Systematic delivery of the luteinizing hormone-releasing hormone (LH-RH) antagonist cetrorelix (SB-75) via pulmonary instillation in the unanesthetized awake sheep

Hans Schreier; Jürgen Engel; Ken J. McNicol; Hartmut Derendorf; Kate Groot; Andrew V. Schally

doi:10.1016/0928-0987(94)90014-0

Systematic delivery of the luteinizing hormone-releasing hormone (LH-RH) antagonist cetrorelix (SB-75) via pulmonary instillation in the unanesthetized awake sheep

Hans Schreier, Jürgen Engel, Ken J. McNicol, Hartmut Derendorf, Kate Groot, Andrew V. Schally

Research output: Contribution to journal › Article › peer-review

5 Scopus citations

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. C_max 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	https://doi.org/10.1016/0928-0987(94)90014-0
State	Published - Nov 1994
Externally published	Yes

Keywords

Cetrorelix
Instillation
LH-RH analogues
Pulmonary absorption
Sheep, unanesthetized

ASJC Scopus subject areas

Pharmaceutical Science

Access to Document

10.1016/0928-0987(94)90014-0

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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, 11.1994, p. 303-306.

Research output: Contribution to journal › Article › peer-review

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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%.",

keywords = "Cetrorelix, Instillation, LH-RH analogues, Pulmonary absorption, Sheep, unanesthetized",

author = "Hans Schreier and J{\"u}rgen Engel and McNicol, {Ken J.} and Hartmut Derendorf and Kate Groot and Schally, {Andrew V.}",

year = "1994",

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AU - Schally, Andrew V.

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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%.

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