US2006093671A1PendingUtilityA1

Controlled release galantamine composition

48
Individually held — no corporate assignee on recordPriority: Dec 24, 1998Filed: Dec 15, 2005Published: May 4, 2006
Est. expiryDec 24, 2018(expired)· nominal 20-yr term from priority
Inventors:John P. McgeePaul Marie Victor GilisMarc Maurice Germain De WeerValentin Florent De CondeHerman Johannes De BruijnFrederic Van Dycke
A61P 43/00A61P 25/28A61P 25/14A61P 25/18A61P 25/30A61K 9/5078A61K 9/2072A61K 9/4858A61K 9/4866A61K 31/55
48
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Claims

Abstract

The present invention is concerned with controlled release compositions for oral administration comprising galantamine; and with processes of preparing such controlled release compositions.

Claims

exact text as granted — not AI-modified
1 - 14 . (canceled)  
     
     
         15 . A controlled release formulation comprising galantamine or a pharmaceutically acceptable salt thereof as the active ingredient and a pharmaceutically acceptable excipient wherein the formulation is capable of releasing in USP buffer pH 6.8 at 37° C. in an Apparatus 2 (USP 23, <711> Dissolution, pp 1791-1793, paddle, 50 rpm) from 20 to 40% of the total amount of the active ingredient in 1 hour, and more than 80% of the total amount of the active ingredient in 10 hours.  
     
     
         16 . A dosage form comprising a therapeutically effective amount of the controlled release formulation of  claim 15 .  
     
     
         17 . A dosage form according to  claim 16  which delivers a therapeutically effective amount of the active ingredient to a patient during the 24 hours following a single once daily administration.  
     
     
         18 . A dosage form according to  claim 16  wherein part of the active ingredient is present in an immediate release form.  
     
     
         19 . A dosage form according to  claim 16  wherein the active ingredient is galantamine hydrobromide.  
     
     
         20 . A formulation according to  claim 15  wherein the active ingredient is galantamine hydrobromide.  
     
     
         21 . A dosage form according to  claim 18  wherein said immediate release form comprises a topcoat comprising galantamine and a water-soluble polymer.  
     
     
         22 . A dosage form according to  claim 16  providing a mean maximum plasma concentration of galantamine from 10 to 60 ng/ml and a mean minimum plasma concentration from 3 to 15 ng/ml after repeated administration every day through steady- state conditions.  
     
     
         23 . A pharmaceutical package suitable for commercial sale comprising a container, a formulation of galantamine as claimed in  claim 15 , and associated with said package written matter specifying how said formulation should be administered.  
     
     
         24 . (canceled)  
     
     
         25 . (canceled)  
     
     
         26 . (canceled)  
     
     
         27 . A method of treating Alzheimer's dementia and related dementias in a human while substantially reducing an adverse effect associated with acetyl cholinesterase inhibitors; comprising administering to a human in need of such treatment; a therapeutically effective amount of the controlled release formulation of  claim 15 , said amount being sufficient to alleviate said Alzheimer's dementia and related dementias, but insufficient to cause said adverse effect.  
     
     
         28 . A method according to  claim 27  wherein the related dementia belongs to the group consisting of vascular dementia, Lewy body disease, autism, mental retardation, bipolar disorder psychiatric conditions, disruptive behaviour, attention deficit, hyperactivity disorder, substance abuse, and extreme aggression, especially conduct disorder.  
     
     
         29 . A method according to  claim 27  wherein the adverse effects effect is selected from the group consisting of nausea, vomiting, sweating, restlessness, and insomnia.  
     
     
         30 . A method according to  claim 27 , wherein the adverse effect is selected from the group consisting of nausea and vomiting.  
     
     
         31 . A method according to  claim 30  wherein the adverse effect is nausea.  
     
     
         32 . A method according to  claim 30  wherein the adverse effect is vomiting.  
     
     
         33 . A method of treating Alzheimer's disease in a human while substantially reducing an adverse effect associated with acetyl cholinesterase inhibitors comprising administering to a human in need of such treatment a therapeutically effective amount of the formulation of  claim 15 .  
     
     
         34 . A method according to  claim 33 , wherein the adverse effect is selected from the group consisting of nausea and vomiting.  
     
     
         35 . A method according to  claim 34 , wherein the adverse effect is nausea.  
     
     
         36 . A method according to  claim 34 , wherein the adverse effect is vomiting.  
     
     
         37 . A formulation according to  claim 15 , wherein the formulation provides a therapeutically effective amount of the active ingredient while substantially reducing an adverse effect selected from the group consisting of nausea and vomiting upon administration of the formulation to a human.  
     
     
         38 . A formulation according to  claim 15 , wherein the formulation provides a therapeutically effective amount of the active ingredient while substantially reducing an adverse effect of nausea upon administration of the formulation to a human.  
     
     
         39 . A formulation according to  claim 15 , wherein the formulation provides a therapeutically effective amount of the active ingredient while substantially reducing an adverse effect of vomiting upon administration of the formulation to a human.  
     
     
         40 . A dosage form according to  claim 16 , wherein the dosage form provides a therapeutically effective amount of the active ingredient while substantially reducing an adverse effect selected from the group consisting of nausea and vomiting upon administration of the dosage form to a human.  
     
     
         41 . A dosage form according to  claim 16 , wherein the dosage form provides a therapeutically effective amount of the active ingredient while substantially reducing an adverse effect of nausea upon administration of the dosage form to a human.  
     
     
         42 . A dosage form according to  claim 16 , wherein the dosage form provides a therapeutically effective amount of the active ingredient while substantially reducing an adverse effect of vomiting upon administration of the dosage form to a human.  
     
     
         43 . A dosage form comprising galantamine or a pharmaceutically acceptable salt thereof as the active ingredient and a pharmaceutically acceptable excipient wherein the dosage form releases from 33.4 to 39.5% of the total amount of the active ingredient in 1 hour when tested in USP buffer pH 6.8 at 37° C. in an Apparatus 2 (USP 23, <711> Dissolution, pp 1791-1793, paddle, 50 rpm).  
     
     
         44 . A dosage form according to  claim 43 , wherein the dosage form releases from 55.1 to 60.9% of the total amount of the active ingredient in 2 hours.  
     
     
         45 . A dosage form according to  claim 43 , wherein the dosage form releases from 81.8 to 91.2% of the total amount of the active ingredient in 4 hours.  
     
     
         46 . A dosage form according to  claim 44 , wherein the dosage form releases from 95.9 to 105.8% of the total amount of the active ingredient in 8 hours.  
     
     
         47 . A dosage form according to  claim 43 , wherein the active ingredient is galantamine hydrobromide.  
     
     
         48 . A dosage form according to  claim 47 , wherein the dosage form provides a therapeutically effective amount of the active-ingredient while substantially reducing an adverse effect selected from the group consisting of nausea and vomiting upon administration of the dosage form to a human.  
     
     
         49 . A dosage form according to  claim 47 , wherein the dosage form provides a therapeutically effective amount of the active ingredient while substantially reducing an adverse effect of nausea upon administration of the dosage form to a human.  
     
     
         50 . A dosage form according to  claim 47 , wherein the dosage form provides a therapeutically effective amount of the active ingredient while substantially reducing an adverse effect of vomiting upon administration of the dosage form to a human.  
     
     
         51 . A method of treating Alzheimer's disease in a human while substantially reducing an adverse effect associated with acetyl cholinesterase inhibitors selected from the group consisting of nausea and vomiting comprising administering to a human in need of such treatment a dosage form of  claim 43 .  
     
     
         52 . A method according to  claim 51 , wherein the adverse effect is nausea.  
     
     
         53 . A method according to  claim 51 , wherein the adverse effect is vomiting.  
     
     
         54 . A formulation according to  claim 20  which delivers a therapeutically effective amount of galantamine to a patient during the 24 hours following a single once daily administration.  
     
     
         55 . A dosage form according to  claim 43  which delivers a therapeutically effective amount of galantamine to a patient during the 24 hours following a single once daily administration.  
     
     
         56 . A dosage form comprising galantamine or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable excipient which delivers a therapeutically effective amount of galantamine to a patient during the 24 hours following a single once. daily administration and wherein the dosage form provides a mean maximum plasma concentration of galantamine from 10 to 60 ng/ml and a mean minimum plasma concentration from 3 to 15 ng/ml after repeated administration every day through steady-state conditions.  
     
     
         57 . A dosage form according to  claim 56 , wherein the dosage form provides a therapeutically effective amount of the active ingredient while substantially reducing an adverse effect selected from the group consisting of nausea and vomiting upon administration of the dosage form to a human.  
     
     
         58 . A dosage form according to  claim 56 , wherein the dosage form provides a therapeutically effective amount of the active ingredient while substantially reducing an adverse effect of nausea upon administration of the dosage form to a human.  
     
     
         59 . A dosage form according to  claim 56 , wherein the dosage form provides a therapeutically effective amount of the active ingredient while substantially reducing an adverse effect of vomiting upon administration of the dosage form to a human.  
     
     
         60 . A method of treating Alzheimer's disease in a human while substantially reducing an adverse effect associated with acetyl cholinesterase inhibitors comprising administering to a human in need of such treatment a dosage form, of  claim 56 .  
     
     
         61 . A method according to  claim 60 , wherein the adverse effect is selected from the group consisting of nausea and vomiting.  
     
     
         62 . A method according to  claim 61 , wherein the adverse effect is nausea.  
     
     
         63 . A method according to  claim 61 , wherein the adverse effect is vomiting.

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