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Sustained release paracetamol formulations

A technology of acetaminophen and sustained-release preparations, which is applied in the direction of anti-inflammatory agents, pill delivery, non-central analgesics, etc., and can solve problems such as difficulty in reaching and pharmacokinetic curves

Inactive Publication Date: 2014-03-19
GLAXO SMITHKLINE LLC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Achieving a suitable pharmacokinetic profile with twice-daily dosing has been found to be extremely difficult
Years of experimentation failed to achieve the desired concentration levels in the necessary time

Method used

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  • Sustained release paracetamol formulations
  • Sustained release paracetamol formulations
  • Sustained release paracetamol formulations

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0227] In a first example, bilayer extended release acetaminophen tablets were prepared using the following ingredients:

Embodiment -1

[0228] Embodiment-1 (two-layer tablet)

[0229]

[0230] The total tablet weight is about 1100 mg, about 1000 mg of acetaminophen per tablet. Layer 1 had a total weight of about 1000 mg (about 900.0 mg acetaminophen) and Layer 2 had a total weight of about 110 mg (about 100 mg acetaminophen). A mixture of the layers is prepared and the layers are compressed on a rotary bilayer tablet press of suitable size.

[0231] Instructions for the preparation of the sustained release layer:

[0232] 1. Mix acetaminophen, HPMC2208, PVP, HPMC2910 and pregelatinized starch in a high shear granulator.

[0233] 2. Add purified water while mixing.

[0234] 3. Continue mixing until a suitable granulation endpoint is reached.

[0235] 4. Dry the pellets to target %LOD.

[0236] 5. Mill the dried granules using a Co-mill fitted with a suitable classifying screen.

[0237] 6. Add the lubricant magnesium stearate and mix.

[0238] 7. The mixture is now ready for pressing.

[0239] Instru...

Embodiment 2

[0242] In another embodiment, a monolayer extended release acetaminophen tablet is prepared using the following ingredients:

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Abstract

The present invention is directed to twice daily sustained release pharmaceutical composition of paracetamol having an immediate release phase of paracetamol and a sustained release phase of paracetamol, said composition having unique and advantageous pharmacokinetic properties and a pharmaceutical composition comprising only a sustained release phase of paracetamol having unique and advantageous pharmacokinetic properties.

Description

field of invention [0001] The present invention relates to a twice-daily sustained release pharmaceutical composition of acetaminophen, which has an immediate release phase and a sustained release phase of acetaminophen and has unique and favorable pharmacokinetic properties. Background of the invention [0002] The present invention relates to a pharmaceutical composition containing N-acetyl-p-aminophenol (commonly known as acetaminophen, paracetamol and APAP, hereinafter referred to as acetaminophen). In particular, the present invention relates to sustained release acetaminophen formulations, which have favorable pharmacokinetic properties. [0003] Acetaminophen is an antipyretic and analgesic drug widely used in prescription and over-the-counter drugs, which is often combined with other biologically active compounds such as various opioid derivatives. [0004] The reported elimination half-life of acetaminophen ranges from 1.9 to 2.5 hours. Following an oral dose of a...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/22A61K31/167
CPCA61K31/167A61K9/2059A61K9/2054A61K9/209A61P9/02A61P29/00A61P29/02
Inventor C.V.布安D.刘K.梅格帕拉
Owner GLAXO SMITHKLINE LLC