Terpenolol is a newly developed hydrophilic derivative of cannabidiol (CBD) designed to overcome the solubility, stability, and pharmacokinetic limitations of conventional lipophilic CBD formulations. This study presents its physicochemical profile, 30-day stability, and preliminary pharmacokinetic behaviour in humans. Terpenolol forms a stable aqueous nanomicellar dispersion with neutral pH (7.0 ± 0.1), consistent viscosity, and minimal variation in tintometric and colloidal parameters over the observation period. In a single-dose, two-period crossover study involving five healthy volunteers, sublingual administration of Terpenolol resulted in markedly higher plasma CBD concentrations at 30 minutes compared with an oil-based reference formulation. Observational data from more than 200 individuals using Terpenolol-based preparations across oral, nasal, cutaneous, and transdermal routes indicate good tolerability and reported improvements in anxiety, panic symptoms, insomnia, psychotic- spectrum disturbances, and musculoskeletal or joint pain. The compound’s complete solubility in aqueous media, combined with its neutral taste and odourless profile, also supports its incorporation into functional beverages, as demonstrated by a prototype mineral water formulation containing 50 mg of CBD in 500 ml. Overall, Terpenolol demonstrates physicochemical stability, improved early systemic exposure to CBD, and broad compatibility with formulations. Controlled studies are planned to further define its pharmacological relevance and potential application domains.