Document Detail


The effects of physiocochemical properties of pethidine and its basic metabolites on their buccal absorption and renal elimination.
MedLine Citation:
PMID:  41039     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
The pKa values, RF values, partition coefficients between n-heptane and phosphate buffer (pH = 7.4), and buccal absorption tests of pethidine and its basic metabolites, norpethidine and pethidine N-oxide, have been determined. The amounts of these compounds recovered in the 48 h urine samples after intramuscular administration of pethidine (1.5 mg kg-1) to six healthy subjects varies with urinary pH values: the recovery from acidic urine (pH 5.0) is 15.2 to 52.0%, 6.7 to 12.9% and 0.2 to 2.3% of dose for pethidine, norpethidine and pethidine N-oxide respectively; in alkaline urine (pH 8.0) the values are 0.8 to 1.8%, 0.6 to 2.8% and 0.3 to 2.1% respectively. The physicochemical properties (pKa values, RF values, partition coefficients) and buccal absorption of pethidine, norpethidine and pethidine N-oxide are in good agreement with the pattern of their renal elimination in acidic and alkaline urine conditions. The contribution of the physiocochemical properties of pethidine and its metabolites to the drug's disposition in the body and the effect of urinary pH on its metabolism should be taken into account in pharmacokinetic studies and interpretation of intersubject variation in response to pethidine.
Authors:
K Chan
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Publication Detail:
Type:  Journal Article    
Journal Detail:
Title:  The Journal of pharmacy and pharmacology     Volume:  31     ISSN:  0022-3573     ISO Abbreviation:  J. Pharm. Pharmacol.     Publication Date:  1979 Oct 
Date Detail:
Created Date:  1980-01-28     Completed Date:  1980-01-28     Revised Date:  2008-11-21    
Medline Journal Info:
Nlm Unique ID:  0376363     Medline TA:  J Pharm Pharmacol     Country:  ENGLAND    
Other Details:
Languages:  eng     Pagination:  672-5     Citation Subset:  IM    
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MeSH Terms
Descriptor/Qualifier:
Absorption
Adult
Biotransformation
Cheek
Chemistry, Physical
Humans
Male
Meperidine / metabolism*,  urine
Middle Aged
Mouth Mucosa / metabolism*
Physicochemical Phenomena
Chemical
Reg. No./Substance:
57-42-1/Meperidine

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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