The invention discloses a
theophylline alkaloid salt, a pharmaceutical composition thereof, a preparation method of the
theophylline alkaloid salt, and an application of the
theophylline alkaloid salt, and belongs to the technical field of pharmaceutical
chemistry. Natural alkaloids with definite pharmacological activity, such as stachydrine,
betaine,
trigonelline,
sophocarpidine,
choline or
berberine, are selected as
saline-forming bases, and a series of novel theophylline alkaloid salts are developed. The functional
salt formation strategy not only fundamentally changes the traditional theophylline
salt formation mode, but also realizes a leap-through breakthrough from single improvement of
solubility to synergistic interaction and active attenuation. Through inherent
gastric mucosa protection, heart function regulation and other effects of alkaloid, an active attenuation mechanism is constructed, the core toxic and side effects of
gastrointestinal irritation, heart excitability and the like caused by theophylline are effectively reduced, the risk of introduction of exogenous sensitizers is avoided, and the
bioavailability of theophylline is improved. The clinical problems of narrow
therapeutic window and large toxic and side effects of traditional theophylline and salt drugs thereof are effectively solved.