Elimination pharmacokinetics of sphaeralcic acid, tomentin and scopoletin mixture from a standardized fraction of Sphaeralcea angustifolia (Cav.) G. Don orally administered.

Sphaeralcea angustifolia (Cav.) G. Don (Malvaceae) is a plant used in inflammatory illnesses. The scopoletin was the main responsible compound for the anti-arthritic effect in this species. The therapeutic effectiveness of a S. angustifolia dichloromethane extract gel standardized in scopoletin was confirmed in patients with osteoarthritis. Cells in suspension cultures from S. angustifolia were established for scopoletin production; in addition, tomentin, and sphaeralcic acid compounds were isolated from this culture. Tomentin and sphaeralcic acid showed also anti-inflammatory and immunomodulatory effects. Validation of HPLC quantification methods for sphaeralcic acid, and scopoletin and tomentin was performed in addition to extraction efficiency and stability of the active compounds. The pharmacokinetic parameters of scopoletin and tomentine in mixture, and sphaeralcic acid after oral administration of standardized active fraction indicated that these compounds followed a two-compartment model; they were bioavailable in plasma (absorbed) and distributed to blank organs. No products derived from their biotransformation were detected. The objective of this work was to determine the pharmacokinetic constants of urinary and fecal elimination in mice of the anti-arthritic compounds, after oral administration (400 mg / kg) of a standardized active fraction (SaTES) of S. angustifolia. It was established that the coumarin mixture (scopoletin and tomentin) were eliminated by the urine; while, sphaeralcic acid was mainly eliminated by fecal path, following both a non-compartmental behavior. No products derived from their biotransformation were detected.