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Modified release famciclovir pharmaceutical compositions

A technology of famciclovir and composition, which is applied in the field of composition for improved release, and can solve problems such as not disclosed

Inactive Publication Date: 2008-04-30
NOVARTIS AG
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, modified-release formulations of famciclovir are not disclosed in the '007 patent

Method used

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  • Modified release famciclovir pharmaceutical compositions
  • Modified release famciclovir pharmaceutical compositions

Examples

Experimental program
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Effect test

preparation example Construction

[0047] The preparation of the pharmaceutical compositions of the present invention begins by mixing the therapeutic compound with a release retardant to form an extrudate using melt granulation. The release retardant may, for example, be present in an amount of from about 5% to about 40% by weight of the extrudate composition, such as from about 10% to about 35%, such as from about 25% to about 30%. Similarly, the therapeutic compound may be present in an amount of from about 60% to about 99% by weight of the extrudate composition, such as from about 70% to about 90%, such as from about 80% to about 85%.

[0048] For example the extrudate is subsequently ground to form granules which form the internal phase of the pharmaceutical composition. One of ordinary skill in the art will know the necessary particle size of the particles required to formulate a particular pharmaceutical composition. For example, suitable particle sizes include those of 1000 μm, 750 μm, 500 μm or 250 μm...

Embodiment 1

[0065] Internal phase ingredients: Famciclovir, PVA / PVP mixture (commercially available from BASF AG (Ludwigshafen, Germany) as KOLLIDON SR) and silicon dioxide were sieved through a #18 mesh sieve (i.e. 1 mm sieve) and a premix was prepared . The internal phase is then introduced into the feed section or funnel of the twin-screw extruder. A suitable twin-screw extruder is a PRISM 16 mm pharmaceutical twin-screw extruder commercially available from Thermo Electron Corp (Waltham, Massachusetts).

[0066] A twin-screw extruder is equipped with 4 separate barrel zones or sections and does not have a 5th zone (i.e. die). Starting from the funnel, the zones were heated to the following temperatures: 90°C, 90°C, 60°C and 40°C, respectively. The speed of the shaft was gradually increased to 150 rpm as the material was processed through the extruder.

[0067] The extrudate or pellets obtained from the extruder are then cooled to room temperature. After cooling the extrudate...

Embodiment 2

[0070] Element

[0071] Example 2 was prepared using the same method disclosed in Example 1, however, the concentrations of the ingredients were different.

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Abstract

A modified release pharmaceutical composition of famciclovir contains at least 60% by weight famciclovir with at least 5% by weight of a release retardant. Particularly useful as a release retardant include polymers, especially a mixture of polyvinyl acetate and polyvinylpyrrolidone. A method of making such pharmaceutical compositions using a extruder and a granulation method is particularly useful.

Description

field of invention [0001] The present invention relates to new pharmaceutical compositions of famciclovir, especially compositions with modified release. Background of the invention [0002] Famciclovir, or the compound 2-[2-(2-amino-9H-purin-9-yl)ethyl]-1,3-propanediol acetate, is an orally administered prodrug of the antiviral drug penciclovir. Penciclovir has inhibitory activity against herpes simplex virus type 1 (HSV-1), type 2 (HSV-2) and varicella zoster virus (VZV). [0003] Famciclovir, as currently marketed, is administered in the form of immediate release tablets containing 125, 250, 500 and 750 mg of therapeutic compound. These tablets contain conventional excipients used in solid oral dosage forms, such as lactose, sodium starch glycolate and magnesium stearate. These tablets are administered up to three times daily. [0004] Famciclovir is rapidly absorbed after oral administration of the immediate release formulation. This may be due to its high solubility...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K9/22A61K31/52
CPCA61K9/1635A61K9/1694A61K9/2077A61P31/12A61K9/16A61K9/20A61K31/52
Inventor W·Y·李李守峰
Owner NOVARTIS AG
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