Pharmaceutical formulation of carboxamide HIV integrase inhibitors containing a release rate control composition

摘要

A pharmaceutical formulation for oral administration as a solid dose, comprising an effective amount of a potassium salt of Compound A and a release rate control composition comprising high viscosity hydroxypropylmethyl cellulose, poloxamer and, optionally, lactose; wherein Compound A is: ** Formula ** and wherein the potassium salt of Compound A is employed in an amount ranging from about 5 to about 75% by weight on a free phenol basis; poloxamer is used in an amount in a range of from about 5 to about 25% by weight; high viscosity hydroxypropylmethyl cellulose is used in an amount ranging from about 2 to about 15% by weight; and lactose is used in an amount ranging from zero to about 15% by weight; and wherein the formulation further comprises a diluent and a lubricant; and wherein the diluent comprises microcrystalline cellulose and, optionally, calcium phosphate; and the lubricant comprises a metal stearate and a metal stearyl fumarate.