| Abstract | SCH 40120 is a potent acute anti-inflammatory agent under development for topical treatment of dermal inflammatory and allergic disorders such as atopic dermatitis, contact dermatitis and psoriasis. In order to support percutaneous absorption studies, a competitive enzyme immunoassay (EIA) was developed to determine SCH 40120 in unextracted plasma samples. SCH 38280, a carboxylated analogue of SCH 40120, was used as the hapten and conjugated with bovine thyroglobulin (Thy). The hapten-Thy conjugate was used as the immunogen to immunize rabbits for antibody production. The hapten was also coupled to horseradish peroxidase (HRP) to form SCH 38280-HRP, which was used as the tracer. The EIA can detect SCH 40120 concentrations as low as 50 pg ml-1 of plasma, and can reliably quantitate SCH 40120 in plasma samples from 100 pg ml-1 to 10 ng ml-1 with good linearity, accuracy and precision. A variety of structurally related compounds and potential metabolites did not significantly cross-react with the antibodies, except for a few analogues. The availability of this sensitive assay makes it possible to evaluate the pharmacokinetics of SCH 40120 in man. |
| Authors | C J Wang, Z Tian, C Gommoll, V Reyes, C C Lin
(Affiliation: Department of Drug Metabolism and Pharmacokinetics, Schering-Plough Research Institute, Kenilworth, NJ 07033.)
|
| Journal | Journal of pharmaceutical and biomedical analysis
(J Pharm Biomed Anal)
Vol. 11
Issue 10
Pg. 871-9
(Oct 1993)
ISSN: 0731-7085 ENGLAND |
| PMID | 8305589
(Publication Type: Journal Article)
|
| Chemical References |
- Anti-Inflammatory Agents, Non-Steroidal
- Lipoxygenase Inhibitors
- Naphthyridines
- Sch 40120
- Thyroglobulin
- Horseradish Peroxidase
|
| Topics |
- Administration, Cutaneous
- Animals
- Anti-Inflammatory Agents, Non-Steroidal
(administration & dosage, blood, pharmacokinetics)
- Horseradish Peroxidase
- Humans
- Immunoenzyme Techniques
- Lipoxygenase Inhibitors
(administration & dosage, blood, pharmacokinetics)
- Naphthyridines
(administration & dosage, blood, pharmacokinetics)
- Rabbits
- Reproducibility of Results
- Sensitivity and Specificity
- Thyroglobulin
|
