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Oral antimicrobial pharmaceutical compositions

A technology of composition and medicine, applied in the field of pharmaceutical composition of rifamycin SV

Active Publication Date: 2011-05-18
COSMO TECH LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0011] Furthermore, currently used drug forms, even though they allow the active ingredient to be administered in discrete doses, release it too quickly compared to the time it takes to pass through the digestive tract, so that the active ingredient is carried out in an indiscriminate manner along the entire gastrointestinal tract its anti-infective activity

Method used

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  • Oral antimicrobial pharmaceutical compositions

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0065] 200 g of rifamycin SV was mixed with 5 g of stearic acid, 7 g of carnauba wax, 8 g of sodium dioctyl sulphosuccinate, 100 g of lactose and 10 g of sodium edetate, and mixed with 25 g of low viscosity polyethylene A solution of pyrrolidone in 0.2 liters of purified water forms granules. When the granulation had been dried, it was mixed with 100 g sodium carboxymethylcellulose, 25 g silicon dioxide, 5 g glycerol palmitostearate and 10 mg talc before being compressed to a unit weight of 495 mg per tablet. The cores thus obtained are then film-coated with a hydroalcoholic dispersion of acrylic and methacrylate esters, titanium dioxide, talc and triethyl citrate, which endow the product with resistance to disintegration in a strongly acidic environment simulating the environment of the stomach and small intestine. sex. The dissolution rate of the tablet is practically zero at a pH less than 7 and is scaled in percentage increments in intestinal buffer at pH 7.2 as follows: ...

Embodiment 2

[0070] 500 g of rifamycin SV was mixed with 10 g of stearic acid, 10 g of beeswax, 10 g of sodium lauryl sulfate, 200 g of mannitol and 10 g of sodium edetate and granulated in a solution containing 50 g of hydroxypropylcellulose in 0.5 liter of water . When the granules have been dried, it is mixed with 150 g sodium hydroxypropyl methylcellulose, 25 g silicon dioxide, 5 g glycerol palmitostearate and 10 mg talc before being compressed to a unit weight of 490 mg / tablet. powder mix. The cores thus obtained are then film-coated with an aqueous dispersion of acrylic acid and methacrylate esters, ferric oxide, talc and triethyl citrate, which confer disintegration of the product in an acidic environment simulating the environment of the stomach and small intestine. Solution resistance. The dissolution rate of the tablet is practically zero at a pH less than 7 and is scaled in percentage increments in intestinal buffer at pH 7.2 as follows:

[0071] Less than 30% after 1 hour re...

Embodiment 3

[0075] 2.5 kg of metronidazole was mixed with 70 g of stearic acid, 70 g of beeswax, 400 g of sucrose, 140 g of hydroxypropylmethylcellulose and 20 g of polysorbate 80, and formed into wet granules by adding purified water to an appropriate viscosity. The granules were then dried and standardized according to size before adding an additional 200 g of hydroxymethylpropylcellulose, 600 g of microcrystalline cellulose, 30 g of palm stearin and 70 g of silicon dioxide. After blending, the powder is compressed to a unit weight of 450 mg / tablet.

[0076]The cores thus obtained are then film-coated with an aqueous alcoholic dispersion of acrylic acid and methacrylate esters, ferric oxide, talc and triethyl citrate, which impart resistance to disintegration in acidic environments. The dissolution rate of the tablet is practically zero at a pH less than 7 and is scaled in percentage increments in intestinal buffer at pH 7.2 as follows:

[0077] less than 25% within the first hour of r...

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Abstract

The present invention relates to oral pharmaceutical compositions with controlled and / or programmed release containing at least one active ingredient having antimicrobial and / or anti-infectious activity for the treatment of infections of the large intestine, in particular the colon.

Description

technical field [0001] The present invention relates to a controlled and / or delayed release oral pharmaceutical composition, in particular to a pharmaceutical composition comprising rifamycin SV in combination with one or more pharmaceutically acceptable excipients. It also relates to the pharmaceutical use of said pharmaceutical composition. Background technique [0002] Intestinal infections are common diseases which are caused by intestinal colonization of exogenous pathogenic agents of different origin, or by the normally existing intestinal microorganisms becoming viral. [0003] What is known is that the intestine is divided into two distinct parts: the proximal part called the "small intestine", which is formed in a craniocaudal direction by the duodenum, jejunum and ileum, and the "large intestine". The distal part, which is formed by the colon and the recto-anus (Fatter A, Scevola G. Anatomia e Fisiologia del Corpo Umano (Anatomy and Physiology of the Human Body). ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/26A61K9/32A61K31/395A61K31/4164A61K9/16A61K9/20A61K9/28
CPCA61K31/395A61K9/2846A61K9/2018A61K9/2054A61K31/4164A61K9/2013A61P1/00A61P1/04A61P1/12A61P1/16A61P3/12A61P31/00A61P31/04A61P39/02Y02A50/30A61K9/20A61K9/282A61K9/2826
Inventor 莫罗·艾尼罗伯塔·宝杰拉吉赛普·塞拉斯克罗伯特·韦拉
Owner COSMO TECH LTD