Pharmacokinetic and Pharmacodynamic Properties of a Micro-Dose Nasal Spray Formulation of Desmopressin (AV002) in Healthy Water-Loaded Subjects.
antidiuresis
bioavailability
hyponatremia
safety
urine osmolality
Journal
Pharmaceutical research
ISSN: 1573-904X
Titre abrégé: Pharm Res
Pays: United States
ID NLM: 8406521
Informations de publication
Date de publication:
29 Apr 2019
29 Apr 2019
Historique:
received:
17
10
2018
accepted:
10
04
2019
entrez:
1
5
2019
pubmed:
1
5
2019
medline:
24
5
2019
Statut:
epublish
Résumé
Antidiuretic therapy with desmopressin for nocturia has been hampered by formulations with high doses, low bioavailability and variable pharmacokinetics. AV002 (SER120), a novel, emulsified, microdose desmopressin nasal spray, with a permeation enhancer (cylcopentadecanolide), was developed to have pharmacokinetic characteristics suitable for nocturia treatment. Twelve healthy subjects participated in an open-label, dose-escalating study. Water-loaded subjects were sequentially dosed every 48 h with AV002 0.5, 1.0, 2.0 μg and 0.12 μg desmopressin subcutaneous (SC) bolus injection. AV002 intranasal administration produced a time-to-maximum concentration (T AV002 demonstrated rapid absorption, high bioavailability, limited duration of action, and low coefficient of variation, suggesting it may be a suitable formulation for nocturia treatment. Trial registration not required (single-center, phase 1).
Identifiants
pubmed: 31037429
doi: 10.1007/s11095-019-2628-1
pii: 10.1007/s11095-019-2628-1
pmc: PMC6488552
doi:
Substances chimiques
Antidiuretic Agents
0
Nasal Sprays
0
Deamino Arginine Vasopressin
ENR1LLB0FP
Types de publication
Clinical Trial, Phase I
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Pagination
92Références
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