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 journalArticle

5 Citations (Scopus)

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 languageEnglish
Pages (from-to)303-306
Number of pages4
JournalEuropean Journal of Pharmaceutical Sciences
Volume2
Issue number4
DOIs
StatePublished - Jan 1 1994
Externally publishedYes

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Hormone Antagonists
Gonadotropin-Releasing Hormone
Sheep
Lung
Cross-Over Studies
Biological Availability
Pharmacokinetics
Injections
cetrorelix

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 journalArticle

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