ORAL THERAPEUTICS AND PHARMACOLOGY
Online ISSN : 1884-4928
Print ISSN : 0288-1012
ISSN-L : 0288-1012
Comparative Study on Human Blood Concentration of Oral Cephem Antibiotics CXM-AX vs CCL
-Effect of Food on Bioavailability-
MASAHIKO YAMAGUCHITAZUKO SATOHFUMIHISA KIKUCHIYOUSUKE IWASHIGEYOSHIKI ISHIGAKICHIE YANAICHIHO TAKADAMOTOHIRO SUZUKINOBORU SONOYAMA
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1992 Volume 11 Issue 2 Pages 99-104

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Abstract
Some of the oral antibiotics which have been developed recently are prodrugs, aiming at im-provement of bioavailability.
These drugs are said to be hardly subject to food and are more smoothly transferred into blood when they are administered after having food. We have conducted a comparative study on a prodrug type-new cephem oral antibiotic, cefuroxime-axetil (CXM-AX) recently approved for the clinical indication in the area of dentistry and oral surgery, vs a non prodrug type cephem oral antibiotic, cefaclor (CCL), commonly used in the field of dentistry to examine influence of food on transfer of the orally given drugs into blood in healthy volunteers.
Results
1) In CXM-AX administration group, the serum concentration attained the peak 0.5 hour later in the group which took the drug after having food and the peak concentration was 1.6 times higher in the same group, compared with the group which took the drug at fasting.
2) In CCL administration group, the serum concentration attained the peak 0.94 hour later in the group which took the drug after having meal, and the such concentration was about twice as higher at fasting, compared with the counterpart group.
3) From the above, it was concluded that CXM-AX is hardly subject to influence of food, and it's transfer rate into blood is higher when it is administered after having meal, whereas, CCL transfer into blood is more subject to influence of food.
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© JAPANESE SOCIETY OF ORAL THERAPEUTICS AND PHARMACOLOGY
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