Patent ID: 7163696

Claim:
A controlled-release pharmaceutical formulation for oral administration comprising 4-amino-6,7-dimethoxy-2-(5-methanesulfonamido-1,2,3,4-tetrahydroisoquinol-2-yl)-5-(2-pyridyl)quinazoline or a pharmaceutically acceptable salt thereof; about 22.5% to about 40% by weight hydroxypropylmethylcellulose; about 25% by weight adipic acid; about 7.6% to about 10.2% by weight lactose monohydrate; about 22.8% to about 30.6% by weight anhydrous calcium hydrogen phosphate; 1% by weight magnesium stearate; and a pharmaceutically acceptable adjuvant, diluent or carrier; characterized in that the formulation is adapted to release at least 50% by weight of the 4-amino-6,7-dimethoxy-2-(5-methanesulfonamido-1,2,3,4-tetrahydroisoquinol-2-yl)-5-(2-pyridyl)quinazoline or the pharmaceutically acceptable salt thereof, after six hours, at least 30% by weight after 3 hours, and less than 30% by weight after one hour, in Apparatus 1 described in the United States Pharmacopoeia 24 (2000), pp 1941–1943, having 1 litre vessel, baskets of 40 mesh (0.4 mm apertures), a rotation speed of 100 rpm, and a dissolution medium consisting of 900 ml of 0.01 M hydrochloric acid containing 0.7% w/v sodium chloride at 37° C. wherein the hydroxypropylmethyl cellulose has a number average molecular weight in the range 20,000–250,000, has a degree of methyl substitution in the range of about 15% to about 35%, has a degree of hydroxy substitution in the range of about 2% to about 15% and wherein the nominal viscosity of a 2% aqueous solution of the hydroxypropylmethylcellulose lies in the range of about 50 to about 150,000 cps.