Pharmacokinetics of mirodenafil and its two metabolites, SK3541 and SK3544, after intravenous and oral administration of mirodenafil to streptozotocin-induced diabetes mellitus rats

Y. S. Lee; Y. H. Choi; T. K. Kim; K. H. Ryu; B. Y. Lee; M. G. Lee

doi:10.3109/00498250903380975

Pharmacokinetics of mirodenafil and its two metabolites, SK3541 and SK3544, after intravenous and oral administration of mirodenafil to streptozotocin-induced diabetes mellitus rats

Y. S. Lee, Y. H. Choi, T. K. Kim, K. H. Ryu, B. Y. Lee, M. G. Lee

Department of Pharmacy

Research output: Contribution to journal › Article › peer-review

4 Scopus citations

Abstract

The area under the curve (AUC) of mirodenafil after intravenous administration in diabetes mellitus induced by streptozotocin (DMIS) rats was significantly smaller (by 28.0%) than the control value, and the AUC _SK3541/AUC_mirodenafil ratio was significantly greater (by 130%) in DMIS rats. This may be explained by the significantly faster hepatic CL_int of mirodenafil, owing to increased hepatic CYP1A, CYP2B1/2, CYP2D, and CYP3A expression, and a faster hepatic blood flow rate, compared with control values. The AUC of mirodenafil after oral administration was comparable between DMIS and control rats, possibly because of the comparable intestinal CL_int, which may be attributable to increased CYP1A2 expression and decreased CYP2D expression in the intestines of DMIS rats.

Original language	English
Pages (from-to)	129-137
Number of pages	9
Journal	Xenobiotica
Volume	40
Issue number	2
DOIs	https://doi.org/10.3109/00498250903380975
State	Published - Feb 2010

Keywords

And SK3544
Diabetes mellitus induced by streptozotocin
Hepatic and intestinal CYP isozymes
Mirodenafil
Pharmacokinetics
Rats
SK3541

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

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10.3109/00498250903380975

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title = "Pharmacokinetics of mirodenafil and its two metabolites, SK3541 and SK3544, after intravenous and oral administration of mirodenafil to streptozotocin-induced diabetes mellitus rats",

abstract = "The area under the curve (AUC) of mirodenafil after intravenous administration in diabetes mellitus induced by streptozotocin (DMIS) rats was significantly smaller (by 28.0\%) than the control value, and the AUC SK3541/AUCmirodenafil ratio was significantly greater (by 130\%) in DMIS rats. This may be explained by the significantly faster hepatic CLint of mirodenafil, owing to increased hepatic CYP1A, CYP2B1/2, CYP2D, and CYP3A expression, and a faster hepatic blood flow rate, compared with control values. The AUC of mirodenafil after oral administration was comparable between DMIS and control rats, possibly because of the comparable intestinal CLint, which may be attributable to increased CYP1A2 expression and decreased CYP2D expression in the intestines of DMIS rats.",

keywords = "And SK3544, Diabetes mellitus induced by streptozotocin, Hepatic and intestinal CYP isozymes, Mirodenafil, Pharmacokinetics, Rats, SK3541",

author = "Lee, \{Y. S.\} and Choi, \{Y. H.\} and Kim, \{T. K.\} and Ryu, \{K. H.\} and Lee, \{B. Y.\} and Lee, \{M. G.\}",

year = "2010",

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doi = "10.3109/00498250903380975",

language = "English",

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pages = "129--137",

journal = "Xenobiotica",

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T1 - Pharmacokinetics of mirodenafil and its two metabolites, SK3541 and SK3544, after intravenous and oral administration of mirodenafil to streptozotocin-induced diabetes mellitus rats

AU - Lee, Y. S.

AU - Choi, Y. H.

AU - Kim, T. K.

AU - Ryu, K. H.

AU - Lee, B. Y.

AU - Lee, M. G.

PY - 2010/2

Y1 - 2010/2

N2 - The area under the curve (AUC) of mirodenafil after intravenous administration in diabetes mellitus induced by streptozotocin (DMIS) rats was significantly smaller (by 28.0%) than the control value, and the AUC SK3541/AUCmirodenafil ratio was significantly greater (by 130%) in DMIS rats. This may be explained by the significantly faster hepatic CLint of mirodenafil, owing to increased hepatic CYP1A, CYP2B1/2, CYP2D, and CYP3A expression, and a faster hepatic blood flow rate, compared with control values. The AUC of mirodenafil after oral administration was comparable between DMIS and control rats, possibly because of the comparable intestinal CLint, which may be attributable to increased CYP1A2 expression and decreased CYP2D expression in the intestines of DMIS rats.

AB - The area under the curve (AUC) of mirodenafil after intravenous administration in diabetes mellitus induced by streptozotocin (DMIS) rats was significantly smaller (by 28.0%) than the control value, and the AUC SK3541/AUCmirodenafil ratio was significantly greater (by 130%) in DMIS rats. This may be explained by the significantly faster hepatic CLint of mirodenafil, owing to increased hepatic CYP1A, CYP2B1/2, CYP2D, and CYP3A expression, and a faster hepatic blood flow rate, compared with control values. The AUC of mirodenafil after oral administration was comparable between DMIS and control rats, possibly because of the comparable intestinal CLint, which may be attributable to increased CYP1A2 expression and decreased CYP2D expression in the intestines of DMIS rats.

KW - And SK3544

KW - Diabetes mellitus induced by streptozotocin

KW - Hepatic and intestinal CYP isozymes

KW - Mirodenafil

KW - Pharmacokinetics

KW - Rats

KW - SK3541

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U2 - 10.3109/00498250903380975

DO - 10.3109/00498250903380975

M3 - Article

C2 - 19929308

AN - SCOPUS:75649115758

SN - 0049-8254

VL - 40

SP - 129

EP - 137

JO - Xenobiotica

JF - Xenobiotica

IS - 2

ER -

Pharmacokinetics of mirodenafil and its two metabolites, SK3541 and SK3544, after intravenous and oral administration of mirodenafil to streptozotocin-induced diabetes mellitus rats

Abstract

Keywords

UN SDGs

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