Abstract
The pharmacokinetics of Cetrorelix acetate (SB-75), [Ac-D-Nal(2)1, D-Phe(4Cl)2, D-Pal(3)3, D-Cit6, D-Ala10]LH-RH, a highly potent LH-RH antagonist following i.v. injection and intratracheal instillation (i.t.), were determined in five unanesthetized, awakw sheep in a cross-over design. After i.t. administration the mean terminal t 1 2 was 11.6±5.2 h, similar to the i.v. elimination t 1 2 of 10.1±0.9 h. Mean residence time (MRT) was prolonged to 11.0±3.4 h vs. 5.9±1.3h i.v., and mean absorption time (MAT) was 5.6 ± 3.9 h. Cmax of 134±79 ng/ml was reached after 1.8±0.5 h (tmax). The mean i.t. bioavailability was 15.4±10.6%.
| Original language | English (US) |
|---|---|
| Pages (from-to) | 303-306 |
| Number of pages | 4 |
| Journal | European Journal of Pharmaceutical Sciences |
| Volume | 2 |
| Issue number | 4 |
| DOIs | |
| State | Published - Nov 1994 |
| Externally published | Yes |
Keywords
- Cetrorelix
- Instillation
- LH-RH analogues
- Pulmonary absorption
- Sheep, unanesthetized
ASJC Scopus subject areas
- Pharmaceutical Science
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Schreier, H., Engel, J., McNicol, K. J., Derendorf, H., Groot, K., & Schally, A. V. (1994). Systematic delivery of the luteinizing hormone-releasing hormone (LH-RH) antagonist cetrorelix (SB-75) via pulmonary instillation in the unanesthetized awake sheep. European Journal of Pharmaceutical Sciences, 2(4), 303-306. https://doi.org/10.1016/0928-0987(94)90014-0