Skip to main content
  • ASM
    • Antimicrobial Agents and Chemotherapy
    • Applied and Environmental Microbiology
    • Clinical Microbiology Reviews
    • Clinical and Vaccine Immunology
    • EcoSal Plus
    • Eukaryotic Cell
    • Infection and Immunity
    • Journal of Bacteriology
    • Journal of Clinical Microbiology
    • Journal of Microbiology & Biology Education
    • Journal of Virology
    • mBio
    • Microbiology and Molecular Biology Reviews
    • Microbiology Resource Announcements
    • Microbiology Spectrum
    • Molecular and Cellular Biology
    • mSphere
    • mSystems
  • Log in
  • My alerts
  • My Cart

Main menu

  • Home
  • Articles
    • Current Issue
    • Accepted Manuscripts
    • COVID-19 Special Collection
    • Archive
    • Minireviews
  • For Authors
    • Submit a Manuscript
    • Scope
    • Editorial Policy
    • Submission, Review, & Publication Processes
    • Organization and Format
    • Errata, Author Corrections, Retractions
    • Illustrations and Tables
    • Nomenclature
    • Abbreviations and Conventions
    • Publication Fees
    • Ethics Resources and Policies
  • About the Journal
    • About AAC
    • Editor in Chief
    • Editorial Board
    • For Reviewers
    • For the Media
    • For Librarians
    • For Advertisers
    • Alerts
    • AAC Podcast
    • RSS
    • FAQ
  • Subscribe
    • Members
    • Institutions
  • ASM
    • Antimicrobial Agents and Chemotherapy
    • Applied and Environmental Microbiology
    • Clinical Microbiology Reviews
    • Clinical and Vaccine Immunology
    • EcoSal Plus
    • Eukaryotic Cell
    • Infection and Immunity
    • Journal of Bacteriology
    • Journal of Clinical Microbiology
    • Journal of Microbiology & Biology Education
    • Journal of Virology
    • mBio
    • Microbiology and Molecular Biology Reviews
    • Microbiology Resource Announcements
    • Microbiology Spectrum
    • Molecular and Cellular Biology
    • mSphere
    • mSystems

User menu

  • Log in
  • My alerts
  • My Cart

Search

  • Advanced search
Antimicrobial Agents and Chemotherapy
publisher-logosite-logo

Advanced Search

  • Home
  • Articles
    • Current Issue
    • Accepted Manuscripts
    • COVID-19 Special Collection
    • Archive
    • Minireviews
  • For Authors
    • Submit a Manuscript
    • Scope
    • Editorial Policy
    • Submission, Review, & Publication Processes
    • Organization and Format
    • Errata, Author Corrections, Retractions
    • Illustrations and Tables
    • Nomenclature
    • Abbreviations and Conventions
    • Publication Fees
    • Ethics Resources and Policies
  • About the Journal
    • About AAC
    • Editor in Chief
    • Editorial Board
    • For Reviewers
    • For the Media
    • For Librarians
    • For Advertisers
    • Alerts
    • AAC Podcast
    • RSS
    • FAQ
  • Subscribe
    • Members
    • Institutions
Pharmacology

Influences of Urinary pH on Ciprofloxacin Pharmacokinetics in Humans and Antimicrobial Activity In Vitro versus Those of Sparfloxacin

Marika Kamberi, Kimiko Tsutsumi, Tsutomu Kotegawa, Koichi Kawano, Koichi Nakamura, Yoshihito Niki, Shigeyuki Nakano
Marika Kamberi
Department of Clinical Pharmacology and Therapeutics, Oita Medical University, Oita,
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
Kimiko Tsutsumi
Department of Clinical Pharmacology and Therapeutics, Oita Medical University, Oita,
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
Tsutomu Kotegawa
Department of Clinical Pharmacology and Therapeutics, Oita Medical University, Oita,
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
Koichi Kawano
Bayer Yakuhin Ltd., Osaka, and
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
Koichi Nakamura
Department of Clinical Pharmacology and Therapeutics, Oita Medical University, Oita,
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
Yoshihito Niki
Division of Respiratory Diseases, Department of Medicine, Kawasaki School of Medicine, Kawasaki, Japan
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
Shigeyuki Nakano
Department of Clinical Pharmacology and Therapeutics, Oita Medical University, Oita,
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
DOI: 10.1128/AAC.43.3.525
  • Article
  • Figures & Data
  • Info & Metrics
  • PDF
Loading

Article Figures & Data

Figures

  • Tables
  • Fig. 1.
    • Open in new tab
    • Download powerpoint
    Fig. 1.

    Changes in the urinary pH over 24 h in healthy subjects treated with ammonium chloride (●), sodium bicarbonate (▵), or water (○). Values represent means ± SDs for nine subjects.

Tables

  • Figures
  • Table 1.

    Influence of urinary pH on ciprofloxacin pharmacokinetics in plasma: a comparison between pharmacokinetic variables on three separate occasions under different conditions of urinary pH

    Pharmacokinetic variablesaResultb(SD) under treatment with:
    NaHCO3NH4ClH2O
    Cmax(μg/ml)1.729 (0.33)1.506 (0.238)1.804 (0.421)
    Tmax(h)1.2 (0.2)1.3 (0.5)1.0 (0.4)
    t1/2(h)4.6 (1.6)4.3 (1.1)4.2 (0.8)
    AUC (μg · h/ml)5.147 (0.680)5.320 (0.770)5.649 (0.884)
    CL/F(liters/h)37.971 (6.711)39.011 (5.599)37.464 (5.194)
    V/F(liters)248.762 (78.602) 234.484 (46.28)223.377 (37.52)
    CLR(liters/h)16.08 (3.02)16.78 (2.67)16.31 (2.67)
    Ae (mg)82.4 (16.5)88.4 (14.5)90.53 (9.8)
    • ↵a Tmax, time to peak concentration in plasma; t1/2, apparent elimination half-life; AUC, area under the plasma concentration-time curve (0 to 24 h); CL/F, apparent total body clearance;V/F, apparent volume of distribution; CLR, renal clearance; Ae, amount of unchanged drug excreted.

    • ↵b The pharmacokinetic parameters were calculated according to a two-compartment open model with first-order absorption. ANOVA was utilized to describe significant differences in the pharmacokinetic parameters and urinary pH; all differences were not significant.

  • Table 2.

    Amount of unchanged drug excreted into urine at various time periods after treatment with ammonium chloride, sodium bicarbonate, or watera

    Collection period (h)Amt (mg) of unchanged drug (SD) under treatment with:
    NaHCO3NH4ClH2O
    0–222.426 (9.679)24.756 (8.564)26.251 (5.156)
    2–420.099 (6.690)19.877 (5.327)21.988 (9.145)
    4–612.763 (3.253)12.695 (5.696)13.700 (3.366)
    6–88.220 (2.015)11.098 (5.958)9.314 (3.884)
    8–1210.935 (2.269)10.116 (2.546)10.598 (2.410)
    12–249.899 (2.604)8.304 (3.246)8.608 (3.927)
    • ↵a ANOVA was utilized to describe significant differences; all differences were not significant.

  • Table 3.

    Influence of pH and Ca2+ and Mg2+cations on the MICs of ciprofloxacin and sparfloxacin

    Strain and drugMIC [μg/ml (fold increase)] in brotha at pH:
    8.0 (MHB-A)7.25.8 (MHB-A)
    MHB-AMHB-BMHB-CMHB-D
    E. coli NIHJ JC-2
     Ciprofloxacin0.0160.031 (2)0.031 (2)0.063 (4)0.063 (4)0.125 (8)
     Sparfloxacin0.0080.031 (4)0.031 (4)0.063 (8)0.063 (8)0.25 (31)
    P. aeruginosa ATCC 27853
     Ciprofloxacin0.500.50 (1)0.50 (1)0.50 (1)1 (2)2 (4)
     Sparfloxacin0.502 (4)2 (4)4 (8)4 (8)8 (16)
    • ↵a MHB-A, MHB with concentrations of Ca2+ and Mg2+ of 25 and 12.5 mg/liter, respectively; MHB-B, MHB with concentrations of Ca2+ and Mg2+ of 50 and 25 mg/liter, respectively; MHB-C, MHB with concentrations of Ca2+ and Mg2+ of 125 and 62.5 mg/liter, respectively; MHB-D, MHB with concentrations of Ca2+ and Mg2+ of 250 and 125 mg/liter, respectively.

  • Table 4.

    Influence of human urine on the in vitro activities of ciprofloxacin (CPFX) and sparfloxacin (SPFX) against E. coliNIHJ JC-2 and P. aeruginosa ATCC 27853

    Subject no.NH4Cl treatmentNaHCO3 treatment
    pHConcn [mg/liter (fold increase)] of:MIC [μg/ml (fold increase)] for:pHConcn [mg/liter (fold increase)] of:MIC [μg/ml (fold increase)] for:
    Ca2+Mg2+E. coli NIHJ JC-2P. aeruginosa ATCC 27853Ca2+Mg2+E. coli NIHJ JC-2P. aeruginosa ATCC 27853
    CPFXSPFXCPFXSPFXCPFXSPFXCPFXSPFX
    15.36320 (4)145 (4.3)0.25 (4)0.25 (4)0.1252 (2)6.2886610.0630.0630.50 (2)1
    25.40220 (4)120 (1.2)0.125 (4)0.125 (4)0.125 (1)2 (4)6.37581000.0310.0310.1250.50
    35.27200 (2)800.50 (8)0.50 (8)0.125 (2)2 (4)6.1097105 (1.3)0.0630.0630.0630.50
    46.39200 (2)135 (2.5)0.063 (4)0.063 (4)0.25 (2)0.50 (4)7.7843530.0160.0160.1250.125
    56.03240 (2)145 (1)0.125 (2)0.25 (4)0.1252 (4)7.282251100.0630.0630.50 (4)0.50
    66.12200 (2)54 (1)0.50 (8)0.50 (8)0.25 (1)2 (1)7.1413440.0630.0630.252
    76.13270 (7)130 (1.3)0.125 (1)0.25 (1)0.25 (1)2 (1)7.43411000.1250.250.252
    85.7980 (1)70 (1)0.125 (2)0.125 (2)0.251 (2)6.3579850.0630.0630.50 (2)0.50
    95.3056 (1)33 (2)0.50 (31)0.50 (31)0.50 (1)2 (4)8.0136180.0160.0160.500.25
     Mean (SD)5.75 (0.43)178.4 (97)101.3 (40.1)6.97 (0.71)75.3 (58.6)75.1 (30.5)
     Range5.27–6.3956–32033–1450.063–0.500.063–0.500.125–0.500.50–26.84–8.113–22518–1100.016–0.1250.016–0.250.125–0.500.125–2
PreviousNext
Back to top
Download PDF
Citation Tools
Influences of Urinary pH on Ciprofloxacin Pharmacokinetics in Humans and Antimicrobial Activity In Vitro versus Those of Sparfloxacin
Marika Kamberi, Kimiko Tsutsumi, Tsutomu Kotegawa, Koichi Kawano, Koichi Nakamura, Yoshihito Niki, Shigeyuki Nakano
Antimicrobial Agents and Chemotherapy Mar 1999, 43 (3) 525-529; DOI: 10.1128/AAC.43.3.525

Citation Manager Formats

  • BibTeX
  • Bookends
  • EasyBib
  • EndNote (tagged)
  • EndNote 8 (xml)
  • Medlars
  • Mendeley
  • Papers
  • RefWorks Tagged
  • Ref Manager
  • RIS
  • Zotero
Print

Alerts
Sign In to Email Alerts with your Email Address
Email

Thank you for sharing this Antimicrobial Agents and Chemotherapy article.

NOTE: We request your email address only to inform the recipient that it was you who recommended this article, and that it is not junk mail. We do not retain these email addresses.

Enter multiple addresses on separate lines or separate them with commas.
Influences of Urinary pH on Ciprofloxacin Pharmacokinetics in Humans and Antimicrobial Activity In Vitro versus Those of Sparfloxacin
(Your Name) has forwarded a page to you from Antimicrobial Agents and Chemotherapy
(Your Name) thought you would be interested in this article in Antimicrobial Agents and Chemotherapy.
CAPTCHA
This question is for testing whether or not you are a human visitor and to prevent automated spam submissions.
Share
Influences of Urinary pH on Ciprofloxacin Pharmacokinetics in Humans and Antimicrobial Activity In Vitro versus Those of Sparfloxacin
Marika Kamberi, Kimiko Tsutsumi, Tsutomu Kotegawa, Koichi Kawano, Koichi Nakamura, Yoshihito Niki, Shigeyuki Nakano
Antimicrobial Agents and Chemotherapy Mar 1999, 43 (3) 525-529; DOI: 10.1128/AAC.43.3.525
del.icio.us logo Digg logo Reddit logo Twitter logo CiteULike logo Facebook logo Google logo Mendeley logo
  • Top
  • Article
    • ABSTRACT
    • MATERIALS AND METHODS
    • RESULTS
    • DISCUSSION
    • ACKNOWLEDGMENTS
    • FOOTNOTES
    • REFERENCES
  • Figures & Data
  • Info & Metrics
  • PDF

KEYWORDS

anti-infective agents
ciprofloxacin
fluoroquinolones

Related Articles

Cited By...

About

  • About AAC
  • Editor in Chief
  • Editorial Board
  • Policies
  • For Reviewers
  • For the Media
  • For Librarians
  • For Advertisers
  • Alerts
  • AAC Podcast
  • RSS
  • FAQ
  • Permissions
  • Journal Announcements

Authors

  • ASM Author Center
  • Submit a Manuscript
  • Article Types
  • Ethics
  • Contact Us

Follow #AACJournal

@ASMicrobiology

       

ASM Journals

ASM journals are the most prominent publications in the field, delivering up-to-date and authoritative coverage of both basic and clinical microbiology.

About ASM | Contact Us | Press Room

 

ASM is a member of

Scientific Society Publisher Alliance

 

American Society for Microbiology
1752 N St. NW
Washington, DC 20036
Phone: (202) 737-3600

Copyright © 2021 American Society for Microbiology | Privacy Policy | Website feedback

Print ISSN: 0066-4804; Online ISSN: 1098-6596