Pharmacokinetic interaction between DA‐8159, a new erectogenic, and metformin in rats: competitive inhibition of metabolism via hepatic CYP3A1/2

作者: Y H Choi , S J Chung , M G Lee

DOI: 10.1038/SJ.BJP.0707680

关键词:

摘要: Background and purpose: Erectile dysfunction is highly prevalent in diabetic patients PDE V inhibitors are effective safe for the treatment of erectile men with diabetes. Therefore, this study we investigated whether a pharmacokinetic interaction occurs between DA-8159 metformin, as both drugs metabolized via hepatic CYP3A1/2 rats. Experimental approach: DA-8159 (30 mg kg–1) metformin (100 mg kg–1), separately together, were administered to rats either intravenously or orally. The Vmax, Km, CLint, apparent inhibition constants (Ki), [I]/Ki concentrations each drug liver intestine then measured. Key results: After i.v. administration simultaneously, AUC was significantly greater (21.2 33.9% increase respectively) than that alone. After p.o. drugs, also (20.7% increase) presence its absence. However, similar absence metformin. Conclusions implications: The after probably due competitive metabolism these CYP3A1/2. AUCs administration, indicates dose used insufficient inhibit intestinal DA-8159. British Journal Pharmacology (2008) 153, 1568–1578; doi:10.1038/sj.bjp.0707680; published online 21 January 2008

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