A comparative study of characteristics of current-type and conventional-type cationic bactericides.
We have synthesized new polycationic bactericides, polyloxyethylene(dimethyliminio)trimethylene(dimethyliminio)ethylene dichloridel (OXD) and poly(hexamethyleneguanidine phosphate) (HEP), in order to develop more active but less skin-irritative bactericides. The effects of these bactericides on Pseudomonas aeruginosa, Escherichia coli, Serratia marcescens, Klebsiella pneumoniae, methicillin resistant Staphylococcus aureus (MRSA) and the degree of their irritations on skin were compared with those of a widely used low molecular-weight cationic bactericide, benzalkonium chloride (BAC), and a polycationic bactericide, poly[2-hydroxyethylene(dimethyliminio)methylene chloride] (2HYC). The minimum bactericidal concentration (MBC) of OXD for 10 min contact incubation was 16 microg/ml against P. aeruginosa, E. coli, S. marcescens and K. pneumoniae, and >1000 microg/ml against MRSA. The MBC of HEP for 10 min contact incubation was 16 microg/ml against P. aeruginosa, 32 microg/ml against E. coli and K. pneumoniae, and 64 microg/ml against S. marcescens and MRSA. Itch, edema, erythema, heat, injury, desquamation and keratinization caused by skin irritation were examined in 21 subjects by patch tests. Only one subject treated with OXD experienced edema, and one subject with HEP experienced keratinization. However, BAC caused itch in 3 subjects, edema in 1, erythema in 10 and desquamation in 2, indicating that the incidence of skin irritation of BAC was higher than that of OXD or HEP. OXD and HEP had sterilization ability similar to BAC, however, they were less skin-irritative than BAC. This indicates that OXD and HEP can be used as safe bactericides.
Ohta
S
S
Department of Pharmacy, Shinshu University Hospital, Matsumoto, Japan. sohta@nagano-med.jrc.or.jp
Misawa
Y
Y
Miyamoto
H
H
Makino
M
M
Nagai
K
K
Shiraishi
T
T
Nakagawa
Y
Y
Yamato
S
S
Tachikawa
E
E
Zenda
H
H
D000328:Adult; D000891:Anti-Infective Agents, Local / Q000737:chemistry* / Q000494:pharmacology* / Q000633:toxicity; D001419:Bacteria / Q000187:drug effects*; D001548:Benzalkonium Compounds / Q000737:chemistry / Q000494:pharmacology / Q000633:toxicity; D003470:Culture Media; D005260:Female; D006146:Guanidines / Q000737:chemistry* / Q000494:pharmacology* / Q000633:toxicity; D006801:Humans; D007509:Irritants / Q000633:toxicity; D008297:Male; D008826:Microbial Sensitivity Tests; D008970:Molecular Weight; D011073:Polyamines / Q000737:chemistry* / Q000494:pharmacology* / Q000633:toxicity; D011092:Polyethylene Glycols / Q000737:chemistry* / Q000494:pharmacology* / Q000633:toxicity; D012867:Skin / Q000187:drug effects / Q000473:pathology
D000891:Anti-Infective Agents, Local; D001548:Benzalkonium Compounds; D003470:Culture Media; D006146:Guanidines; D007509:Irritants; D011073:Polyamines; C446507:poly(2-hydroxyethylene(dimethyliminio)methylene chloride); C446506:poly(oxyethylene(dimethyliminio)trimethylene(dimethyliminio)ethylene dichloride); C060540:polyhexamethyleneguanidine; D011092:Polyethylene Glycols