Pharmacokinetics of Three Organic Nitrates in Chinese Healthy Male Volunteers

Summary Eighteen Chinese male subjects completed a single-blind, randomized, three-treatment, three-period, cross-over study. In each treatment phase, subjects received a single dose of 20 mg isosor-bide dinitrate (CAS 87-33-2, ISDN) intravenous infusion, 20 mg isosorbide 5-mononitrate (CAS 16051-77...

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Published in:	Arzneimittel-Forschung Vol. 54; no. 4; pp. 203 - 206
Main Authors:	Chen, Jun, Jiang, Xin Guo, Cai, Lei, Lu, Wei, Gao, Ke Pan, Shi, Zheng Qi, Zhang, Qi Zhiang
Format:	Journal Article
Language:	English
Published:	Aulendorf (Germany) Editio Cantor Verlag 01-01-2004 Cantor
Subjects:	Administration, Oral Adult Area Under Curve Biological and medical sciences Biological Availability Cardiac Drugs Cardiac Stimulants Chromatography, Gas Coronary Drugs Cross-Over Studies Electrocardiography - drug effects Humans Infusions, Intravenous Isosorbide Dinitrate - analogs & derivatives Isosorbide Dinitrate - pharmacokinetics Male Medical sciences Nitrates - pharmacokinetics Pharmacology. Drug treatments Vasodilator Agents - pharmacokinetics Asia China CAS 16051-77-7 Isosorbide 5-mononitrate, clinical studies, pharmacokinetics, relative bioavailability Isosorbide dinitrate, clinical studies, pharmacokinetics, relative bioavailability CAS 87-33-2 Antianginal agent Human Isosorbide dinitrate CAS 37-33-2 Coronary vasodilator agent Isosorbide mononitrate Bioavailability Antiarrhythmic agent Organic nitrate Pharmacokinetics
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Summary:	Summary Eighteen Chinese male subjects completed a single-blind, randomized, three-treatment, three-period, cross-over study. In each treatment phase, subjects received a single dose of 20 mg isosor-bide dinitrate (CAS 87-33-2, ISDN) intravenous infusion, 20 mg isosorbide 5-mononitrate (CAS 16051-77-7, 5-ISMN) tablet or 20 mg isosorbide 5-mononitrate intravenous infusion. Each consecutive dosing was separated by a washout period of 7 days. Following each dosing, venous blood samples were collected over a period of 16 h. Plasma concentrations of ISDN and its two active metabolites isosorbide 2-mononitrate (2-ISMN), 5-ISMN had been measured by a validated gas chromatographic method. Various pharmacokinetic parameters including AUC 0 . ti AUC 0–∞ , C max , tmax, t 1/2 , K elm and MRT were determined for the three formulations and found to be in good agreement with literature values. AUC 0 . t and AUC 0–∞ „ of 5-ISMN tablet and intravenous infusion were 2694 ± 496 ng · ml −1 h vs. 2548 ± 556 ng · ml −1 · h and 3266 ± 624 ng · ml −1 · h vs. 3178 ± 769 ng · ml −1 h, respectively, and the relative bioavailability of 5-ISMN tablet was 105 ± 20 %. As compared with 5-ISMN intravenous infusion, ISDN can rapidly reach the plateau concentration and metabolize to its active metabolites 5-ISMN and 2-ISMN, which both have vasodilator effect. The results of this study suggest that as evaluated from the pharmacokinetic profiles of the three formulations, 5-ISMN tablet and ISDN intravenous infusion are ideal vasodilators and anti-angina drugs especially in acute conditions due to their rapid onset and long duration of action.
Bibliography:	ObjectType-Article-2 SourceType-Scholarly Journals-1 ObjectType-Feature-1 ObjectType-News-3 content type line 23
ISSN:	0004-4172 1616-7066
DOI:	10.1055/s-0031-1296960