Muto N, Mitoh Y, Yamamoto I
Department of Immunochemistry, Faculty of Pharmaceutical Sciences, Okayama University, Japan.
J Immunoassay. 1990;11(1):1-16. doi: 10.1080/01971529008053254.
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.
开发了一种用于新型吡啶酮羧酸抗菌剂OPC-7251的灵敏酶免疫测定法，并将其应用于人体血浆水平的测定。OPC-7251通过形成N-羟基琥珀酰亚胺酯与牛血清白蛋白偶联。通过免疫兔子，获得了高度特异性的抗血清。使用该抗血清和β-D-半乳糖苷酶标记的半抗原，同源测定系统能够检测到2 pg的该化合物。血浆样品经热处理后可精确分析至最低值200 pg/ml。该系统通过回收率测试以及与高效液相色谱分析的相关性进一步得到验证。对健康志愿者经皮涂抹10 g 1%的OPC-7251乳膏，给药后约8小时血浆峰值为1.6 ng/ml，表明经皮系统的吸收效率极低。
