Formulation containing amphipathic weak base and/or...

Details Formulation containing amphipathic weak base and/or... Formulation containing amphipathic weak base and/or...

2005-04-05

2005-04-05

Naff, David M. (Department: 1651)

Drug, bio-affecting and body treating compositions

Preparations characterized by special physical form

Biocides; animal or insect repellents or attractants

C424S049000, C424S058000, C424S404000, C514S001000, C514S254090, C514S279000, C514S280000, C514S359000, C514S415000

Reexamination Certificate

active

06875439

ABSTRACT:
Methods are provided relating to the enhanced cytoplasmic accumulation of amphipathic weakly basic or amphipathic cationic molecules in prokaryotes and eukaryotes under conditions of high extracellular pH. Furthermore, the methods relate to the unexpected synergistic effects of high extracellular pH and disrupted cellular efflux mechanisms on the cytoplasmic accumulation of amphipathic weakly basic or amphipathic cationic molecules in prokaryotes and eukaryotes. Methods are also provided for increasing the therapeutic potency of amphipathic weakly basic or amphipathic cationic compounds, e.g. antiseptics and disinfectants by using the antiseptic or disinfectant in the presence of a multiple drug resistance inhibitor such as reserpine. Finally, methods also relate to the exploitation of the aforementioned discoveries in the screening of small molecules, and libraries thereof, for biological activity in prokaryotes and eukaryotes. Also provided is a formulation comprising an amphipathic weak base, an amphipathic cation, or both, and a multiple drug resistance inhibitor wherein the pH of the formulation is 9.0. Furthermore, the combination of these ingredients have antiseptic and/or disinfectant effects.

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