LEMBOREXANT DRUG SUBSTANCE AND MEDICINAL COMPOSITION CONTAINING SAME Russian patent published in 2025 - IPC A61K31/506 A61K9/20 

FIELD: medicine; pharmaceutics.

SUBSTANCE: group of inventions relates to the field of pharmaceutics, specifically to an active pharmaceutical ingredient of lemborexant, a pharmaceutical composition of lemborexant and a method for preparing a pharmaceutical composition of lemborexant containing lemborexant, lactose hydrate, low-substituted hydroxypropyl cellulose, hydroxypropyl cellulose, water and magnesium stearate. Active pharmaceutical ingredient lemborexant which is a granular material having 90% cumulative diameter (D90) 20 mcm or more and 64 mcm or less. Pharmaceutical composition of lemborexant containing: 2.5 mg of lemborexant and 96.38 mg of lactose hydrate, or 5 mg of lemborexant and 93.88 mg of lactose hydrate, or 10 mg of lemborexant and 88.88 mg of lactose hydrate and 16.8 mg of low-substituted hydroxypropyl cellulose, 3.6 mg of hydroxypropyl cellulose, water and 0.72 mg of magnesium stearate, wherein lemborexant is said granulated material. Method of producing a pharmaceutical composition of lemborexant containing lemborexant, lactose hydrate, low-substituted hydroxypropyl cellulose, hydroxypropyl cellulose, water and magnesium stearate, containing: a) a step of mixing said active pharmaceutical ingredient of lemborexant, lactose hydrate, low-substituted hydroxypropyl cellulose, hydroxypropyl cellulose and water to produce granules; b) a step of mixing the granules obtained in step a), low-substituted hydroxypropyl cellulose and magnesium stearate to obtain a mixture; and c) a step of compressing the mixture obtained in step b) to obtain tablets.

EFFECT: said group of inventions makes it possible to produce a pharmaceutical composition of lemborexant, characterized by a favorable dissolution profile.

9 cl, 8 dwg, 23 tbl, 5 ex