PHARMACEUTICAL COMPOSITIONS BASED ON GUANFACIN, SUITABLE FOR DAILY ADMINISTRATION AS A UNIT DOSED FORM

摘要

1. A pharmaceutical composition containing an effective amount of guanfacin or a pharmaceutically acceptable salt thereof and at least one carrier, which makes it possible to achieve effective once-daily administration of said guanfacin to a person at least 18 years old, and which makes it possible to achieve a single dose of said guanfacin on an empty stomach, at a dose of 1 mg guanfacin, PPK0-last about 29.3 ± 20% ng · h / ml, Cmax about 0.98 ± 20% ng / ml, or at a dose of 2 mg or another dose, the FC profile of which is linearly correlated with the specified profile for a dose of 1 mg, PPK0-last and Cma x, linearly related to the indicated values for a dose of 1 mg, the total weight of the composition for a dose of 1 mg being up to 170 mg, and for a dose of 2 mg or another dose, it is linearly related to a dose of 1 mg, and the total weight of the tablet linearly proportional to the specified,! or ! a person aged at least 18 years, and allowing to achieve for the specified guanfacin with a single dose on an empty stomach at a dose of 2.5 mg guanfacin, PPK0-last about 81.3 ± 20% ng · h / ml, Cmax about 2.49 ± 20% ng / ml, or another dose, the PK profile of which linearly correlates with the specified profile for a dose of 2.5 mg, PPK0-last and Cmax, linearly related to the indicated values for a dose of 2.5 mg, and the total weight of the composition for doses of 2.5 mg is up to 255 mg, and for another dose it is linearly interconnected with a dose of 2.5 mg, and the total weight of the tablet is linearly proportional to the indicated,! or ! a person aged at least 18 years, and allowing to achieve for the specified guanfacin with a single dose on an empty stomach, at a dose of 4 mg guanfacin, PPK-last about 120 ± 20% ng · h / ml, Cmax about 3.58 ± 20% ng / ml, or, for doses of 3 mg, 3.5 mg, or another dose, the PK profile of which linearly correlates with the indicated