Patent Evaluation: Novel Compositions for the Improved Gastrointestinal Absorption of Antibiotics

Summary

Novelty: Oral antibacterial compositions containing a penem or carbapenem antibiotic in combination with an absorption improver, are disclosed. The absorption improver is selected from substances able to inhibit the dipeptidase localized on or in epithelial cells of the small intestine.

Biology: The degradation of a penem in vivo in rat epithelial cell isolated by citric acid from the small intestine was assayed by HPLC. After 60 minute incubation of 9 μg/ml of the penem and 35 μg/ml of cilastatin, 7.38 μg/ml of the free acid of the penem was measured, compared to 2.08 μ/ml remaining on addition of the penem alone. Five in vivo tests on Sprague-Dawley male rats and two tests on dogs are described. Six of the tests appear to shown an increase in the area under the plasma concentration time curve with the use of an absorption improver.

Chemistry: The use of cilastalin, glutathione and N-acetyl-L-cysteine are specifically claimed. No antibiotics are specifically claimed.