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Intranasal Administration of Insulin With Phospholipid as Absorption Enhancer: Pharmacokinetics in Normal Subjects
Author(s) -
Drejer Kirsten,
Vaag A.,
Bech K.,
Hansen P.,
Sørensen A.R.,
Mygind N.
Publication year - 1992
Publication title -
diabetic medicine
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.474
H-Index - 145
eISSN - 1464-5491
pISSN - 0742-3071
DOI - 10.1111/j.1464-5491.1992.tb01792.x
Subject(s) - medicine , nasal administration , insulin , pharmacokinetics , endocrinology , bioavailability , glucagon , pharmacology
The pharmacokinetics of intranasal insulin containing a medium‐chain phospholipid (didecanoyl‐L‐alpha‐phosphatidylcholine) as absorption enhancer, was studied in normal volunteers by measuring plasma glucose, insulin, C‐peptide, and glucagon. Eleven fasting subjects received 4 U insulin intravenously, 6 U subcutaneously, or three doses intranasally (approximately 0.3 U kg −1 , 0.6 U kg −1 , 0.8 U kg −1 ) in random order on five separate days. Intranasal insulin was absorbed in a dose‐dependent manner with a mean plasma insulin peak 23 ± 7 (± SE) min after administration. Mean plasma glucose nadir was seen after 44 ± 6 min, 20 min later than following intravenous injection. Furthermore, intranasal administration of insulin resulted in a faster time‐course of absorption than subcutaneous injection, with significantly reduced intersubject variation ( p < 0.001). Bioavailability for the nasal formulation was 8.3% relative to an intravenous bolus injection when plasma insulin was corrected for endogenous insulin production estimated by C‐peptide. A dose‐dependent suppression of C‐peptide and stimulation of glucagon secretion occurred after intranasal administration of insulin. Nasal irritation from spraying was absent or slight.