In a previous paper3), we reported on the synthesis and the biological activity of 3-methoxymethyl cephalosporin derivatives, one of which, cefpodoxime proxetil (Fig. 1), has been successfully developed as a prodrug for oral use. Our further elaboration for developing orally active cephalosporins has been made in the direction of chemical modification of the C-7 acyl substituent of the 3-methox...

Three groups of six healthy adult volunteers were randomly assigned to a treatment with 400 mg of oral cefpodoxime proxetil, oral cefixime, or placebo per day for 10 days. Informed consent was obtained from all volunteers. Clostridium difficile was not detected in the feces of any subject before treatment or at any time in the subjects in the placebo group. C. difficile was, however, detected i...

A new, simple, precise, rapid and accurate RP-HPLC method has been developed for the simultaneous estimation of cefpodoxime proxetil and clavulanic acid from pharmaceutical dosage forms. The method was carried out on a Zorbax Eclipse XDB 5 mu C 18 (150x4.6 mm) column with a mobile phase consisting of acetonitrile:50 mM potassium dihydrogen phosphate buffer (pH 3.0, 70:30 v/v) at a flow rate of ...

BACKGROUND AND THE PURPOSE OF THE STUDY The objective of the present work was to improve bioavailability of cepodoxime proxetil through gastroretentive microballoon formulation. METHODS Microballoons of cefpodoxime proxetil were formulated by solvent evaporation and diffusion method employing hydroxypropylmethyl cellulose (HPMC) and ethyl cellulose (EC) polymers and characterized for particle...

We compared the effects of nifedipine and diltiazem on the uptake of cefpodoxime proxetil (CP). The study was aimed at establishing the impact of increased mesenteric blood flow due to calcium channel blockers on passive transport. Twelve volunteers were given CP (200 mg) orally in a crossover design. The absorption, disposition, and elimination parameters of cefpodoxime were compared among the...

      The objective of the present study was to develop floating microspheres of cefpodoxime proxetil in order to achieve an extended retention in the upper GIT, which may result in enhanced absorption and thereby improved bioavailability. The microspheres were prepared by non-aqueous solvent evaporation method using polymers such as hydroxyl propyl methyl cellulose (HPMC K 15 M), ethyl cellulo...

OBJECTIVE To discuss the pharmacokinetics, spectrum of activity, clinical trials, and adverse effects of cefprozil, cefpodoxime proxetil, loracarbef, cefixime, and ceftibuten, an investigational cephalosporin. DATA SOURCES Literature was identified by a MEDLINE search from 1986 to January 1995. STUDY SELECTION Randomized, controlled studies were selected for evaluation; however, uncontrolle...