Biomaterial Database

Pharmacokinetics of detirelix following intratracheal instillation and aerosol inhalation in the unanesthetized awake sheep. 1994

H Schreier, and K J McNicol, and D B Bennett, and Z Teitelbaum, and H Derendorf

Drug Delivery Laboratory, University of Florida Progress Center, Alachua.

The unanesthetized awake sheep was employed as large animal model for the determination of bioavailability and pharmacokinetics following the pulmonary instillation of the decapeptide detirelix. After intratracheal administration of a 80 micrograms/kg dose, the average t1/2 of elimination was 9.8 +/- 1.3 hours (n = 5) which was similar to the elimination kinetics of a 30 micrograms/kg i.v. dose (7.2 +/- 2.9 hours). Mean residence time (MRT) was prolonged to 10.3 +/- 2.0 hours vs. 2.7 +/- 0.8 hours i.v., and mean absorption time (MAT) was calculated to be 7.5 +/- 1.8 hours. Maximum plasma levels (cmax) of 9.2 ng/ml were reached after 2 hours. The average bioavailability was 9.8 +/- 3.9% of the dose. The pharmacokinetic profile was found to be similar after aerosol administration. It was concluded that detirelix was absorbed systemically when administered by pulmonary instillation or aerosolization and that the unanesthetized awake sheep is a suitable model to study resulting drug profiles.

UI	MeSH Term	Description	Entries
D007987	Gonadotropin-Releasing Hormone	A decapeptide that stimulates the synthesis and secretion of both pituitary gonadotropins, LUTEINIZING HORMONE and FOLLICLE STIMULATING HORMONE. GnRH is produced by neurons in the septum PREOPTIC AREA of the HYPOTHALAMUS and released into the pituitary portal blood, leading to stimulation of GONADOTROPHS in the ANTERIOR PITUITARY GLAND.	FSH-Releasing Hormone,GnRH,Gonadoliberin,Gonadorelin,LH-FSH Releasing Hormone,LHRH,Luliberin,Luteinizing Hormone-Releasing Hormone,Cystorelin,Dirigestran,Factrel,Gn-RH,Gonadorelin Acetate,Gonadorelin Hydrochloride,Kryptocur,LFRH,LH-RH,LH-Releasing Hormone,LHFSH Releasing Hormone,LHFSHRH,FSH Releasing Hormone,Gonadotropin Releasing Hormone,LH FSH Releasing Hormone,LH Releasing Hormone,Luteinizing Hormone Releasing Hormone,Releasing Hormone, LHFSH
D008954	Models, Biological	Theoretical representations that simulate the behavior or activity of biological processes or diseases. For disease models in living animals, DISEASE MODELS, ANIMAL is available. Biological models include the use of mathematical equations, computers, and other electronic equipment.	Biological Model,Biological Models,Model, Biological,Models, Biologic,Biologic Model,Biologic Models,Model, Biologic
D000280	Administration, Inhalation	The administration of drugs by the respiratory route. It includes insufflation into the respiratory tract.	Drug Administration, Inhalation,Drug Administration, Respiratory,Drug Aerosol Therapy,Inhalation Drug Administration,Inhalation of Drugs,Respiratory Drug Administration,Aerosol Drug Therapy,Aerosol Therapy, Drug,Drug Therapy, Aerosol,Inhalation Administration,Administration, Inhalation Drug,Administration, Respiratory Drug,Therapy, Aerosol Drug,Therapy, Drug Aerosol
D000336	Aerosols	Colloids with a gaseous dispersing phase and either liquid (fog) or solid (smoke) dispersed phase; used in fumigation or in inhalation therapy; may contain propellant agents.	Aerosol
D000818	Animals	Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA.	Animal,Metazoa,Animalia
D001682	Biological Availability	The extent to which the active ingredient of a drug dosage form becomes available at the site of drug action or in a biological medium believed to reflect accessibility to a site of action.	Availability Equivalency,Bioavailability,Physiologic Availability,Availability, Biologic,Availability, Biological,Availability, Physiologic,Biologic Availability,Availabilities, Biologic,Availabilities, Biological,Availabilities, Physiologic,Availability Equivalencies,Bioavailabilities,Biologic Availabilities,Biological Availabilities,Equivalencies, Availability,Equivalency, Availability,Physiologic Availabilities
D012756	Sheep	Any of the ruminant mammals with curved horns in the genus Ovis, family Bovidae. They possess lachrymal grooves and interdigital glands, which are absent in GOATS.	Ovis,Sheep, Dall,Dall Sheep,Ovis dalli
D014132	Trachea	The cartilaginous and membranous tube descending from the larynx and branching into the right and left main bronchi.	Tracheas