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Text
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<a href="http://doi.org/10.1038/clpt.1988.159" target="_blank" rel="noreferrer">http://doi.org/10.1038/clpt.1988.159</a>
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Title
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Sublingual absorption of selected opioid analgesics
Publisher
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Clinical Pharmacology And Therapeutics
Date
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1988
Subject
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Humans; Adult; Analgesics; Time Factors; Analysis of Variance; Non-U.S. Gov't; P.H.S.; Research Support; U.S. Gov't; Comparative Study; Administration; Biological Availability; Buprenorphine/pharmacokinetics; Fentanyl/pharmacokinetics; Heroin/pharmacokinetics; Hydromorphone/pharmacokinetics; Levorphanol/pharmacokinetics; Methadone/pharmacokinetics; Morphine/blood/pharmacokinetics; Mouth/metabolism; Naloxone/pharmacokinetics; Opioid/administration & dosage/pharmacokinetics; Oxycodone/pharmacokinetics; Sublingual
Creator
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Weinberg DS; Inturrisi CE; Reidenberg B; Moulin DE; Nip TJ; Wallenstein S; Houde RW; Foley KM
Description
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Ongoing interest in the improvement of pain management with opioid analgesics had led to the investigation of sublingual opioid absorption. The present report determined the percent absorption of selected opioid analgesics from the oral cavity of normal subjects under conditions of controlled pH and swallowing when a 1.0 ml aliquot of the test drug was placed under the tongue for a 10-minute period. Compared with morphine sulfate at pH 6.5 (18% absorption), buprenorphine (55%), fentanyl (51%), and methadone (34%) were absorbed to a significantly greater extent (p less than 0.05), whereas levorphanol, hydromorphone, oxycodone, heroin, and the opioid antagonist naloxone were not. Overall, lipophilic drugs were better absorbed than were hydrophilic drugs. Plasma morphine concentration-time profiles indicate that the apparent sublingual bioavailability of morphine is only 9.0% +/- 11.9% (SD) of that after intramuscular administration. In the same subjects the estimated sublingual absorption was 22.4% +/- 9.2% (SD), indicating that the sublingual absorption method may overestimate apparent bioavailability. When the oral cavity was buffered to pH 8.5, methadone absorption was increased to 75%. Thus, an alkaline pH microenvironment that favors the unionized fraction of opioids increased sublingual drug absorption. Although absorption was found to be independent of drug concentration, it was contact time dependent for methadone and fentanyl but not for buprenorphine. These results indicate that although the sublingual absorption and apparent sublingual bioavailability of morphine are poor, the sublingual absorption of methadone, fentanyl, and buprenorphine under controlled conditions is relatively high.
1988
Identifier
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<a href="http://doi.org/10.1038/clpt.1988.159" target="_blank" rel="noreferrer">10.1038/clpt.1988.159</a>
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Article information provided for research and reference use only. PedPalASCNET does not hold any rights over the resource listed here. All rights are retained by the journal listed under publisher and/or the creator(s).
Type
The nature or genre of the resource
Journal Article
1988
Administration
Adult
Analgesics
Analysis of Variance
Backlog
Biological Availability
Buprenorphine/pharmacokinetics
Clinical Pharmacology And Therapeutics
Comparative Study
Fentanyl/pharmacokinetics
Foley KM
Heroin/pharmacokinetics
Houde RW
Humans
Hydromorphone/pharmacokinetics
Inturrisi CE
Journal Article
Levorphanol/pharmacokinetics
Methadone/pharmacokinetics
Morphine/blood/pharmacokinetics
Moulin DE
Mouth/metabolism
Naloxone/pharmacokinetics
Nip TJ
Non-U.S. Gov't
Opioid/administration & dosage/pharmacokinetics
Oxycodone/pharmacokinetics
P.H.S.
Reidenberg B
Research Support
Sublingual
Time Factors
U.S. Gov't
Wallenstein S
Weinberg DS