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Comparative single-dose pharmacokinetics of sildenafil after oral and rectal administration in healthy beagle dogs

Yang, Hyuck-Joo, Oh, Ye-In, Jeong, Jong-Woo, Song, Kun-Ho, Koo, Tae-Sung, Seo, Kyoung-Won
BMC veterinary research 2018 v.14 no.1 pp. 291
Beagle, blood sampling, citrates, dogs, drug therapy, enzymes, hypertension, liquid chromatography, oral administration, patients, pharmacokinetics, tandem mass spectrometry, veterinary medicine
BACKGROUND: Sildenafil citrate, a highly selective phosphodiesterase type 5 inhibitor, is used to treat pulmonary hypertension (PH) in veterinary medicine. The objective of this study was to investigate pharmacokinetic profiles by oral administration of orally disintegrating film (ODF) and film coated tablet (FCT) formulations and rectal administration of ODF formulation in healthy dogs. Twelve healthy beagle dogs were administered four separate doses of sildenafil: FCT formulation 2 mg/kg orally, ODF formulation 2 mg/kg orally, ODF formulation 2 mg/kg rectally, and ODF formulation 10 mg/kg rectally. For 24 hours following administration, blood samples were collected and the plasma concentrations of sildenafil were assayed by liquid chromatography-tandem mass spectrometry. RESULTS: There were no significant differences in all the pharmacokinetic parameters between FCT and ODF formulations when administrated orally. Cₘₐₓ at the time of rectal administration was lower when the same dose was given as that orally administered. No serious systemic adverse events (AEs) were observed. CONCLUSIONS: These findings suggest that sildenafil ODF formulation can be used as an alternative to FCT formulation in the treatment of canine PH patients; additionally, rectal administration of sildenafil ODF may be a beneficial treatment option for canine patients who are unable to receive medication orally.