Providing a controlled-release formulation containing dorotaberine or its salts, or an active substance with a similar tendency to degrade through oxidation /
hydrolysis. [Solution] The present invention provides a controlled-release formulation containing dorotaberine or a salt thereof, or an active substance with a similar tendency to degrade through oxidation /
hydrolysis. The present invention provides a once- or twice-daily controlled-release formulation of dorotaberine or a salt thereof that avoids fluctuations in
plasma levels, reduces
pill burden and side effects through a simplified dosing schedule, and consequently improves
patient compliance. The present invention also provides a method for preparing a controlled-release formulation of dorotaberine or a salt thereof. The present invention further provides a controlled-release formulation of dorotaberine or a salt thereof for the treatment of at least one symptom of gastrointestinal, biliary, urinary, and gynecological disorders characterized by a spastic state of
smooth muscle in a subject.