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Modified release ibuprofen dosage form

a technology of ibuprofen and modified release, which is applied in the direction of biocide, drug composition, inorganic non-active ingredients, etc., can solve the problems of tablets sticking, not maintaining the therapeutic level of one treatment, and substantial delay between administration

Inactive Publication Date: 2007-04-05
SCOLR PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0004] In accordance with the foregoing, we have provided a solid dosage form for oral administration of ibuprofen comprising a modified release formulation of ibuprofen which provides an immediate bu

Problems solved by technology

They do not maintain therapeutic levels from one treatment over an extended period of time.
Formulations that claim extended release fail to have an initial burst of the drug and thus exhibit substantial delay between administration and the achievement of an effective therapeutic blood level.
It is known ibuprofen is not directly compressible, and attempts to directly manufacture ibuprofen results in tablets which stick to the faces of the tableting press, are too friable for storage or transport, or split into two or more segments when expelled from the tableting press.

Method used

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  • Modified release ibuprofen dosage form
  • Modified release ibuprofen dosage form
  • Modified release ibuprofen dosage form

Examples

Experimental program
Comparison scheme
Effect test

example 1

[0043] In one embodiment, the formulation comprised ibuprofen, hydroxypropyl methylcellulose (HPMC K15M and HPMC K100LV), glycine and sodium carbonate, in which HPMC K15M was present at a concentration of 18% by weight of ibuprofen, Ex. 1a, and at a concentration of 21% by weight of ibuprofen, Ex. 1b, HPMC K100LV was present at a concentration of 17% by weight of ibuprofen, glycine was present at a concentration of 2.5% by weight of ibuprofen, and sodium carbonate was present at a concentration of 17% by weight of ibuprofen within a monolithic compressed tablet. The specific formulations are as follows:

Ex. 1amgEx. 1bmgIbuprofen 90 grade600Ibuprofen 90 grade600HPMC K15M110HPMC K15M125HPMC K100LV100HPMC K100LV100MCC PH102100MCC PH102100Na2CO3, anhydrous150Na2CO3, anhydrous150Glycine15Glycine15Silica, Syloid 24420Silica, Syloid 24420Mg Stearate10Mg Stearate10Total:1105Total:1120

[0044] All ingredients were passed through a 30-mesh screen and blended with the remaining formulation comp...

example 2

[0046] In another embodiment, the formulation comprised ibuprofen, hydroxypropyl methylcellulose (HPMC K100M and HPMC K100LV), sodium carbonate, flow agents and tableting aids, in which HPMC K100M was present at a concentration of 17% by weight of ibuprofen, HPMC K100LV was present at a concentration of 17% by weight of ibuprofen, and sodium carbonate was present at a concentration of 25% by weight of ibuprofen within a compressed monolithic tablet. The specific formula is as follows:

Ex. 2mgIbuprofen600HPMC K100M100HPMC K100LV100Na2CO3, anhydrous150MCC PH102150Silica, Syloid 24420Mg Stearate10Total:1130

[0047] The formulation components were mixed in a V-blender. The resulting powder was compressed into tablets using conventional technologies. In this Example a combination of a medium to high viscosity HPMC and a low viscosity HPMC were used.

[0048] As shown in FIG. 2, the results of this Example demonstrate an in vitro release profile comprising a burst effect, followed by the sus...

example 3

[0049] In another embodiment, the formulation comprised ibuprofen, hydroxypropyl methylcellulose (HPMC K15M and HPMC K100LV), sodium carbonate, glycine, flow agents and tableting aids, in which HPMC K15M was present at a concentration of 17% by weight of ibuprofen, HPMC K100LV was present at a concentration of 17% by weight of ibuprofen and sodium carbonate was present at a concentration of 25% by weight of ibuprofen within a compressed monolithic tablet.

Ex. 3mgIbuprofen600HPMC K15M100HPMC K100LV100MCC PH102100Na2CO3, anhydrous150Glycine15Silica, Syloid 24420Mg Stearate10Total:1095

[0050] The formulation components were mixed in a V-blender. The resulting powder was compressed into tablets using conventional compression technology. In this Example a combination of a medium to high viscosity HPMC and a low viscosity HPMC was used.

[0051] As shown in FIG. 3, the results of this Example demonstrate an in vitro release profile comprising a burst effect providing release of 20% of ibupr...

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Abstract

The present invention is a solid dosage form for oral administration of ibuprofen comprising a modified release formulation of ibuprofen which provides an immediate burst effect and thereafter a sustained release of sufficient ibuprofen to maintain blood levels at least 6.4 μg / ml over an extended period of at least 8 hours following administering of a single dose.

Description

CROSS REFERENCE TO RELATED APPLICATIONS [0001] The present invention is a continuation-in-part of U.S. application Ser. No. 11 / 238,802, filed Sep. 29, 2005, which claims the benefit of U.S. Provisional Applications Nos. 60 / 614,932, filed Sep. 30, 2004 and 60 / 689,631, filed Jun. 10, 2005.BACKGROUND OF THE INVENTION [0002] Ibuprofen is 2-(4-isobutylphenyl)propionic acid and is a non-steroidal anti-inflammatory compound (NSAID), which exhibits high levels of anti-inflammatory, analgesic and antipyretic activities necessary for the effective treatment of rheumatoid arthritis and osteo-arthritis and other inflammatory conditions. Most dosage forms of ibuprofen are immediate release dosage forms that provide rapid onset of therapeutic action, then rapidly declining levels of active ingredient, necessitating repeated dosing. They do not maintain therapeutic levels from one treatment over an extended period of time. Repeat dosing is thus required at intervals of four to six hours. Formulati...

Claims

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Application Information

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IPC IPC(8): A61K31/192A61K9/20
CPCA61K9/2009A61K9/2013A61K9/2031A61K9/2054A61K31/192A61K47/02A61K47/183A61K47/38A61P19/02A61P29/00A61K9/20A61K9/2059
Inventor HITE, MICHAELFEDERICI, CATHYBRUNELLE, ALANTURNER, STEPHEN
Owner SCOLR PHARMA
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