| 主权项 |
1. A modified release pharmaceutical composition comprising a mixture of immediate release febuxostat beads in an amount ranging from approximately 20% to approximately 40% (w/w) of the total composition weight and delayed release febuxostat beads having a solubility at pH levels greater than or equal to 6.8 in an amount ranging from approximately 60% to approximately 80% (w/w) of the total composition weight, wherein the beads are incorporated into an oral dosage form selected from the group consisting of a pill, a tablet, and a capsule, wherein febuxostat is the only active agent in the modified release pharmaceutical composition,
wherein the immediate release beads comprise (a) an inert core in an amount ranging from about 50% to about 55% (w/w) of the weight of the immediate release bead, and (b) an immediate release layer that encapsulates the inert core comprising a mixture of febuxostat and hydroxypropyl methylcellulose in an amount ranging from about 45% to about 50% (w/w) of the weight of the immediate release bead, the ratio of febuxostat to hydroxypropyl methylcellulose ranging from about 1.5 to about 3; and wherein the delayed release beads comprise (a) an inert core in an amount ranging from about 40.5% to about 43% (w/w) of the weight of the delayed release bead, (b) an immediate release layer encapsulating the inert core comprising a mixture of febuxostat and hydroxypropyl methylcellulose in an amount ranging from about 35% to about 40% (w/w) of the weight of the delayed release bead, the ratio of febuxostat to hydroxypropyl methylcellulose ranging from about 1.5 to about 3, (c) a delayed release enteric polymer layer encapsulating the immediate release layer comprising a delayed release enteric polymer in an amount ranging from about 1% to about 20% (w/w) of the delayed release bead, the delayed release enteric polymer comprising a mixture of methacrylic acid copolymer type A and methacrylic acid copolymer type B in a ratio ranging from approximately 0.1 to approximately 0.5, and (d) a plasticizer in an amount ranging from about 1% to about 3% (w/w) of the weight of the delayed-controlled release bead, the plasticizer comprising triethyl citrate. |
