FIELD: medicine; pharmaceutics.
SUBSTANCE: group of inventions relates to pharmaceutical industry, namely to an oral combination preparation for treating type 2 diabetes mellitus and a method for preparing it. Oral combined preparation for treating type 2 diabetes mellitus, which includes hemigliptin or a pharmaceutically acceptable salt thereof and dapagliflozin or a pharmaceutically acceptable salt thereof as active ingredients; microcrystalline cellulose or a mixture of lactose and microcrystalline cellulose as a diluent; baking powder; and a lubricant which includes hemigliptin or a pharmaceutically acceptable salt thereof and dapagliflozin or a pharmaceutically acceptable salt thereof in a weight ratio of 5 to 1 in terms of free forms, and contains from 20% to 60% by weight of active ingredients, from 20% to 70% by weight of a diluent, from 0.5% to 15% by weight of a baking powder and from 0.2% to 15% by weight of a lubricant, where the baking powder is croscarmellose sodium or crospovidone, and the lubricant is sodium stearyl fumarate; and dapagliflozin is amorphous dapagliflozin. Method for preparing the above oral combination preparation for treating type 2 diabetes, which includes: i) sieving hemigliptin or a pharmaceutically acceptable salt thereof and dapagliflozin or a pharmaceutically acceptable salt thereof as active ingredients, microcrystalline cellulose as a diluent or a mixture of lactose and microcrystalline cellulose, and a disintegrant; and mixing; and ii) adding a lubricant to the mixture obtained in step (i), mixing and tabletting the resulting mixture, where the oral combination preparation contains from 20 wt.% to 60 wt.% of active ingredients, from 20 wt.% to 70 wt.% of a diluent, from 0.5 wt.% to 15 wt.% of baking powder and from 0.2 wt.% to 15 wt.% of a sliding substance, the baking powder is croscarmellose sodium or crospovidone, and the lubricant is sodium stearyl fumarate. Above preparation effectively treats type 2 diabetes by increasing bioavailability and stability of the active ingredients.
EFFECT: method enables to obtain a combined preparation with high efficiency with simultaneous increase in the stability of the active ingredients.
10 cl, 2 dwg, 10 tbl, 16 ex
