NOVEL CLONIDINE FORMULATION
An oral clonidine dosage unit providing a twenty-four hour extended release profile following a single dose administration is provided. The dosage unit comprises a pharmaceutically effective amount of a coated complex comprising clonidine bound to a cationic exchange resin, which is characterized by a twenty-four hour release profile with a single peak, wherein said oral clonidine dosage unit provides a therapeutically effective plasma concentration for at least about 70%, or at least 85% of the twenty-four hour period following the single dose administration. Both liquid and solid formulations are provided, as are methods of treating a patient by a single administration of a formulation of the invention so as to achieve a therapeutic effect for 24-hours.
1 . An oral clonidine composition having a single plasma concentration peak following a single oral dose in a 24-hour period, said dosage unit comprising:
pharmaceutically effective amount of cured, modified release barrier coated, clonidine-cation exchange resin complex-matrix particles which comprise clonidine bound to a cationic exchange resin in a ratio of about 1:120 to about 1:180 clonidine to cation exchange resin in a particulate matrix with a matrix forming component, said matrix forming component comprising a water-insoluble polymer or copolymer or hydrophilic polymer or copolymer, said cured barrier coating comprising polyvinylacetate and a plasticizer and being a cured, water-permeable, high tensile strength, water-insoluble, barrier coating having an elongation factor in the range of about 150% to 400%, wherein said cured barrier coating is over the clonidine-cation exchange resin complex-matrix particles.
2 . The oral clonidine composition according to claim 1 , wherein the clonidine-cation exchange resin complex-matrix comprises a hydrophilic polymer.
3 . The oral clonidine composition according to claim 1 , wherein the hydrophilic polymer is polyvinylpyrrolidone.
4 . The oral clonidine composition according to claim 1 , wherein the matrix polymer is about 5% w/w to about 20% w/w added to the uncoated clonidine-cation exchange resin complex.
5 . The oral composition according to claim 1 , wherein the cured barrier coating comprises about 70% w/w to about 90% w/w polyvinylacetate and about 2.5% w/w to about 10% w/w plasticizer.
6 . A method for delivering an effective amount of clonidine for a twenty-four hour period which provides a single peak plasma concentration, the method comprising administering to a subject a single oral clonidine composition according to claim 1 in the evening.