MICROVESICLE FORMULATION CONTAINING SODIUM 3 ,7 - DIHYDROXY-12- KETO-5 - CHOLANATE ENHANCES ORAL ABSORPTION OF CEFOTAXIME

Abstract

Cefotaxime sodium (CEF) is a water-soluble semi-synthetic cephalosporin, which exhibits a potent activity against various bacteria. CEF is not appreciably absorbed from the gastrointestinal tract and is therefore only available in an injection form, as the sodium salt. Bioavailability of CEF after oral administration is less than 5%. CEF is class III based upon the biopharmaceutical classification system. The low oral bioavailability is mostly due to its instability in the harsh environment of the stomach and intestine. Studies have shown that CEF solution exhibits maximum stability in the pH range of 4.3-6.5. Degradation appears to be rapid at pH 1.5. It was reported that the - lactam moiety undergoes hydrolysis at lower pH while at higher pH~8, the side chain undergoes hydrolysis (1).