Pharmacokinetics and urinary excretion of DW116, a new fluoroquinolone antibacterial agent, in humans as a phase I study
Pharmacokinetics and urinary excretion of the new fluoroquinolone antibacterial agent DW116 [1-(5-fluoro-2-pyridyl)-6-fluoro-7-(4-methyl-1-piperazynyl)-1, 4-dihydro-4-oxoquinolone-3-carboxylic acid, hydrochloride] following oral administration (200, 400, 600 mg) were studied in humans as a phase I study. The plasma concentration of DW116 declined monoexponentially with a half-life range of 16-22 hr. The area under the curve (AUC) and Cmax increased proportionally as the dose increased. The T1/2 and mean residence time (MRT) (28.3-30.9 hr) were independent of dose. The Tmax appeared within 3 hr (0.9-2.7 hr) after drug administration. The Ka ranged from 1.3 to 4.1 (hr-1). The plasma half-life was much longer, and Cmax was higher by about two- to three-fold than conventional fluoroquinolones. Urinary recovery of DW116 was 29.6-61.6% of the dose. The maximum excretion rate appeared within 4 hr and decreased continuously after drug administration. A urinary metabolite was not detected in the urine extract obtained before and after hydrolysis by beta-glucuronidase (from Escherichia coli); this was different from other fluoroquinolone antibacterial agents. Poor metabolism in the kidney may contribute to the good oral bioavailability, but due to the low recovery (< 60%) in urine, it is possible that DW116 is metabolized in the liver or other organs.
| Medienart: |
Artikel |
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| Erscheinungsjahr: |
2000 |
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| Erschienen: |
2000 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:26 |
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| Enthalten in: |
Drug development and industrial pharmacy - 26(2000), 1 vom: 16. Jan., Seite 103-6 |
| Sprache: |
Englisch |
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| Beteiligte Personen: |
Jung, B H [VerfasserIn] |
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| Themen: |
Anti-Infective Agents |
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| Anmerkungen: |
Date Completed 28.03.2000 Date Revised 21.09.2019 published: Print Citation Status MEDLINE |
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| Förderinstitution / Projekttitel: |
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| PPN (Katalog-ID): |
NLM106058916 |
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| 100 | 1 | |a Jung, B H |e verfasserin |4 aut | |
| 245 | 1 | 0 | |a Pharmacokinetics and urinary excretion of DW116, a new fluoroquinolone antibacterial agent, in humans as a phase I study |
| 264 | 1 | |c 2000 | |
| 336 | |a Text |b txt |2 rdacontent | ||
| 337 | |a ohne Hilfsmittel zu benutzen |b n |2 rdamedia | ||
| 338 | |a Band |b nc |2 rdacarrier | ||
| 500 | |a Date Completed 28.03.2000 | ||
| 500 | |a Date Revised 21.09.2019 | ||
| 500 | |a published: Print | ||
| 500 | |a Citation Status MEDLINE | ||
| 520 | |a Pharmacokinetics and urinary excretion of the new fluoroquinolone antibacterial agent DW116 [1-(5-fluoro-2-pyridyl)-6-fluoro-7-(4-methyl-1-piperazynyl)-1, 4-dihydro-4-oxoquinolone-3-carboxylic acid, hydrochloride] following oral administration (200, 400, 600 mg) were studied in humans as a phase I study. The plasma concentration of DW116 declined monoexponentially with a half-life range of 16-22 hr. The area under the curve (AUC) and Cmax increased proportionally as the dose increased. The T1/2 and mean residence time (MRT) (28.3-30.9 hr) were independent of dose. The Tmax appeared within 3 hr (0.9-2.7 hr) after drug administration. The Ka ranged from 1.3 to 4.1 (hr-1). The plasma half-life was much longer, and Cmax was higher by about two- to three-fold than conventional fluoroquinolones. Urinary recovery of DW116 was 29.6-61.6% of the dose. The maximum excretion rate appeared within 4 hr and decreased continuously after drug administration. A urinary metabolite was not detected in the urine extract obtained before and after hydrolysis by beta-glucuronidase (from Escherichia coli); this was different from other fluoroquinolone antibacterial agents. Poor metabolism in the kidney may contribute to the good oral bioavailability, but due to the low recovery (< 60%) in urine, it is possible that DW116 is metabolized in the liver or other organs | ||
| 650 | 4 | |a Clinical Trial | |
| 650 | 4 | |a Clinical Trial, Phase I | |
| 650 | 4 | |a Journal Article | |
| 650 | 7 | |a Anti-Infective Agents |2 NLM | |
| 650 | 7 | |a DW-116 |2 NLM | |
| 650 | 7 | |a Fluoroquinolones |2 NLM | |
| 650 | 7 | |a Piperazines |2 NLM | |
| 650 | 7 | |a Quinolones |2 NLM | |
| 700 | 1 | |a Choi, M H |e verfasserin |4 aut | |
| 700 | 1 | |a Chung, B C |e verfasserin |4 aut | |
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