US2005226926A1PendingUtilityA1

Sustained-release tablet composition of pramipexole

39
Assignee: PFIZERPriority: Jul 25, 2002Filed: Jul 23, 2003Published: Oct 13, 2005
Est. expiryJul 25, 2022(expired)· nominal 20-yr term from priority
Inventors:Gregory AmidonLoksidh GanorkarJohn HeimlichErnest LeeRobert NoackJoseph P. ReoConnie Skoug
A61P 43/00A61P 25/16A61P 25/28A61P 25/00A61K 9/2059A61K 31/4745A61K 31/428A61K 9/2054A61K 9/2866A61K 9/20
39
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Claims

Abstract

A sustained-release pharmaceutical composition in a form of an orally deliverable tablet comprises a water-soluble salt of pramipexole, dispersed in a matrix comprising a hydrophilic polymer and a starch having a tensile strength of at least about 0.15 kN cm −2 at a solid fraction representative of the tablet.

Claims

exact text as granted — not AI-modified
1 . A sustained-release pharmaceutical composition in a form of an orally deliverable tablet comprising a water-soluble salt of pramipexole, dispersed in a matrix comprising a hydrophilic polymer and a starch having a tensile strength of at least about 0.15 kN cm −2  at a solid fraction representative of the tablet.  
     
     
         2 . The composition of  claim 1  wherein the starch has a tensile strength of at least about 0.175 kN cm −2 .  
     
     
         3 . The composition of  claim 1  wherein the starch has a tensile strength of at least about 0.2 kN cm −2 .  
     
     
         4 . The composition of  claim 1  wherein the starch is a pregelatinized starch.  
     
     
         5 . The composition of  claim 1  wherein the starch is present in an amount of about 25% to about 75% by weight.  
     
     
         6 . The composition of  claim 1  wherein the starch is present in an amount of about 40% to about 70% by weight.  
     
     
         7 . The composition of  claim 1  wherein the starch is present in an amount of about 45% to about 65% by weight.  
     
     
         8 . The composition of  claim 1  wherein the hydrophilic polymer is selected from the group consisting of methylcellulose, hydroxypropylmethylcellulose, carmellose sodium and carbomer.  
     
     
         9 . The composition of  claim 1  wherein the hydrophilic polymer is hydroxypropylmethylcellulose.  
     
     
         10 . The composition of  claim 1  wherein the hydrophilic polymer is present in an amount of about 20% to about 70% by weight.  
     
     
         11 . The composition of  claim 1  wherein the hydrophilic polymer is present in an amount of about 30% to about 60% by weight.  
     
     
         12 . The composition of  claim 1  wherein the hydrophilic polymer is present in an amount of about 35% to about 50% by weight.  
     
     
         13 . The composition of  claim 1  wherein the salt has solubility not less than about 50 mg/ml.  
     
     
         14 . The composition of  claim 1  wherein the salt has solubility not less than about 100 mg/ml.  
     
     
         15 . The composition of  claim 1  wherein the salt is pramipexole dihydrochloride.  
     
     
         16 . The composition of  claim 1  that comprises about 0.1 to about 10 mg pramipexole per tablet, expressed as pramipexole dihydrochloride monohydrate equivalent.  
     
     
         17 . The composition of  claim 1  that comprises about 0.2 to about 6 mg pramipexole per tablet, expressed as pramipexole dihydrochloride monohydrate equivalent.  
     
     
         18 . The composition of  claim 1  that comprises about 0.3 to about 5 mg pramipexole per tablet, expressed as pramipexole dihydrochloride monohydrate equivalent.  
     
     
         19 . The composition of  claim 1 , further comprising a coating on the tablet.  
     
     
         20 . The composition of  claim 19  wherein said coating is a release-controlling layer.  
     
     
         21 . The composition of  claim 20  wherein said release-controlling layer constitutes about 1% to about 15% by weight of the tablet.  
     
     
         22 . The composition of  claim 19  wherein said coating is a nonfunctional coating.  
     
     
         23 . A pharmaceutical composition in a form of an orally deliverable tablet having a core comprising pramipexole dihydrochloride monohydrate in an amount of about 0.375, 0.75, 1.5, 3 or 4.5 mg, dispersed in a matrix comprising (a) HPMC type 2208 in an amount of about 35% to about 50% by weight of the tablet and (b) a pregelatinized starch having a tensile strength of at least about 0.15 kN cm −2  at a solid fraction of 0.8, in an amount of about 45% to about 65% by weight of the tablet; said core being substantially enclosed in a coating that constitutes about 2% to about 7% of the weight of the tablet, said coating comprising an ethylcellulose-based hydrophobic or water-insoluble component and an HPMC-based pore-forming component in an amount of about 10% to about 40% by weight of the ethylcellulose-based component.  
     
     
         24 . A method of treatment of a subject having a condition or disorder for which a dopamine D 2  receptor agonist is indicated, the method comprising orally administering to the subject the pharmaceutical composition of any of the preceding claims.  
     
     
         25 . The method of  claim 24  wherein the composition is administered not more than once daily.  
     
     
         26 . The method of  claim 24  wherein the condition or disorder is Parkinson's disease or a complication associated therewith.

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