DOSAGE FORM WITH IMPROVED CHARACTERISTICS OF pH-DEPENDENT RELEASE OF PREPARATION CONTAINING ESOMEPRAZOLE OR PHARMACEUTICALLY ACCEPTABLE SALT THEREOF Russian patent published in 2020 - IPC A61K31/4439 A61K47/34 A61K9/22 A61K9/30 A61K9/52 A61P1/04 

FIELD: medicine; pharmaceuticals.

SUBSTANCE: presented is a dosage form containing esomeprazole or its pharmaceutically acceptable salt for treating gastric and reflux oesophageal diseases. Dosage form comprises a nucleus containing esomeprazole, a layer of endothelial coating formed on the nucleus, and a coating release coating layer formed on the endothelial coating layer. Layer of endothelial coating contains at least one substance selected from hydroxypropyl methyl cellulose, polyvinylpyrrolidone, low-substituted hydroxypropyl cellulose, starch and gelatin. Layer of release-controlling coating contains a polymer in which copolymer S of methacrylic acid and copolymer L of methacrylic acid are mixed in weight ratio of 1.5:1 to 3.5:1 as base material of release-controlling coating, where methacrylic acid copolymer S is an anionic copolymer containing methacrylic acid and methyl methacrylate in ratio of 1:2, and methacrylic acid copolymer L is an anionic copolymer containing methacrylic acid and methyl methacrylate in ratio of 1:1. Weight of copolymer S of methacrylic acid and copolymer L of methacrylic acid as base materials of release-controlling coating ranges from 15 to 40 % relative to weight of the tablet with endothelial coating. Dosage form when eliciting release after 2 hours elutes 5 % or less of esomeprazole or its pharmaceutically acceptable salt, and after 6 hours eluates at least 90 % of esomeprazole or its pharmaceutically acceptable salt. Described also is a method for preparing a dosage form of esomeprazole.

EFFECT: dosage form according to the invention is characterized by improved characteristics of pH-dependent release of the preparation, starts releasing esomeprazole or its pharmaceutically acceptable salt after a given delay time for oral administration, continues release for a given time and ends the release through a predetermined time, thereby providing excellent patient comfort and excellent therapeutic effects compared to other standard forms.

8 cl, 2 dwg, 10 tbl, 4 ex