Abstract
The aim of this work was to prepare pH-dependent clarithromycin microsphere formulation by emulsion solvent evaporation method, employing Eudragit® L-100. Prepared microspheres were evaluated by carrying out in vitro release and in vivo pharmacokinetics studies. Drug–polymer interactions were studied by differential scanning calorimetry, X-ray diffractometry analyses and results showed that clarithromycin was molecularly dispersed in the polymer. The particle size distribution of microspheres was found over the range of 10~50 μm. The drug is hardly released in the HCl solution pH 1.2 in the first 2 h, but is rapidly released in phosphate buffer pH 7.2, and the cumulated release reached 98.1 % at 8 h. The pharmacokinetic profiles were conducted open, randomized, two-period crossover design with a 7-day interval between doses in healthy beagle dogs. The results indicated that the extent of absorption of the clarithromycin-load microspheres was the same as pure drug, but different in the rate of drug absorption in vivo.
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This work was supported by grant of the young teacher career development support foundation of Shenyang Pharmaceutical University.
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J. Xu and W. Li contributed equally to the work.
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Xu, J., Li, W., Liu, Z. et al. Preparation, characterization and pharmacokinetics evaluation of clarithromycin-loaded Eudragit® L-100 microspheres. Eur J Drug Metab Pharmacokinet 41, 287–293 (2016). https://doi.org/10.1007/s13318-015-0261-x
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DOI: https://doi.org/10.1007/s13318-015-0261-x