دورية أكاديمية
Pharmacokinetics of three organic nitrates in Chinese healthy male volunteers.
| العنوان: | Pharmacokinetics of three organic nitrates in Chinese healthy male volunteers. |
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| المؤلفون: | Chen J; Department of Pharmaceutics, School of Pharmacy, Fudan University, Shanghai, The People's Republic of China., Jiang XG, Cai L, Lu W, Gao KP, Shi ZQ, Zhang QZ |
| المصدر: | Arzneimittel-Forschung [Arzneimittelforschung] 2004; Vol. 54 (4), pp. 203-6. |
| نوع المنشور: | Clinical Trial; Comparative Study; Journal Article; Randomized Controlled Trial |
| اللغة: | English |
| بيانات الدورية: | Publisher: Editio Cantor Country of Publication: Germany NLM ID: 0372660 Publication Model: Print Cited Medium: Print ISSN: 0004-4172 (Print) Linking ISSN: 00044172 NLM ISO Abbreviation: Arzneimittelforschung Subsets: MEDLINE |
| أسماء مطبوعة: | Original Publication: Aulendorf, Editio Cantor |
| مواضيع طبية MeSH: | Isosorbide Dinitrate/*analogs & derivatives , Nitrates/*pharmacokinetics, Administration, Oral ; Adult ; Area Under Curve ; Biological Availability ; Chromatography, Gas ; Cross-Over Studies ; Electrocardiography/drug effects ; Humans ; Infusions, Intravenous ; Isosorbide Dinitrate/pharmacokinetics ; Male ; Vasodilator Agents/pharmacokinetics |
| مستخلص: | 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 isosorbide 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 AUC0-t, AUC0-infinity, Cmax, tmax, t1/2, Kelm and MRT were determined for the three formulations and found to be in good agreement with literature values. AUC0-t and AUC0-infinity of 5-ISMN tablet and intravenous infusion were 2694 +/- 496 ng x ml(-1) x h vs. 2548 +/- 556 ng x ml(-1) x h and 3266 +/- 624 ng x ml(-1) x h vs. 3178 +/- 769 ng x ml(-1) x 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. |
| المشرفين على المادة: | 0 (Nitrates) 0 (Vasodilator Agents) IA7306519N (Isosorbide Dinitrate) LX1OH63030 (isosorbide-5-mononitrate) |
| تواريخ الأحداث: | Date Created: 20040519 Date Completed: 20040629 Latest Revision: 20161124 |
| رمز التحديث: | 20240829 |
| DOI: | 10.1055/s-0031-1296960 |
| PMID: | 15146932 |
| قاعدة البيانات: | MEDLINE |
| تدمد: | 0004-4172 |
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| DOI: | 10.1055/s-0031-1296960 |