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Compositions and methods of treatment comprising amoxicillin and potassium clavulante with xanthan

a technology of potassium clavulanate and amoxicillin, which is applied in the field of amoxicillin and potassium clavulanate novel treatment methods and novel formulations, can solve the problems of reducing bioavailability, no advantage, and failing to show any advantage over a conventional capsul

Inactive Publication Date: 2007-05-10
BEECHAM PHARMACEUTICALS PTE LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0011] The present invention relates to a method of treating bacterial infections in humans which comprises administering thereto a therapeutically effective amount of amoxicillin and potassium clavulanate such that the amount of amoxicillin is in the range 1900 to 2600 mg and the amount of potassium clavula

Problems solved by technology

This showed no advantage over a conventional capsule formulation, with bioavailability being diminished.
This however failed to show any advantage over a conventional capsule.
The time above MIC was found to be significantly extended, compared to a capsule formulation, but not enough for a 12 h dosing interval.

Method used

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  • Compositions and methods of treatment comprising amoxicillin and potassium clavulante with xanthan
  • Compositions and methods of treatment comprising amoxicillin and potassium clavulante with xanthan
  • Compositions and methods of treatment comprising amoxicillin and potassium clavulante with xanthan

Examples

Experimental program
Comparison scheme
Effect test

example 1

1000 / 62.5 mg Modified Release Tablet

[0145]

Ingredientmg / tablet% w / wImmediate Release LayerAmoxicillin Trihydrate (ERH 654.1*40.88Potassium Clavulanate76.2#4.76Microcrystalline Cellulose136.48.52Sodium Starch Glycollate18.01.12Colloidal Silicon Dioxide6.30.39Magnesium Stearate9.00.56Total (Immediate Release Layer)900.056.23Slow Release LayerCrystallised Sodium Amoxicillin480.8**30.05Microcrystalline Cellulose113.27.08Xanthan Gum14.00.87Citric Acid78.04.87Colloidal Silicon Dioxide1.500.08Magnesium Stearate14.00.87Total (Sustained Release Layer)700.043.74Film coatOpadry YS-1-7700 - Composition:Hydroxypropylmethylcellulose 2910 6 cp11.6Hydroxypropylmethylcellulose 2910 15 cp3.9Titanium dioxide15.1Polyethylene Glycol 33502.3Polyethylene Glycol 80002.3Total weight of coated tablet1635.2

*Equivalent to 562.5 mg of amoxicillin based on an assay of 86.0%

#Equivalent to 62.5 mg of clavulanic acid based on an assay of 82.0%

**Equivalent to 437.5 mg amoxicillin based on an assay of 91.0%

example 2

[0146] 1000 / 62.5 mg modified release tablet The immediate release layer and film coat are as for the tablet of Example 1

Ingredientmg / tablet% w / wSlow Release LayerCrystallised Sodium Amoxicillin480.8**30.05Microcrystalline Cellulose127.27.95Citric Acid78.04.87Colloidal Silicon Dioxide1.50.09Magnesium Stearate14.00.87Total (Slow Release Layer)700.043.74Total Weight of coated tablet1635.2

**Equivalent to 437.5 mg amoxicillin based on an assay of 91.0%

Preparation of Modified Release Tablets

[0147] Modified release tablets were prepared according to the process flow diagram shown in FIG. 2. In brief, immediate and modified release blends are prepared which involve initial sieving and milling, as indicated, before roller compaction in a Chilsonater and further milling, sieving and blending. The two containers comprising amoxicillin trihydrate and the two containers comprising sodium amoxicillin comprise about equal weights of amoxicillin trihydrate and sodium amoxicillin, respectively....

example 3

Slow Release Tablet (875 mg)

[0152]

mg / ta(a) Sodium Amoxicillin TabletCrystallised Sodium Amoxicillin 91%*96173Dried Microcrystalline Cellulose27321Magnesium Stearate11Xanthan gum 200 mesh**54Total1(b) Sodium Amoxicillin Tablet with citric acidCrystallised Sodium Amoxicillin 91%*96166Dried Microcrystalline Cellulose28819Magnesium Stearate141Citric acid10Xanthan gum 200 mesh**22Total1(c) Amoxicillin Trihydrate TabletAmoxicillin Trihydrate 86%*10178Dried Microcrystalline Cellulose2116Magnesium Stearate11Xanthan Gum, 200 mesh**54Total1

*adjusted for the potency of the amoxicillin component and corresponding to 875 mg amoxicillin,

**Xantural 75

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Abstract

Bacterial infections may be treated using a high dosage regimen of amoxicillin and potassium clavulanate. Preferably, the dosage is provided by a bilayer tablet.

Description

FIELD OF THE INVENTION [0001] This invention relates to a novel method of treatment using amoxicillin and potassium clavulanate and for novel formulations, in particular tablet formulations, for use in such methods. BACKGROUND OF THE INVENTION [0002] Amoxicillin and potassium clavulanate are respectively a known β-lactam antibiotic and a known β-lactamase inhibitor. Products comprising amoxicillin and potassium clavulanate are marketed under the trade name “Augmentin” by SmithKline Beecham. Such products are particularly effective for treatment of community acquired infections, in particular upper respiratory tract infections in adults and otitis media in children. [0003] Various tablet formulations of amoxicillin and potassium clavulanate have been approved for marketing, comprising various different weights and ratios of amoxicillin and potassium clavulanate, for instance, conventional swallow tablets comprising 250 / 125, 500 / 125, 500 / 62.5, and 875 / 125 mg amoxicillin / clavulanic aci...

Claims

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Application Information

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IPC IPC(8): A61K9/20A61K9/22A61K31/43A61K31/407A61K9/24A61K9/28
CPCA61K9/2013A61K9/205A61K9/209A61K9/2866A61K31/407A61K31/43A61K45/06A61K2300/00
Inventor STORM, KEVIN H.CONLEY, CREIGHTON P.ROUSH, JOHN A.
Owner BEECHAM PHARMACEUTICALS PTE LTD
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