FIELD: pharmacy. SUBSTANCE: invention relates to composition for controlled-release of stimulating agent - xanthine or its derivative, for example, caffeine and method of its preparing. Composition is used for courage and/or somnolence increase. Composition has microparticles of stimulating agent and biodegradable matrix from which the stimulating agent is released for the long time. Composition is used by orally route. For 2 h after the preparation ingestion 20-50 wt.-% of stimulating agent is released and remained part - for 8-10 h after intake. Binding agent is water-soluble material which is bound to the stimulating agent and distributed in its uniformly as solid particles. Agent that retards the release of the stimulating agent from composition is water-insoluble material. Composition consists of microparticles containing spherical core made of pharmaceutically acceptable organic material. Core is covered by the first and the second matrix layers. The first matrix layer has 55-95% of stimulating agent and the second one - 5-45% of its total amount. For additional inhibition of stimulating agent release from matrix an intermediate cover can be between matrix layers. In part, the core can include polysaccharide, sugar and sugar derivative. Synthetic polymer can be used as water-soluble material and shellac - as water-insoluble material. Caffeine can be used as the stimulating agent. Amount of stimulating agent in the first layer is 80-90% and in the second layer - 10-20 preferably. Invention claims the composition described above that is composed of many microparticles closed into capsule and the method of preparing compositions involving preparing solid spherical cores and applying two layers of envelopes on their surface. Compositions of layers are given above. Application of envelope layers is carried out by spraying the stimulating agent mixture, binding agent from water-soluble material and agent inhibiting release of the stimulating agent. Core have preferable initial diameter 350-1000 mcm and stimulating agent exists as powder (particles size is less 100 mcm). In the process of the composition preparing humidity value should be regulated at the level below 5%. Invention provides effect for some hours without increase of the stimulating agent level that can show undesirable effects. EFFECT: enhanced effectiveness of composition, improved method of preparing. 15 cl, 5 dwg, 10 ex
