Bioavailability of ciprofloxacin and fleroxacin: results of a preliminary investigation in healthy adult Nigerian male volunteers. 2000

C M Chukwuani, and H A Coker, and A M Oduola, and A Sowunmi, and N D Ifudu
Department of Pharmaceutical Chemistry, School of Pharmacy, College of Medicine, University of Lagos, Idi-Araba, Nigeria. chukwuani@cs.com

The absolute bioavailability (BA) of ciprofloxacin and fleroxacin were evaluated in 19 adult Nigerian male volunteers. Subjects meeting the selection criteria were randomized to receive treatment either with fleroxacin (200 mg-i.v. and 200 mg oral dose) or ciprofloxacin (200 mg-i.v. and 250 mg oral dose). The i.v./oral or oral/i.v. switch was made after a one week washout period. Blood and urine samples were collected at pre-determined time intervals over a 72 h period for analysis of drug levels. Following intravenous administration the maximum serum concentration (Cmax) was 2.7+/-1.06mg/l for ciprofioxacin and 0.99+/-0.41 mg/l for fleroxacin; the area under the blood level curve (AUC) was 8.82+/-3.19 mg x h/l with ciprofloxacin and 8.52+/-3.83 mg x h/l with fleroxacin. Following oral administration the Cmax was 1.52+/-0.94 mg/l with ciprofloxacin and 0.57+/-0.08 mg/l with fleroxacin; the AUC was 9.87+/-4.10 and 7.55+/-1.42 mg x h/l, respectively. The absolute BA following oral administration was found to be 0.79+/-0.47 for ciprofloxacin and 1.01+/-0.78 for fleroxacin. When these BA results were corrected for renal clearance [Cl(r)] and elimination half-life (t1/2) the values were reduced to 0.37+/-0.17 and 0.31+/-0.18, respectively, for ciprofloxacin and 0.53+/-0.23 and 0.99+/-0.38, respectively, for fleroxacin. Only 38% with ciprofloxacin and 59% with fieroxacin, of the administered dose, was excreted unchanged following oral administration. More work, however, needs to be done on ciprofloxacin to support and/or confirm the above findings. Fleroxacin, on the one hand, exhibited a different trend from that observed in the literature with respect to Cmax and AUC where the values observed in this study were 3--4 fold lower than expected following identical doses, whilst on the other hand the observed BA profile in this study was consistent with literature trends.

UI MeSH Term Description Entries
D008297 Male Males
D012016 Reference Values The range or frequency distribution of a measurement in a population (of organisms, organs or things) that has not been selected for the presence of disease or abnormality. Normal Range,Normal Values,Reference Ranges,Normal Ranges,Normal Value,Range, Normal,Range, Reference,Ranges, Normal,Ranges, Reference,Reference Range,Reference Value,Value, Normal,Value, Reference,Values, Normal,Values, Reference
D002939 Ciprofloxacin A broad-spectrum antimicrobial carboxyfluoroquinoline. Bay-09867,Ciprinol,Cipro,Ciprofloxacin Hydrochloride,Ciprofloxacin Hydrochloride Anhydrous,Ciprofloxacin Monohydrochloride Monohydrate,Anhydrous, Ciprofloxacin Hydrochloride,Bay 09867,Bay09867,Hydrochloride Anhydrous, Ciprofloxacin,Hydrochloride, Ciprofloxacin,Monohydrate, Ciprofloxacin Monohydrochloride,Monohydrochloride Monohydrate, Ciprofloxacin
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D000328 Adult A person having attained full growth or maturity. Adults are of 19 through 44 years of age. For a person between 19 and 24 years of age, YOUNG ADULT is available. Adults
D000890 Anti-Infective Agents Substances that prevent infectious agents or organisms from spreading or kill infectious agents in order to prevent the spread of infection. Anti-Infective Agent,Anti-Microbial Agent,Antimicrobial Agent,Microbicide,Microbicides,Anti-Microbial Agents,Antiinfective Agents,Antimicrobial Agents,Agent, Anti-Infective,Agent, Anti-Microbial,Agent, Antimicrobial,Agents, Anti-Infective,Agents, Anti-Microbial,Agents, Antiinfective,Agents, Antimicrobial,Anti Infective Agent,Anti Infective Agents,Anti Microbial Agent,Anti Microbial Agents
D001682 Biological Availability The extent to which the active ingredient of a drug dosage form becomes available at the site of drug action or in a biological medium believed to reflect accessibility to a site of action. Availability Equivalency,Bioavailability,Physiologic Availability,Availability, Biologic,Availability, Biological,Availability, Physiologic,Biologic Availability,Availabilities, Biologic,Availabilities, Biological,Availabilities, Physiologic,Availability Equivalencies,Bioavailabilities,Biologic Availabilities,Biological Availabilities,Equivalencies, Availability,Equivalency, Availability,Physiologic Availabilities
D016576 Fleroxacin A broad-spectrum antimicrobial fluoroquinolone. The drug strongly inhibits the DNA-supercoiling activity of DNA GYRASE. AM-833,Quinodis,Ro 23-6240,AM 833,AM833,Ro 23 6240,Ro 236240
D019540 Area Under Curve A statistical means of summarizing information from a series of measurements on one individual. It is frequently used in clinical pharmacology where the AUC from serum levels can be interpreted as the total uptake of whatever has been administered. As a plot of the concentration of a drug against time, after a single dose of medicine, producing a standard shape curve, it is a means of comparing the bioavailability of the same drug made by different companies. (From Winslade, Dictionary of Clinical Research, 1992) AUC,Area Under Curves,Curve, Area Under,Curves, Area Under,Under Curve, Area,Under Curves, Area

Related Publications

C M Chukwuani, and H A Coker, and A M Oduola, and A Sowunmi, and N D Ifudu
October 1988, The Journal of antimicrobial chemotherapy,
C M Chukwuani, and H A Coker, and A M Oduola, and A Sowunmi, and N D Ifudu
October 2003, Clinical therapeutics,
C M Chukwuani, and H A Coker, and A M Oduola, and A Sowunmi, and N D Ifudu
January 1995, Drugs,
C M Chukwuani, and H A Coker, and A M Oduola, and A Sowunmi, and N D Ifudu
January 1989, European journal of drug metabolism and pharmacokinetics,
C M Chukwuani, and H A Coker, and A M Oduola, and A Sowunmi, and N D Ifudu
December 2003, International journal of clinical pharmacology and therapeutics,
C M Chukwuani, and H A Coker, and A M Oduola, and A Sowunmi, and N D Ifudu
January 2011, Pakistan journal of pharmaceutical sciences,
C M Chukwuani, and H A Coker, and A M Oduola, and A Sowunmi, and N D Ifudu
October 1988, The Journal of antimicrobial chemotherapy,
C M Chukwuani, and H A Coker, and A M Oduola, and A Sowunmi, and N D Ifudu
April 2011, Biopharmaceutics & drug disposition,
C M Chukwuani, and H A Coker, and A M Oduola, and A Sowunmi, and N D Ifudu
April 2015, Journal of clinical pharmacology,
C M Chukwuani, and H A Coker, and A M Oduola, and A Sowunmi, and N D Ifudu
January 1987, European journal of clinical pharmacology,
Copied contents to your clipboard!