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

Cited 3 time in Web of Science Cited 2 time in Scopus
Authors
Yang, Hyuck-Joo; Oh, Ye-In; Jeong, Jong-Woo; Song, Kun-Ho; Koo, Tae-Sung; Seo, Kyoung-Won
Issue Date
2018-09-24
Publisher
BioMed Central
Citation
BMC Veterinary Research, 14(1):291
Keywords
DogOrally disintegrating film formulationRectal administrationSildenafilPulmonary hypertension
Abstract
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.
ISSN
1746-6148
Language
English
URI
https://hdl.handle.net/10371/144953
DOI
https://doi.org/10.1186/s12917-018-1617-7
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College of Veterinary Medicine (수의과대학)Dept. of Veterinary Medicine (수의학과)Journal Papers (저널논문_수의학과)
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