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Investigations showed that the synergistic polymer pair guar gum and carboxymethylcellulose (CMC) (1:1) was the most rational matrix platform for ensuring the gastroretentive action of tablets with aspen bark dry extract. A composition and technology for gastroretentive tablets Ekorsin GR based on it using compression molding with preliminary dry granulation of the tableting mixture were developed. In vitro tests established that these tablets (due to an increase and retention of its diameter >15 mm in a solution corresponding to stomach pH) could remain in the stomach for a long time and exhibit targeted gastro-protective action for 22 h with controlled release of the active ingredients. Quality parameters and standards for the experimental dosage form Ekorsin GR were proposed. Antiulcer studies using an indomethacin-induced ulcer model indicated that Ekorsin GR gastroretentive tablets were more efficacious than previously developed tableted and encapsulated dosage forms of aspen bark dry extract.