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 - 1994/11
Y1 - 1994/11
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
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U2 - 10.1016/0928-0987(94)90014-0
DO - 10.1016/0928-0987(94)90014-0
M3 - Article
AN - SCOPUS:0028117799
VL - 2
SP - 303
EP - 306
JO - European Journal of Pharmaceutical Sciences
JF - European Journal of Pharmaceutical Sciences
SN - 0928-0987
IS - 4
ER -