FIELD: medicine; pharmaceutics.
SUBSTANCE: group of inventions relates to pharmaceutical industry, namely to a formulation for oral delivery of a kappa-opioid receptor agonist, a method for preparing said formulation and a dosage form containing said formulation. Formulation for oral delivery of a kappa-opioid receptor agonist, wherein the formulation contains a particle comprising a kappa-opioid receptor agonist and an oligosaccharide, where the kappa opioid receptor agonist is selected from the group consisting of CR845, characterized by formula 
D-Phe-D-Phe-D-Leu-D-Lys-[ω(4-aminopiperidine-4-carboxylic acid)]-OH, or its HCl salt or HCl salt hydrate, where the oligosaccharide is trehalose. A dosage form containing CR845 or its HCl salt or a hydrate of HCl salt and trehalose, where the dosage form is selected from a group consisting of a tablet, a capsular tablet, a capsule, a powder, a suspension, a liquid suspension and a gel. Method for preparing a formulation for oral delivery of a kappa-opioid receptor agonist, comprising spray drying a mixture containing CR845 or its HCl salt or HCl salt hydrate and trehalose, to form particles of CR845 or an HCl salt thereof or a hydrate of an HCl salt embedded in trehalose; or application as a coating of a mixture containing CR845 or its HCl salt or hydrate of HCl salt and trehalose, into one or more granules or microgranules to form one or more granules or microgranules coated with CR845 or its HCl salt or HCl salt hydrate embedded in trehalose.
EFFECT: use of said group of inventions enables to obtain a composition which is stable for a year under various temperature conditions and has enhanced absorption.
13 cl, 6 dwg, 6 tbl, 7 ex
