MODIFIED RELEASE FORMULATIONS OF A BUPROPION SALT
The present invention relates to pharmaceutical compositions, formulations and medicaments comprising a bupropion salt, in particular, modified-release tablets comprising an effective amount of bupropion hydrobromide, and the use of the bupropion salt to prepare a medicament to treat a condition.
1 . A microparticle comprising a solid core, said core comprising bupropion hydrobromide and at least one pharmaceutically acceptable excipient, said core of said microparticle being at least partially surrounded by a controlled release coat which permits entry of an aqueous liquid into the core and delivery of the bupropion hydrobromide from the core to the exterior of the microparticle through the controlled release coat.
2 . The microparticle of claim 1 , wherein said bupropion hydrobromide is in admixture with said at least one pharmaceutically acceptable excipient.
3 . The microparticle of claim 1 , wherein said microparticle exhibits an in-vitro release rate such that after 2 hours from 0 to 20% by weight of the bupropion hydrobromide is released, after 4 hours from 15% to 45% by weight of the bupropion hydrobromide is released, after 8 hours, from 40% to 90% by weight of the bupropion hydrobromide is released, and after 16 hours, more than 80% by weight of the bupropion hydrobromide is released.
4 . The microparticle of claim 1 , wherein said microparticle exhibits an in-vitro release rate such that after 2 hours no more than 40% is released, after 4 hours from 40-75% is released, after 8 hours at least 75% is released and after 16 hours at least 85% is released.
5 . The microparticle of claim 1 , comprising a sugar sphere or nonpareil bead coated with at least one layer comprising bupropion hydrobromide and at least one pharmaceutically acceptable excipient and/or osmagent, said at least one layer surrounded by a semipermeable membrane, said microparticle exhibiting an in-vitro release rate such that after 2 hours from 0 to 20% by weight of the bupropion hydrobromide is released, after 4 hours from 15% to 45% by weight of the bupropion hydrobromide is released, after 8 hours, from 40% to 90% by weight of the bupropion hydrobromide is released, and after 16 hours, more than 80% by weight of the bupropion hydrobromide is released.
6 . A microparticle comprising a homogenous solid core, said core comprising bupropion hydrobromide and at least one pharmaceutically acceptable excipient, osmagent, and/or absorption enhancer, said microparticles compressed into a tablet, said tablet surrounded by a semipermeable membrane which permits entry of an aqueous liquid into the core and delivery of the bupropion hydrobromide from the tablet interior to the exterior thereof through at least one passageway in the semipermeable membrane and/or by diffusion through the semipermeable membrane.
7 . The microparticle of claim 1 , wherein said core comprises an osmopolymer.
8 . The microparticle of claim 5 , wherein said core comprises an osmopolymer.
9 . The microparticle of claim 6 , wherein said core comprises an osmopolymer.