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Devil's claw is used for the treatment of inflammatory symptoms and degenerative disorders in horses since many years, but without the substantive pharmacokinetic data. The pharmacokinetic parameters of harpagoside, the main active constituent of  Harpagophytum procumbens   DC  ex Meisn., were evaluated in equine plasma after administration of  Harpagophytum  extract  FB  8858 in an open, single‐dose, two‐treatment, two‐period, randomized cross‐over design. Six horses received a single dose of  Harpagophytum  extract, corresponding to 5 mg/kg  BM  harpagoside, and after 7 days washout period, 10 mg/kg  BM  harpagoside via nasogastric tube. Plasma samples at certain time points (before and 0–24 hr after administration) were collected, cleaned up by solid‐phase extraction, and harpagoside concentrations were determined by  LC ‐ MS / MS  using apigenin‐7‐glucoside as internal standard. Plasma concentration‐time data and relevant parameters were described by noncompartmental model through  PKS olver software. Harpagoside could be detected up to 9 hr after administration.  C  max  was found at 25.59 and 55.46 ng/ml,  t  1/2  at 2.53 and 2.32 hr, respectively, and  t  max  at 1 hr in both trials.  AUC  0–inf  was 70.46 and 117.85 ng hr ml −1 , respectively. A proportional relationship between dose,  C  max  and  AUC  was observed. Distribution ( V  z / F ) was 259.04 and 283.83 L/kg and clearance ( CL /F) 70.96 and 84.86 L hr −1  kg −1 , respectively. Treatment of horses with  Harpagophytum  extract did not cause any clinically detectable side effects.

Pharmacokinetics of harpagoside in horses after intragastric administration of a Devil's claw (Harpagophytum procumbens) extract