We developed a rapid screening method for determination of pK(a) of candidate drugs by pressure-assisted capillary electrophoresis (CE) coupled with a photodiode array detector. Application of pressure during CE analysis allowed completion of one CE run in less than 1 min, and the obtained pH-metric mobility shifts as well as pH-metric UV spectrum were analyzed by a nonlinear regression fitting software to determine pK(a) values. The difference between pK(a) values by this method and by other conventional methods is within 0.25 units for 82 ionic functional groups of 77 drugs. The pK(a) values of 96 compounds in dimethylsulfoxide solution on a 96-well microplate could be measured in 1 day. Our method provides rapid and accurate determination of pK(a) value.

01 Feb 2000·Expert Opinion on Investigational DrugsQ2 · MEDICINE

Novel oral cephalosporins

Q2 · MEDICINE

Review

Author: Cazzola, M

The therapeutic use of oral cephalosporins to treat infectious diseases continues to challenge clinicians; many attempts have been made over recent years to improve the efficacy and spectrum of these anti-infectives. Many oral cephalosporins are in development and include cefdinir, cefprozil, cefetamet pivoxil, cefcapene pivoxil, cefcanel daloxate hydrochloride in Phase II trials, S-1090 in Phase III trials and the novel compounds E1100, E1101 and BRL-57347. Differences between these drugs are sometimes subtle and the improvement over existing compounds modest, although recent cephalosporins have shown greater activity against Gram-negative bacterial infections. A better knowledge of the pharmacodynamic and pharmacokinetic interrelationships of existing oral cephalosporins is demanded for a more rational use of these compounds and to avoid the subsequent development of resistance. Perhaps with such an approach, the perceived need for new cephalosporins will diminish.

01 Jan 1999·ChemotherapyQ4 · MEDICINE

In vitro Bactericidal Activities of a New Oral Cephalosporin, E1100, and Morphologic Changes on Escherichia coli

Q4 · MEDICINE

Article

Author: Satoh, Masaru ; Sato, Yasumasa ; Kai, Jyunko ; Mikamo, Hiroshige ; Hayasaki, Yoh ; Tamaya, Teruhiko

Escherichia coli is one of the most common aerobic bacteria in pelvic inflammatory diseases. Oral cephalosporins have been widely used against those infections. We investigated in vitro morphologic changes induced on E. coli by a new oral cephalosporin, E1100, and its bactericidal activity on this organism. Morphologic changes were observed by electron microscopy. E1100 induced morphologic changes (filamentation) and exerted a bactericidal activity on E. coli. The filamentation induced by E1100 was time and concentration dependent.

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Indication	Highest Phase	Country/Location	Organization	Date
Bacterial Infections	Phase 2	Japan	Eisai Co., Ltd.	-

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