MODIFIED RELEASE PHARMACEUTICAL COMPOSITION BASED ON CLOZAPINE POLYMORPHS Russian patent published in 2025 - IPC A61K31/551 A61K47/02 A61K47/10 A61K47/12 A61K47/26 A61K47/38 A61K47/58 A61K9/22 A61K9/28 A61P25/18 

FIELD: chemistry.

SUBSTANCE: group of inventions relates to medical chemistry and chemical-pharmaceutical industry, particularly to a pharmaceutical composition based on the neuroleptic clozapine and a method for preparing it. Composition for the treatment of mental disease with a modified release of clozapine, characterized by a combination of fast and prolonged release in the form of a tablet, film-coated, contains in a core tablet as an active substance clozapine in the form of a crystalline polymorph of clozapine monohydrate of a certain form and auxiliary substances: microcrystalline cellulose (MCC); lactose monohydrate; hydroxypropyl methylcellulose K15M CR (“ГПМЦ” K15M CR); binder and wetting agent selected from hydroxypropyl methylcellulose of 2910 type 606 (“ГПМЦ” 2910 type 606) and/or Povidone of K-17 brand; colloidal silicon dioxide and magnesium stearate in a certain amount. Method of producing said composition includes the following steps: separately sieving said clozapine polymorph, MCC, lactose monohydrate and colloidal silicon dioxide; obtaining a binding and wetting component, which is an aqueous solution of “ГПМЦ” 2910 type 606, K-17 grade povidone or a mixture of said solutions; said clozapine polymorph, MCC and lactose monohydrate are mixed until homogeneous, binder and wetting component are added and mixed again; obtained wet mixture is dried and granulated; granulated mass is mixed with “ГПМЦ” K15M CR, then colloidal silicon dioxide and magnesium stearate are added; the obtained mixture is tabletted by pressing and then the tablets are coated with a film coating.

EFFECT: use of the group of inventions provides fast release of clozapine when taking a tablet and fast achievement of its maximum concentration in blood plasma with prolonged release pattern and long-term maintenance of effective concentration in blood plasma.

9 cl, 1 tbl, 6 dwg, 5 ex