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 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. 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 (US)
Pages (from-to)303-306
Number of pages4
JournalEuropean Journal of Pharmaceutical Sciences
Volume2
Issue number4
DOIs
StatePublished - Nov 1994
Externally publishedYes

Keywords

  • Cetrorelix
  • Instillation
  • LH-RH analogues
  • Pulmonary absorption
  • Sheep, unanesthetized

ASJC Scopus subject areas

  • Pharmaceutical Science

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