COMBINED PHARMACEUTICAL WITH TABLET IN CORE, CONTAINING MOSAPRIDE AND RABEPRAZOLE Russian patent published in 2021 - IPC A61K9/22 A61K9/24 A61K31/4439 A61K31/535 

FIELD: medicine.

SUBSTANCE: group of inventions relates to the field of medicine, namely to a combined "tablet-in-tablet" pharmaceutical containing mosapride and rabeprazole for oral administration in gastrointestinal diseases, consisting of: an inner core containing rabeprazole or a pharmaceutically acceptable salt thereof as an active substance, and a component of the outer layer containing mosapride or a pharmaceutically acceptable salt thereof as an active substance, wherein the entire surface of the inner core is surrounded by the component of the outer layer and the component of the outer layer has a two-layer structure of an immediate-release layer containing the active substance, a disintegrant and an excipient, and a layer sustained release containing the active ingredient, a disintegrating agent, a substance changing the release process, and an excipient, wherein a mixture of hydroxypropyl methylcellulose with a viscosity of 75,000 to 140,000 mPa∙s and hydroxypropyl methylcellulose with a viscosity of 3,000 to 5,600 mPa∙s is used as a substance changing the release process, and considering the total weight of the substance changing the release process, 60 to 70% wt. of hydroxypropyl methylcellulose with a viscosity of 75,000 to 140,000 mPa∙s and 30 to 40% wt. of hydroxypropyl methylcellulose with a viscosity of 3,000 to 5,600 mPa∙s should be included, hydroxypropyl cellulose with a low degree of substitution or crospovidone is used as a disintegrating agent, and microcrystalline cellulose, lactose hydrate or D-mannitol is used as an excipient; wherein the weight ratio of the sustained-release layer and the immediate-release layer of the component of the outer layer is from 1:1.5 to 1:2.5; the surface area of the inner core surrounded by the immediate-release layer of the component of the outer layer is larger than the surface area of the inner core surrounded by the sustained-release layer of the component of the outer layer, and also relates to a method for preparing a combined "tablet-in-tablet" pharmaceutical containing mosapride and rabeprazole for oral administration in gastrointestinal diseases.

EFFECT: group of inventions ensures the creation of a combined "tablet-in-tablet" pharmaceutical improving bioavailability and demonstrating the effect of both the active substance of the inner core and the active substance of the component of the outer layer even at a single oral administration of one tablet per day.

7 cl, 9 dwg, 11 tbl