Development of a sensitive enzyme immunoassay for OPC-7251, a novel antimicrobial agent for percutaneous application.
A sensitive enzyme immunoassay for OPC-7251, a novel pyridone carboxylic acid antimicrobial agent, was developed and applied for the determination of human plasma levels. OPC-7251 was coupled to bovine serum albumin through a formation of N-hydroxysuccinimide ester. By immunization of rabbits, highly specific antiserum was raised. Using the antiserum and beta-D-galactosidase-labeled hapten, the homologous assay system allowed the detection of 2 pg of this compound. Plasma samples were precisely analyzed down to the minimum value of 200 pg/ml after heat treatment. The system was further validated by the recovery test and correlation with the HPLC analyses. Percutaneous application of 10 g of 1% OPC-7251 cream to healthy volunteers resulted in the peak plasma value of 1.6 ng/ml about 8 hours after dosing, indicating extremely low absorption efficiency through a transdermal system.
Muto
N
N
Department of Immunochemistry, Faculty of Pharmaceutical Sciences, Okayama University, Japan.
Mitoh
Y
Y
Yamamoto
I
I
D000279:Administration, Cutaneous; D000818:Animals; D000890:Anti-Infective Agents; D000891:Anti-Infective Agents, Local / Q000097:blood*; D003432:Cross-Linking Reagents; D024841:Fluoroquinolones; D006801:Humans; D007106:Immune Sera; D007124:Immunoenzyme Techniques; D008297:Male; D011807:Quinolizines / Q000097:blood*; D011817:Rabbits; D051381:Rats; D012710:Serum Albumin, Bovine
D000890:Anti-Infective Agents; D000891:Anti-Infective Agents, Local; D003432:Cross-Linking Reagents; D024841:Fluoroquinolones; D007106:Immune Sera; D011807:Quinolizines; D012710:Serum Albumin, Bovine; C062127:nadifloxacin