Comparative pharmacokinetics of single doses of doxylamine succinate following intranasal, oral and intravenous administration in rats

  title={Comparative pharmacokinetics of single doses of doxylamine succinate following intranasal, oral and intravenous administration in rats},
  author={Andries Pelser and Douw G M{\"u}ller and Jeanetta du Plessis and Jan L. du Preez and Colleen Goosen},
  journal={Biopharmaceutics \& Drug Disposition},
The intranasal route of administration provides a potential useful way of administering a range of systemic drugs. In order to assess the feasibility of this approach for the treatment of nausea and vomiting, doxylamine succinate was studied in rats for the pharmacokinetics (AUC, Cmax, tmax) following intranasal, oral and intravenous administrations. 
A Phase I Study of the Pharmacokinetics and Pharmacodynamics of Intranasal Doxylamine in Subjects with Chronic Intermittent Sleep Impairment
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Bioavailability of Δ9-tetrahydrocannabinol following intranasal administration of a mucoadhesive gel spray delivery system in conscious rabbits
The results of the present study suggest that intranasal administration of THC in solution or in a chitosan-based nasal gel formulation could be an attractive modality for delivery of THC systemically. Expand
Intranasal absorption of Δ9-tetrahydrocannabinol and WIN55,212-2 mesylate in rats
Abstract The aim of this study was to examine the potential of the nasal route for systemic delivery of Δ9-tetrahydrocannabinol (Δ9-THC) and WIN55,212-2 mesylate. Anesthetized rats were surgicallyExpand
Intranasal delivery of systemic-acting drugs: small-molecules and biomacromolecules.
An anatomical, histological and mechanistic overview of drug systemic absorption after nasal administration and the relevant aspects of the therapeutic interest and limitations of the intranasal systemic delivery are provided. Expand
Simultaneous determination of dextromethorphan, dextrorphan and doxylamine in human plasma by HPLC coupled to electrospray ionization tandem mass spectrometry: application to a pharmacokinetic study.
The analytical procedure herein described was used to assess the pharmacokinetics of dextromethorphan, dextrorphan and doxylamine in healthy volunteers after a single oral dose of a formulation containing 30 mg of dexfinity hydrobromide and 12.5mg of doxyamine succinate. Expand
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The general practitioner encounters all three forms of insomnia: idiopathic, chronic and acute. Idiopathic and chronic patients should receive specialized care by neurologist, psychiatrist or sleepExpand
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The cooperative effect of Lewis pairs in the Friedel-Crafts hydroxyalkylation reaction: a simple and effective route for the synthesis of (±)-carbinoxamine.
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Metal-Free Halogen(I) Catalysts for the Oxidation of Aryl(heteroaryl)methanes to Ketones or Esters: Selectivity Control by Halogen Bonding.
With the help of a selectivity study, for the first time, the strength of the XB interaction and the frontier orbital mixing between the substrates and acyl hypoiodites determined the extent of the background electron-transfer process and, thus, the selectivity of the reaction. Expand


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Children randomly assigned to receive midazolam 0.2 mg·kg−1 either by the intravenous (IV) or intranasal (IN) routes showed consistent with an estimated mean bioavailability of 55%. Expand
Nasal absorption of propranolol from different dosage forms by rats and dogs.
The blood levels of propranolol in rats and dogs were compared after the administration of nasal, intravenous, and oral solutions, and the bioavailability of the sustained-release formulation was identical to that of the intravenous administration. Expand
Pharmacokinetics and Pharmacodynamics of Midazolam After Intranasal Administration
After in tranasal administration, midazolam concentrations rapidly achieve values considered sufficient to induce conscious sedation and produce predictable changes in digit symbol substitution score. Expand
The Intranasal Absorption of the Quaternary Ammonium Compounds Neostigmine Bromide and Tubocurarine Chloride in the Rat
AbstractThe systemic absorptions of the quaternary ammonium compounds, neostigmine bromide and (+)-tubocurarine chloride, from the nasal cavity were compared in the adult male rat with those obtainedExpand
Pharmacokinetics of intranasal alfentanil.
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Bioavailability of nafarelin in healthy volunteers.
  • M. Chaplin
  • Medicine
  • American journal of obstetrics and gynecology
  • 1992
Nafarelin's bioavailability is adequate to achieve the desired therapeutic effect because of its inherent high biologic potency and its pharmacokinetic properties. Expand
Nasal delivery of progestational steroids in ovariectomized rabbits: I. progesterone — comparison of pharmacokinetics with intravenous and oral administration
The nasal device was observed to achieve a more prolonged and elevated plasma level of progesterone than the other routes of administration and to compare the effect of immediate and controlled drug release on nasal bioavailability of drugs. Expand
Clearance of the Antihistamine Doxylamine
The reduced doxylamine clearance and prolonged half-life in elderly men, but not in elderly women, is similar to results for many other drugs which are transformed by oxidation. Expand
The interaction potential of vigabatrin with phenytoin and carbamazepine
Abstract The effect of vigabatrin on the pharmacokinetic profiles of orally coadministered doses of phenytoin (PT) and carbamazepine (CBZ) was examined in the rat. Plasma PT and CBZ levels wereExpand
The Nasal Mucociliary Clearance: Relevance to Nasal Drug Delivery
The mucociliary system and the methods used for its characterization are described and possible approaches for increasing the residence time of drugs in the nasal cavity, thereby improving intranasal drug delivery are presented. Expand