Single-dose pharmacokinetic study of ciprofloxacin and fleroxacin in healthy adult Nigerian volunteers. 1998

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

The kinetics of absorption, distribution and elimination of ciprofloxacin and fleroxacin (following an intravenous dose of 200 mg), were evaluated in 24 adult healthy male Nigerian volunteers. Appropriate mathematical models were applied with the aid of a microcomputer software program for the estimation of the basic pharmacokinetic parameters. Appropriate statistical tests and profiles formed the basis for accepting or rejecting a proposed model. For parametric comparisons between the profile of the two drugs, the null hypothesis of no difference in their pharmacokinetic profile was proposed. All statistical tests were performed at a significance level of 95% (alpha = 0.05) and the 95% confidence level was determined where appropriate. Additionally, the model-independent or stochastic method of analysis was also employed in the pharmacokinetic evaluation of the blood level data. The parametric estimates obtained from both methods were compared. The plasma elimination half-life (t1/2) was estimated as 13.8 +/- 5.5 h for fleroxacin and 7.5 +/- 4.0 h for ciprofloxacin; the maximal plasma concentration (Cmax) was 0.8 +/- 0.3 and 2.3 +/- 1.0 mg/l for fleroxacin and ciprofloxacin, respectively, whilst the volume of distribution (Vd) was 2.5 +/- 1.6 and 0.4 +/- 0.3 liters/kg for fleroxacin and ciprofloxacin, respectively. 71 and 70% of unchanged drug were excreted in urine for fleroxacin and ciprofloxacin, respectively. With respect to comparative values, the results confirmed trends already observed in the literature, particularly as regards the t1/2. However, for fleroxacin there was a significant deviation from the literature trends with respect to Vd, Cmax and AUC. The results also confirmed earlier findings, advocating a once-daily dosage schedule for fleroxacin also in the Negroid population.

UI MeSH Term Description Entries
D007262 Infusions, Intravenous The long-term (minutes to hours) administration of a fluid into the vein through venipuncture, either by letting the fluid flow by gravity or by pumping it. Drip Infusions,Intravenous Drip,Intravenous Infusions,Drip Infusion,Drip, Intravenous,Infusion, Drip,Infusion, Intravenous,Infusions, Drip,Intravenous Infusion
D008297 Male Males
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
D004334 Drug Administration Schedule Time schedule for administration of a drug in order to achieve optimum effectiveness and convenience. Administration Schedule, Drug,Administration Schedules, Drug,Drug Administration Schedules,Schedule, Drug Administration,Schedules, Drug Administration
D005260 Female Females
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D000042 Absorption The physical or physiological processes by which substances, tissue, cells, etc. take up or take in other substances or energy.
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
D014018 Tissue Distribution Accumulation of a drug or chemical substance in various organs (including those not relevant to its pharmacologic or therapeutic action). This distribution depends on the blood flow or perfusion rate of the organ, the ability of the drug to penetrate organ membranes, tissue specificity, protein binding. The distribution is usually expressed as tissue to plasma ratios. Distribution, Tissue,Distributions, Tissue,Tissue Distributions

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