Composition

a technology of compositions and compositions, applied in the field of pharmaceutical compositions, can solve the problems of inconvenient long-term treatment of sub-chronic or chronic pain, and achieve the effect of prolonging the treatment time and improving the effect of pain

Inactive Publication Date: 2011-07-21
SMITHKLINE BEECHAM LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although this regimen is acceptable in the short-term treatment of acute pain, it becomes inconvenient in the context of long-term treatment of sub-chronic or chronic pain.

Method used

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Examples

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example 1

[0051]This Example compares the properties of a commercially available immediate release 500 mg paracetamol tablet with two prototype sustained release bilayer tablets (Formulations A and B) which both have an in vitro dissolution profile outside the scope of the present invention.

[0052]These prototype tablets containing a total of about 650 mg of paracetamol were prepared from the following ingredients:

Tablet Formulation ATablet Formulation BIngredientmg / tablet% w / wmg / tablet% w / wSustained Release LayerParacetamol264.0834.75403.3952.10High viscosity HPMC18.962.4928.963.74Pregelatinised Starch21.052.7732.154.15Polyvinylpyrrolidone5.880.778.981.16Low viscosity HPMC5.090.677.771.00Magnesium Stearate0.950.121.450.19Immediate Release LayerDirectly compressible436.0057.36283.536.62paracetamol granulationDC90#(Paracetamol content in(389.80)(51.28)(260.00)(33.58)DC90)Film and Wax Coating8.051.068.051.04Total760.05100.000774.25100.00% w / w SR:IR APAP41.1:59.960.5:39.5# DC90 is a commercially ...

example 2

[0057]This Example compares the properties of a commercially available immediate release 500 mg paracetamol tablet with a sustained release bilayer tablet (Formulation C) having an in vitro dissolution profile falling within the scope of the present invention.

[0058]This advantageous bilayer tablet containing a total of 666.6 mg of paracetamol was prepared from the following ingredients:

Tablet Formulation CIngredientmg / tablet% w / wSustained Release LayerParacetamol473.5764.39High viscosity HPMC15.432.10Pregelatinised Starch5.140.70Polyvinylpyrrolidone10.281.40Low viscosity HPMC8.231.12Magnesium Stearate1.540.21Immediate Release LayerDirectly compressible214.9229.22paracetamol granulationDC90(Paracetamol content in(193.43)(26.30)DC90)Film and Wax Coating6.3050.86Total735.42100.00% w / w SR:IR APAP71:29

[0059]The release profile of test formulation C was characterised using the USP type III apparatus (reciprocating basket) as hereinbefore described and was found to have the following disso...

example 3

[0063]This Example compares the properties of a commercially available immediate release 500 mg paracetamol tablet with another sustained release bilayer tablet (Formulation D) having an in vitro dissolution profile falling within the scope of the present invention.

[0064]The bilayer tablet of Formulation D was essentially similar to Formulation C but contained a total of 665 mg of paracetamol and had a slightly different ratio of sustained release to immediate release paracetamol (% w / w SR:IR APAP was 69:31).

[0065]The release profile of test formulation D was characterised using the USP type III apparatus (reciprocating basket) as hereinbefore described and was found to have the following dissolution rate as detailed in table 3.

TABLE 3Dissolution Profile for Formulation DTimeIn-vitro release Results(minutes)(% paracetamol released)1540.8%6065.0%12090.2%180101.8%

[0066]Formulation D was assessed in a further biostudy which involved 27 subjects. The study was an open multiple dose cros...

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Abstract

A pharmaceutical composition comprising an immediate release phase and a sustained release phase of paracetamol is described which has a unique in vitro dissolution profile resulting in advantageous pharmacokinetic properties.

Description

RELATED APPLICATION INFORMATION[0001]This application is a continuation of application Ser. No. 10 / 257,077, filed 6 Jun. 2003, (allowed) which is a §371 national stage entry of International Application No. PCT / EP01 / 04302, filed 12 Apr. 2001, which claims the benefit of priority from GB 0009522.4, filed 19 Apr. 2000.BACKGROUND OF THE INVENTION[0002]The present invention relates to pharmaceutical compositions containing N-acetyl-p-aminophenol, known by the generic names paracetamol, acetaminophen and APAP (hereinafter referred to as paracetamol). In particular, the invention relates to a sustained release paracetamol formulation having an advantageous pharmacokinetic profile.[0003]Paracetamol is an analgesic and antipyretic agent which is widely used in prescription and non-prescription medicines, often in combination with other biologically active compounds.[0004]The elimination half-life of paracetamol is reported to be in the range of 1.9-2.5 hours. Its absorption following oral d...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K9/24A61K31/167A61P25/00A61K9/22A61K9/52A61K47/32A61K47/38
CPCA61K31/167A61K9/209A61P25/00A61P29/00
Inventor CHAN, SHING YUEGRATTAN, TIMOTHY JAMESSENGMANEE, BOUNKHIENE
Owner SMITHKLINE BEECHAM LTD
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