SUSTAINED-RELEASE PHARMACEUTICAL COMPOSITION CONTAINING RIVASTIGMINE Russian patent published in 2020 - IPC A61K9/00 A61K9/16 A61K47/34 A61K47/38 A61K31/27 

FIELD: medicine; pharmaceuticals.

SUBSTANCE: present invention relates to a sustained-release pharmaceutical composition containing rivastigmine. Disclosed delayed-release pharmaceutical composition for the once-a-day regimen comprises: pH-dependent composition with delayed release and matrix form of pH-independent composition with delayed release. PH-dependent composition with delayed release is in form of granules or pellets and contains 25–90 wt % of rivastigmine in total rivastigmine content, and the pH-independent composition with delayed release contains inside the matrix form a pH-dependent composition with delayed release and 10–75 wt % of rivastigmine in the total rivastigmine content. pH-dependent composition with delayed release contains a polymer having the property of dissolving at pH 5.0 or higher, wherein said polymer is at least one polymer selected from a group consisting of an acrylic acid-based copolymer, hydroxypropyl methyl cellulose phthalate and cellulose acetate phthalate, or a mixture thereof. Pharmaceutical composition is presented in tableted form.

EFFECT: composition is a sustained release preparation containing a pH-dependent phase with delayed release, where, by controlling that the release of the pharmaceutical composition in the stomach at the initial administration stage is minimized, pharmaceutical composition can reduce the maximum blood concentration (C_max) compared to existing products when achieving the effective blood concentration, thereby reducing side effects and further maintaining the effective blood concentration by delayed release of the main ingredients; as a result of which the disclosed pharmaceutical composition in dosage only once a day shows the same effect as the existing dosage twice a day, and can improve clinical effectiveness of patients due to improvement in ease of use.

5 cl, 3 tbl, 6 ex