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

The nasal spray did not increase doxylamine absorption or systemic bioavailability compared with the oral tablet, and changes from baseline in psychomotor parameters did not show a relationship to intranasal dose, and did not distinguish between intran asal versus oral dosing.

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.

Intranasal delivery of systemic-acting drugs: small-molecules and biomacromolecules.


A high pressure liquid chromatography-diode array detector (HPLC-DAD) method using amylose tris(3,5-dimethylphenyl carbamate) chiral stationary phase (Chiralpak AD-H) is described for the

Insomnia in general practice: the role of doxylamine

A portrait of doxylamine is presented and comments on its clinical niches and contraindications, and the pharmacology of doXYlamine, drug interactions, and prescription modes are discussed.

Iodine-Promoted Controlled and Selective Oxidation of (Aryl)(Heteroaryl)Methanes.

An iodine-catalyzed controlled oxidation of aryl heteroaryl methanol derivatives is disclosed under metal-free reaction conditions and the preliminary mechanistic investigation proves that the primary source of oxygen is DMSO.



Pharmacokinetics of midazolam in children: comparative study of intranasal and intravenous administration

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%.

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.

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.

The Intranasal Absorption of the Quaternary Ammonium Compounds Neostigmine Bromide and Tubocurarine Chloride in the Rat

Differences in the rate and extent of absorption of the quaternary ammonium compounds across the nasal mucosa appeared to reflect differences in molecular weight.

Bioavailability of nafarelin in healthy volunteers.

  • M. Chaplin
  • Medicine, Biology
    American journal of obstetrics and gynecology
  • 1992

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.

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.