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DOI: 10.1055/s-0039-3399645
Devil’s claw (Harpagophytum procumbens) – Pharmacokinetics of harpagoside in horses
Publikationsverlauf
Publikationsdatum:
20. Dezember 2019 (online)
Devil’s claw is used for the treatment of chronic inflammatory symptoms and degenerative disorders [1] in horses since many years, but without the substantive equine pharmacokinetic data [2],[3],[4].
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, randomised 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 h 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 non-compartmental model through PKSolver software. Harpagoside could be detected up to 9 h after administration. Cmax was found at 25.59 and 55.46 ng/ml, t1/2 at 2.53 h and 2.32 h, respectively and tmax at one hour in both trials. AUC0-inf was 70.46 and 117.85 ng h ml-1, respectively. A proportional relationship between dose, Cmax and AUC was observed. Distribution (Vz/F) was 259.04 and 283.83 L/kg and clearance (CL/F) 70.96 and 84.86 L h-1 kg-1, respectively.
Treatment of horses with Harpagophytum extract did not cause any clinically detectable side effects. The knowledge of basic equine pharmacokinetics, based on the results of this study, will help to link results from in vitro assays and clinical studies and optimise therapeutic efficacy.
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References
- 1 ESCOP Monographs: The scientific foundation for herbal medicinal products. . 2nd ed.. Stuttgart: Thieme; Supplement. 2009: 135-146
- 2 Loew D, Möllerfeld J, Schrödter A, Puttkammer S, Kaszkin M. Investigations on the pharmacokinetic properties of Harpagophytum extracts and their effects on eicosanoid biosynthesis in vitro and ex vivo. Clin Pharmacol Ther 2001; 69: 356-364
- 3 Colas C, Garcia P, Popot M. Liquid chromatography/electrospray ionization mass spectrometric characterization of Harpagophytum in equine urine and plasma. Rapid Commun Mass Spectrom 2006; 20: 3257-3266
- 4 Colas C, Garcia P, Popot M. Optimization of solid-phase extraction for the liquid chromatography-mass spectrometry analysis of harpagoside, 8-para-coumaroyl harpagide, and harpagide in equine plasma and urine. J Chromatogr Sci 2008; 46: 174-183
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References
- 1 ESCOP Monographs: The scientific foundation for herbal medicinal products. . 2nd ed.. Stuttgart: Thieme; Supplement. 2009: 135-146
- 2 Loew D, Möllerfeld J, Schrödter A, Puttkammer S, Kaszkin M. Investigations on the pharmacokinetic properties of Harpagophytum extracts and their effects on eicosanoid biosynthesis in vitro and ex vivo. Clin Pharmacol Ther 2001; 69: 356-364
- 3 Colas C, Garcia P, Popot M. Liquid chromatography/electrospray ionization mass spectrometric characterization of Harpagophytum in equine urine and plasma. Rapid Commun Mass Spectrom 2006; 20: 3257-3266
- 4 Colas C, Garcia P, Popot M. Optimization of solid-phase extraction for the liquid chromatography-mass spectrometry analysis of harpagoside, 8-para-coumaroyl harpagide, and harpagide in equine plasma and urine. J Chromatogr Sci 2008; 46: 174-183
![](https://www.thieme-connect.de/media/plantamedica/201918/thumbnails/10.1055s-0039-3399645-f0001.jpg)
![Zoom Image](/products/assets/desktop/css/img/icon-figure-zoom.png)