Determination of mirodenafil and sildenafil in the plasma and corpus cavernous of SD male rats.
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.
Lee
Sang Kyu
SK
Doping Control Center, Korea Institute of Science and Technology, Seoul 130-650, Republic of Korea.
Kim
Yoon
Y
Kim
Tae Kon
TK
Im
Guang-Jin
GJ
Lee
Bong-Yong
BY
Kim
Dong-Hyun
DH
Jin
Changbae
C
Yoo
Hye Hyun
HH
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
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