required, vancomycin for injection can be dissolved in distilled water and then taken orally. Time-resistant environment, which can easily lead to the emergence of vancomycin-resistant enterococci (VRE)

Method used

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  • Colon-targeted pellets containing vancomycin and preparation method thereof
  • Colon-targeted pellets containing vancomycin and preparation method thereof
  • Colon-targeted pellets containing vancomycin and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037]

[0038] Take by weighing 0.75g vancomycin hydrochloride and 3g talcum powder, first vancomycin hydrochloride is dissolved in 110g water, then talcum powder is added in the solution and homogenized for 10 minutes with a high-shear homogenizer to make a suspension; The suspension was slowly dispersed in 146.25g under stirring FS30D (based on solid content) polymer suspension, pass through 80 mesh sieve to prepare water dispersion suspension for coating. In addition, weigh 1.5g of talcum powder and 6g of triethyl citrate, add 220g of water and mix to make a water-dispersed suspension, and slowly add the suspension to the weighed 292.5g In FS30D, at the same time, mix with a common mixer at a medium speed for 45 minutes to form a water-dispersed suspension, and pass the suspension through an 80-mesh sieve to prepare a colonic enteric coating solution. Using the fluidized bed coating technology, spray the medicinal water dispersion suspension and the colon enteric coa...

Embodiment 2

[0040]

[0041]Take by weighing 1.25% vancomycin hydrochloride and 1g talcum powder, first vancomycin hydrochloride is dissolved in 10g water, then talcum powder is made suspension with high-shear homogenizer homogenization 10 minutes in adding solution; The suspension was slowly dispersed in 2.75g of FS30D (based on solid content) polymer suspension, pass through 80 mesh sieve to prepare water dispersion suspension for coating. In addition, weigh 15 g of talc powder and 3.75 g of triethyl citrate, add 60 g of water and mix to make a water-dispersed suspension, and slowly add the suspension to the weighed 6.25 g In FS30D, at the same time, mix with a common mixer at a medium speed for 45 minutes to form a water-dispersed suspension, and pass the suspension through an 80-mesh sieve to prepare a colonic enteric coating solution. Using the fluidized bed coating technology, spray the medicinal water dispersion suspension and the colon enteric coating solution on the blank pe...

Embodiment 3

[0043]

[0044] Take by weighing 5g vancomycin hydrochloride and 4g talcum powder, first vancomycin hydrochloride is dissolved in 60g water, then talcum powder is made suspension with high-shear homogenizer homogenization 10 minutes in adding solution; The suspension was slowly dispersed in 41g under stirring FS30D (based on solid content) polymer suspension, pass through 80 mesh sieve to prepare water dispersion suspension for coating; in addition, weigh 22.5g of talcum powder, 7.5g of triethyl citrate, add 120g of water and mix well Make water dispersion suspension, add this suspension slowly to weigh 45g In FS30D, at the same time, mix with a common mixer at a medium speed for 45 minutes to form a water-dispersed suspension, and pass the suspension through an 80-mesh sieve to prepare a colonic enteric coating solution. Using the fluidized bed coating technology, spray the medicinal water dispersion suspension and the colon enteric coating solution on the blank pellet ...

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Abstract

The invention discloses a colon-targeting pellet with vancomycin as an active ingredient and a preparation method thereof. The targeted pellet preparation is composed of a blank core, a drug coating layer and a colonic enteric coating layer, wherein the blank core is a commercially available product, and the drug layer is composed of vancomycin, anti-adhesive agent and methyl acrylate copolymer , the colonic enteric coating layer is composed of anti-adhesive agent, plasticizer and methyl acrylate, and the colon-targeted micropills of vancomycin are prepared by adopting a fluidized bed micropellet coating method. The colon-targeted pellet preparation is used for the treatment of pseudomembranous colitis caused by Clostridium difficile caused by long-term administration of broad-spectrum antibiotics. The targeted drug release can not only improve the curative effect, but more importantly, avoid vancomycin Exposure to non-acting sites effectively reduces the incidence of vancomycin-resistant enterococci (VRE).

Description

technical field [0001] The invention relates to a colon-targeted pellet with vancomycin as an active ingredient, which is used for treating pseudomembranous colitis caused by Clostridium difficile caused by long-term administration of broad-spectrum antibiotics. Background technique [0002] Clostridium difficile is a Gram-positive anaerobic bacterium that exists in the form of spores and produces toxins. With the widespread use of broad-spectrum antibiotics, the number of Clostridium difficile colitis caused by antibiotics is increasing. At present, the drugs used to treat Clostridium difficile colitis mainly include metronidazole and vancomycin, both of which have a cure rate of more than 85%. Vancomycin has slightly better curative effect than metronidazole, but due to It is cheap and easy to obtain clinically, so methazole has become the drug of choice for clinical treatment of Clostridium difficile colitis. With the widespread use of metronidazole in clinical practice,...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/14A61K9/52A61K38/14A61P1/00A61P31/02
Inventor 易德平张国钧田治科
Owner ZHEJIANG MEDICINE CO LTD XINCHANG PHAMACEUTICAL FACTORY
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