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 |
|---|---|
| Pages (from-to) | 303-306 |
| Number of pages | 4 |
| Journal | European Journal of Pharmaceutical Sciences |
| Volume | 2 |
| Issue number | 4 |
| DOIs | |
| State | Published - Jan 1 1994 |
| Externally published | Yes |
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Keywords
- Cetrorelix
- Instillation
- LH-RH analogues
- Pulmonary absorption
- Sheep, unanesthetized
ASJC Scopus subject areas
- Pharmaceutical Science
Cite this
Systematic delivery of the luteinizing hormone-releasing hormone (LH-RH) antagonist cetrorelix (SB-75) via pulmonary instillation in the unanesthetized awake sheep. / Schreier, Hans; Engel, Jürgen; McNicol, Ken J.; Derendorf, Hartmut; Groot, Kate; Schally, Andrew V.
In: European Journal of Pharmaceutical Sciences, Vol. 2, No. 4, 01.01.1994, p. 303-306.Research output: Contribution to journal › Article
}
TY - JOUR
T1 - Systematic delivery of the luteinizing hormone-releasing hormone (LH-RH) antagonist cetrorelix (SB-75) via pulmonary instillation in the unanesthetized awake sheep
AU - Schreier, Hans
AU - Engel, Jürgen
AU - McNicol, Ken J.
AU - Derendorf, Hartmut
AU - Groot, Kate
AU - Schally, Andrew V
PY - 1994/1/1
Y1 - 1994/1/1
N2 - 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%.
AB - 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%.
KW - Cetrorelix
KW - Instillation
KW - LH-RH analogues
KW - Pulmonary absorption
KW - Sheep, unanesthetized
UR - http://www.scopus.com/inward/record.url?scp=0028117799&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=0028117799&partnerID=8YFLogxK
U2 - 10.1016/0928-0987(94)90014-0
DO - 10.1016/0928-0987(94)90014-0
M3 - Article
VL - 2
SP - 303
EP - 306
JO - European Journal of Pharmaceutical Sciences
JF - European Journal of Pharmaceutical Sciences
SN - 0928-0987
IS - 4
ER -