title: Determination of mirodenafil and sildenafil in the plasma and corpus cavernous of SD male rats.
abstract: The purpose of the present study was to determine sildenafil and a novel PDE-5 inhibitor, mirodenafil in the plasma and corpus cavernosum tissue of rats to compare their pharmacokinetic properties. The concentrations of mirodenafil and sildenafil in the rat plasma and corpus cavernosum tissue samples were analyzed using LC-MS/MS after a single oral administration at a dose of 40mg/kg to rats. Although the T(max), Tlambda(1/2) and MRT were not different between mirodenafil and sildenafil, the C(max) and AUC of mirodenafil were significantly higher than those of sildenafil in the plasma and corpus cavernosum tissue. Consequently mirodenafil remained longer than sildenafil in the plasma and tissue. This may provide pharmacokinetic evidence for assessment of the in vivo efficacy of mirodenafil and sildenafil.
authors.affiliation: Doping Control Center, Korea Institute of Science and Technology, Seoul 130-650, Republic of Korea.
authors.forename: Sang Kyu
authors.initials: SK
authors.lastname: Lee
authors.forename: Yoon
authors.initials: Y
authors.lastname: Kim
authors.forename: Tae Kon
authors.initials: TK
authors.lastname: Kim
authors.forename: Guang-Jin
authors.initials: GJ
authors.lastname: Im
authors.forename: Bong-Yong
authors.initials: BY
authors.lastname: Lee
authors.forename: Dong-Hyun
authors.initials: DH
authors.lastname: Kim
authors.forename: Changbae
authors.initials: C
authors.lastname: Jin
authors.forename: Hye Hyun
authors.initials: HH
authors.lastname: Yoo
mesh_terms: D000284:Administration, Oral; D000818:Animals; D019540:Area Under Curve; D002853:Chromatography, Liquid / Q000379:methods; D054706:Cyclic Nucleotide Phosphodiesterases, Type 5 / Q000097:blood* / Q000493:pharmacokinetics / Q000494:pharmacology; D005215:Fasting; D006207:Half-Life; D006863:Hydrogen-Ion Concentration; D008297:Male; D013058:Mass Spectrometry / Q000379:methods; D008657:Metabolic Clearance Rate; D015394:Molecular Structure; D008970:Molecular Weight; D010413:Penis / Q000098:blood supply* / Q000187:drug effects; D010726:Phosphodiesterase Inhibitors / Q000097:blood* / Q000493:pharmacokinetics / Q000494:pharmacology; D010879:Piperazines / Q000008:administration & dosage / Q000097:blood* / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D011092:Polyethylene Glycols / Q000737:chemistry; D011687:Purines / Q000008:administration & dosage / Q000097:blood / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D011744:Pyrimidinones / Q000008:administration & dosage / Q000097:blood* / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D011786:Quality Control; D011897:Random Allocation; D051381:Rats; D017207:Rats, Sprague-Dawley; D012015:Reference Standards; D015203:Reproducibility of Results; D000068677:Sildenafil Citrate; D012996:Solutions / Q000737:chemistry; D013047:Specific Pathogen-Free Organisms; D013449:Sulfonamides / Q000008:administration & dosage / Q000097:blood* / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D013450:Sulfones / Q000008:administration & dosage / Q000097:blood* / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology
chemical_list: D010726:Phosphodiesterase Inhibitors; D010879:Piperazines; D011687:Purines; D011744:Pyrimidinones; D012996:Solutions; D013449:Sulfonamides; D013450:Sulfones; D011092:Polyethylene Glycols; C528396:mirodenafil; D000068677:Sildenafil Citrate; D054706:Cyclic Nucleotide Phosphodiesterases, Type 5