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US 6,296,873 B1Granted
Zero-order sustained release delivery system for carbamazephine derivatives
AssigneeYissum Research Development Company of the Hebrew University of Jerusalem
InventorsIfat Katzhendler, Michael Friedman
Life of this patent
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Abstract
A zero-order sustained-release delivery system for delivery of carbamazepine or a derivative thereof. A polymeric matrix formulation of carbamazepine comprises hydrophilic polymer or hydrophilic/hydropholic polymer mixture which permits carbamazepine or carbamezepine derivative to be released from the polymer matrix in zero-order release kinetics.
Claims19
An erodible oral composition for sustained release delivery of carbamazepine or a derivative thereof at a zero-order release kinetics comprising:
- (a) carbamazepine or the derivative thereof;
- (b) an erodible polymeric matrix comprising at least one hydrophilic polymer or a mixture of two or more hydrophilic polymers, having viscosity between about 3 and about 100,000 mpa.s (cp) at concentration of 2% at 20° C. and a molecular weight between about 10,000 and about 246,000;
- wherein said composition erodes and releases carbamazepine or the derivative thereof in a zero-order release kinetics.
An erodible tablet for oral sustained delivery of carbamazepine or a derivative thereof released from the tablet in a zero-order release kinetics, said tablet comprising carbamazepine or a derivative thereof selected from the group consisting of:
- 10,11-dihydro-10-oxo-5H-dibenz/b,f/azepine-5-carboxamide/(oxcarbazepine);
- 10,11-dihydro-10-hydroxy-5H-dibenz/b,f/azepine-5-carboxamide;
- 10-acetoxy-10,11-dihydro-5H-dibenz/b,f/azepine-5-carboxamide;
- 10-benzoyloxy-10,11-dihydro-5H-dibenz/b,f/azepine-5-carboxamide;
- 10-(4-methoxybenzoyloxy)-10,11-dihydro-5H-dibenz/b,f/azepine-5-carboxamide;
- 10-(3-methoxybenzoyloxy)-10,11-dihydro-5H-dibenz/b,f/azepine-5-carboxamide;
- 10-(2-methoxybenzoyloxy)-10,11-dihydro-5H-dibenz/b,f/azepine-5-carboxamide;
- 10-(4-nitrobenzoyloxy)-10,11-dihydro-5H-dibenz/b,f/azepine-5-carboxamide;
- 10-(3-nitrobenzoyloxy)-10,11-dihydro-5H-dibenz/b,f/azepine-5-carboxamide;
- 10-(2-nitrobenzoyloxy)-10,11-dihydro-5H-dibenz/b,f/azepine-5-carboxamide;
- 10-(4-chlorobenzoyloxy)-10,11-dihydro-5H-dibenz/b,f/azepine-5-carboxamide;
- 10-(3-chlorobenzoyloxy)-10,11-dihydro-5H-dibenz/b,f/azepine-5-carboxamide;
- 10-(2-acetoxybenzoyloxy)-10,11-dihydro-5H-dibenz/b,f/azepine-5-carboxamide;
- 10-propionyloxy-10,11-dihydro-5H-dibenz/b,f/azepine-5-carboxamide;
- 10-butyryloxy-10,11-dihydro-5H-dibenz/b,f/azepine-5-carboxamide;
- 10-pivaloyloxy-10,11-dihydro-5H-dibenz/b,f/azepine-5-carboxamide;
- 10-[(2-propyl)pentanoyloxy]-10,11-dihydro-5H-dibenz/b,f/azepine-5-carboxamide;
- 10-[(2-ethyl)hexanoyloxy]-10,11-dihydro-5H-dibenz/b,f/azepine-5-carboxamide;
- 10-stearoyloxy-10,11-dihydro-5H-dibenz/b,f/azepine-5-carboxamide;
- 10-clopentanoyloxy-10,11-dihydro-5H-dibenz/b,f/azepine-5-carboxamide;
- 10-cyclohexanoyloxy-10,11-dihydro-5H-dibenz/b,f/azepine-5-carboxamide;
- 10-phenylacetoxy-10,11-dihydro-5H-dibenz/b,f/azepine-5-carboxamide;
- 10-(4-methoxyphenyl)acetoxy-10,11-dihydro-5H-dibenz/b,f/-azepine-5-carboxamide;
- 10-(3-methoxyphenyl)acetoxy-10,11-dihydro-5H-dibenz/b,f/-azepine-5-carboxamide;
- 10-(4-nitrophenyl)acetoxy-10,11-dihydro-5H-dibenz/b,f/azepine-5-carboxamide;
- 10-(3-nitrophenyl)acetoxy-10,11-dihydro-5H-dibenz/b,f/azepine-5-carboxamide;
- 10-nicotinoyloxy-10,11-dihydro-5H-dibenz/b,f/azepine-5-carboxamide;
- 10-isonicotinoyloxy-10,11-dihydro-5H-dibenz/b,f/azepine-5-carboxamide;
- 10-(4-aminobutanoyloxy)-10,11-dihydro-5H-dibenz/b,f/azepine-5-carboxamide;
- 10-(2-amino-3-methylbutanoyloxy)-10,11-dihydro-5H-dibenz/b,f/-azepine-5-carboxamide;
- 10-chloroacetoxy-10,11-dihydro-5H-dibenz/b,f/azepine-5-carboxamide;
- 10-bromoacetoxy-10,11-dihydro-5H-dibenz/b,f/azepine-5-carboxamide;
- 10-formyloxy-10,11-dihydro-5H-dibenz/b,f/azepine-5-carboxamide;
- 10-ethoxycarbonyloxy-10,11-dihydro-5H-dibenz/b,f/azepine-5-carboxamide;
- 10-(2-chloropropionyloxy)-10,11-dihydro-5H-dibenz/b,f/azepine-5-carboxamide;
- 10,11-dihydro-10-hydroxyimino-5H-dibenz/b,f/azepine-5-carboxamide;
- 10,11-benzyloxyimino-10,11-dihydro-5H-dibenz/b,f/azepine-5-carboxamide;
- 10-acetyloxyimino-10,11-dihydro-5H-dibenz/b,f/azepine-5-carboxamide;
- 10,11-dihydro-10-propionyloxyimino-5H-dibenz/b,f/azepine-5-carboxamide;
- 10-butyroyloxyimino-10,11-dihydro-5H-dibenz/b,f/azepine-5-carboxamide;
- 10,11-dihydro-10-pivaloyloxyimino-5H-dibenz/b,f/azepine-5-carboxamide;
- 10,11-dihydro-10-[(1-napthoyloxy)imino]-5H-dibenz/b,f/azepine-5-carboxamide;
- 10-benzoyloxyimino-10,11-dihydro-5H-dibenz/b,f/azepine-5-carboxamide;
- 10,11-dihydro-10-succinoyloxyimino-5H-dibenz/b,f/azepine-5-carboxamide;
- 10,11-dihydro-10-glutaroyloxyimino-5H-dibenz/b,f/azepine-5-carboxamide;
- 10,11-dihydro-10-isobutoxycarbonyloxyimino-5H-dibenz/b,f/azepine-5-carboxamide;
- 10,11-dihydro-10-methoxyimino-5H-dibenz/b,f/azepine-5-carboxamide;
- 10,11-dihydro-10-(S)-(—)-camphanoyloxyimino 5H-dibenz/b,f/azepine-5-carboxamide;
- 10,11-dihydro-10-[(3-ethoxybenzoyloxyimino)]-5H-dibenz/b,f/azepine-5-carboxamide;
- 10,11-dihydro-10-nicotinoyloxyimino-5H-dibenz/b,f/azepine-5-carboxamide;
- 10,11-dihydro-10-ethoxycarbonyloxyimino-5H-dibenz/b,f/azepine-5-carboxamide;
- 10-butoxycarbonyloxyimino-10,11-dihydro-5H-dibenz/b,f/azepine-5-carboxamide;
- and
- 10-benzyloxycarbonyloxyimino-10,11-dihydro-5H-dibenz/b,f/azepine-5-carboxamide
- formulated in a polymeric matrix comprising a mixture of at least one hydrophilic polymer and at least one hydrophobic polymer, wherein said hydrophilic polymer having viscosity between about 3 and about 100,000 mPa.s(cp) at concentration of 2% at 20° C. and a molecular weight between about 10,000 and about 246,000;
- wherein said composition erodes and releases carbamazepine or the derivative thereof in a zero-order release kinetics.
53 more elements
A method for a sustained and controlled zero-order release kinetics of drug delivery comprising:
- (a) preparation of erodible formulation in form of an erodible tablet, erodible capsule or erodible granules comprising a matrix consisting of carbamazepine or a carbamazepine derivative in admixture with a hydrophilic polymer having a viscosity between about 3 and about 100,000 mpa.s cp concentration of 2% at 20 or in admixture with a mixture of the hydrophilic and a hydrophobic polymer;
- and
- (b) administering said erodible formulation orally to a patient wherein upon contact of the erodible formulation with aqueous condition of the digestive system, the formulation erodes at a zero-order release kinetics and releases carbamazepine or a derivative thereof in the zero-order release kinetics.
Dependencies are inferred from the claim text.