Trial reportJournal of translational medicine2015
Gastrointestinal delivery of propofol from fospropofol: its bioavailability and activity in rodents and human volunteers.
Trial report in Journal of translational medicine, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 10 papers.
What it found
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
10 citing papers in PubMed, 14 citations in OpenAlex.
- Chronic Chrysin, but Not Diazepam, Induces Anxiolytic-like Effects Without Behavioral Tolerance.Molecules (Basel, Switzerland) · 2026Article
- Breaking the Limitations of 'Milk': Research Progress on New Derivatives of Propofol.Molecules (Basel, Switzerland) · 2026Review
- Propofol: Current Updates, Challenges, and Strategies for Improved Self-Nanoemulsifying Formulation.ACS pharmacology & translational science · 2025Review
- Novel Prodrug Strategies for the Treatment of Tuberculosis.Chemistry, an Asian journal · 2024Review
- The Development and Optimization of Lipid-Based Self-Nanoemulsifying Drug Delivery Systems for the Intravenous Delivery of Propofol.Molecules (Basel, Switzerland) · 2023Article
- Discovery of Orally Bioavailable and Brain-Penetrable Prodrugs of the Potent nSMase2 Inhibitor DPTIP.Journal of medicinal chemistry · 2022Article
- Structural Modification in Anesthetic Drug Development for Prodrugs and Soft Drugs.Frontiers in pharmacology · 2022Review
- Thiodipeptides targeting the intestinal oligopeptide transporter as a general approach to improving oral drug delivery.European journal of medicinal chemistry · 2018Article
- Neurobiology of Propofol Addiction and Supportive Evidence: What Is the New Development?Brain sciences · 2018Review
- Metabolic Profiles of Propofol and Fospropofol: Clinical and Forensic Interpretative Aspects.BioMed research international · 2018Review
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
6 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
backgroundPropofol is a safe and widely used intravenous anesthetic agent, for which additional clinical uses including treatment of migraine, nausea, pain and anxiety have been proposed (Vasileiou et al. Eur J Pharmacol 605:1-8, 2009). However, propofol suffers from several disadvantages as a therapeutic outside anesthesia including its limited aqueous solubility and negligible oral bioavailability. The purpose of the studies described here was to evaluate, in both animals and human volunteers, whether fospropofol (a water soluble phosphate ester prodrug of propofol) would provide higher propofol bioavailability through non-intravenous routes.
methodsFospropofol was administered via intravenous, oral and intraduodenal routes to rats. Pharmacokinetic and pharmacodynamic parameters were then evaluated. Based on the promising animal data we subsequently conducted an oral and intraduodenal pharmacokinetic/pharmacodynamic study in human volunteers.
resultsIn rats, bioavailability of propofol from fospropofol delivered orally was found to be appreciable, in the order of around 20-70%, depending on dose. Availability was especially marked following fospropofol administration via the intraduodenal route, where bioavailability approximated 100%. Fospropofol itself was not appreciably bioavailable when administered by any route except for intravenous. Pharmacologic effect following oral fospropofol was confirmed by observation of sedation and alleviation of thermal hyperalgesia in the rat chronic constrictive injury model of neuropathic pain. The human data also showed systemic availability of propofol from fospropofol administration via oral routes, a hereto novel finding. Assessment of sedation in human volunteers was correlated with pharmacokinetic measurements.
conclusionsThese data suggest potential utility of oral administration of fospropofol for various therapeutic indications previously considered for propofol.
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