OBJECTIVE: To study the pharmacokinetics and relative bioavailability of clarithromycin capsule. METHODS: A microbiological agar diffusion assay using Micrococcus luteus(ATCC 28001) was used as a bioassay for clarithromycin in serum following a single oral dose 500 mg of clarithromycin capsule and tablet respectively given to 10 healthy volunteers in an open randomized crossover test.The data obtained were fitted with PKBP-N1 program. RESULTS: A linear relationship was obtained between the peak area ratio and the concentration of clarithromycin from 0.05 to 4.00 μg·ml-1and the lowest limit of detection of clarithromycin in serum was 0.05 μg·ml-1Precisions were under 8.20%.The recoveries were 99.04%~101.48%.The onecompartment open model with first order absorption was used to described the time course of serum concentrations of clarithromycin in human following administration of a single oral dose 500 mg as capsule and tablet.The results were tpeak=(1.45±0.50) h and (1.55±0.44) h,cmax=(2.20±0.39) μg·ml-1and (2.15±0.33) μg·ml-1,AUC=(17.60±2.85) μg·h·ml-1 and (17.74±3.46) μg·h·ml-1. CONCLUSION: There were no significant differneces between their pharmacokinetic parameters.The tested capsule and the reference tablet is bioequivalent with Frel=101.64%.
Key words
clarithromycin /
pharmacokinetics
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References
[1]Peters DH,Clissold SP.Clarithromycin,a review of its antimicro-bial activity,pharmacokinetics properties and therapeutic poten-
tial.Drugs,1992,44(l):117.
[2]Chu SY,Deaton R,Cavanaugh J.Absolute bioavailability of clar-ithromycin after oral administration in hnrr,anc.Antimicrob Agents Cleemother,1992,36(5):1147.
[3]Edited by Brittain HG.Analytical Profiles of Drug Substances and Excipents.Academic Press,lnc.,1996,24:78一81.
[4]Eernandes PB,Hardy DJ,Mcdaniel D,et al.In vitro and in vi-vo activities of clarithromycin against Mycrobacterium avium.
Antimicrob八gents Chemother,1989:33(9):1531.
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Footnotes
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