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Open AccessArticle

Enhanced Bioavailability of Tadalafil after Intranasal Administration in Beagle Dogs

1
Dong-A ST Co. Ltd., Giheung-gu, Yongin, Gyeonggi 446-905, Korea
2
College of Pharmacy, Pusan National University, Busan 46241, Korea
3
College of Pharmacy, Kyungsung University, 309 Suyeong-ro, Nam-gu, Busan 48434, Korea
*
Authors to whom correspondence should be addressed.
Pharmaceutics 2018, 10(4), 187; https://doi.org/10.3390/pharmaceutics10040187
Received: 14 September 2018 / Revised: 12 October 2018 / Accepted: 13 October 2018 / Published: 15 October 2018
(This article belongs to the Special Issue New Approaches to Enhance Drug Solubility and Bioavailability)
Tadalafil is an oral selective phosphodiesterase type-5 inhibitor with demonstrated efficacy and safety that is used to treat erectile dysfunction. The purpose of this study is to compare the pharmacokinetic properties of tadalafil after conventional oral tablet administration and novel intranasal administration in beagle dogs. Fourteen 13-month-old male beagle dogs were randomly divided into two groups, and were given 5 mg tadalafil orally or intranasally in a parallel design. Blood samples were collected before and 0.5, 1, 1.5, 2, 4, 6, 8, 12, 24, and 36 h after administration. The plasma concentration of tadalafil was determined via liquid chromatography-tandem mass spectrometry (LC-MS/MS). The systemic exposure and absorption rate of tadalafil were significantly greater in the intranasal administration group than in the oral administration group. A one-compartment model with first-order absorption and elimination was sufficient to explain the pharmacokinetic characteristics observed after both oral and intranasal administration. This study indicates that the development of tadalafil nasal delivery systems is feasible and may lead to better results than the conventional oral route. View Full-Text
Keywords: tadalafil; pharmacokinetics; intranasal; modeling; dog tadalafil; pharmacokinetics; intranasal; modeling; dog
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MDPI and ACS Style

Kim, J.-S.; Kim, M.-S.; Baek, I.-H. Enhanced Bioavailability of Tadalafil after Intranasal Administration in Beagle Dogs. Pharmaceutics 2018, 10, 187.

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