Document Detail


Influence of formulation on the pharmacokinetics and bioavailability of racemic ketoprofen in horses.
MedLine Citation:
PMID:  8789698     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
The bioavailability of S(+) and R(-) ketoprofen (KTP) in six horses was investigated after oral administration of the racemic (rac) mixture. Two oral formulations were studied, an oil-based paste containing micronised rac-KTP and powder from the same source in hard gelatin capsules, each at a dose rate of 2.2 mg/kg. For the oil-based paste two feeding schedules were used; horses were either allowed free access to food or access to food was restricted for 4 h before and 5 h after dosing. The drug in hard gelatin capsules was administered to horses with restricted access to food. After intravenous administration of rac-KTP, S(+) enantiomer concentrations exceeded those of the R(-) enantiomer. For S(+) and R(-)KTP, respectively, pharmacokinetic parameters were, t1/2 beta 0.99 +/- 0.14 h, 0.70 +/- 0.13 h; ClB 0.56 +/- 0.09, 0.92 +/- 0.20 L/h/kg; Vd(ss) 0.53 +/- 0.11, 0.61 +/- 0.10 L/kg. Following oral administration of rac-KTP as the oil-based paste to horses with free access to food, there were no detectable concentrations in plasma in three animals at any sampling time, while a fourth animal showed very low concentrations at two sampling times only. In the two remaining horses very low but detectable concentrations were present for 5 h. In the horses with restricted access to food, rac-KTP paste administration produced higher concentrations in plasma. However, bioavailability was very low, 2.67 +/- 0.43 and 5.75 +/- 1.48% for R(-) and S(+)KTP, respectively. When administered as pure drug substance in hard gelatin capsules, absorption of KTP was fairly rapid, but incomplete. Bioavailability was 50.55 +/- 10.95 and 54.17 +/- 9.9% for R(-) and S(+)KTP, respectively. This study demonstrates that rac-KTP had a modest bioavailability when administered as a micronised powder in hard gelatin capsules to horses with restricted access to food. When powder from the same source was administered as an oil-based paste, it was for practical purposes not bioavailable, regardless on the feeding schedule.
Authors:
M F Landoni; P Lees
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Publication Detail:
Type:  Clinical Trial; Controlled Clinical Trial; Journal Article; Research Support, Non-U.S. Gov't    
Journal Detail:
Title:  Journal of veterinary pharmacology and therapeutics     Volume:  18     ISSN:  0140-7783     ISO Abbreviation:  J. Vet. Pharmacol. Ther.     Publication Date:  1995 Dec 
Date Detail:
Created Date:  1996-10-22     Completed Date:  1996-10-22     Revised Date:  2006-11-15    
Medline Journal Info:
Nlm Unique ID:  7910920     Medline TA:  J Vet Pharmacol Ther     Country:  ENGLAND    
Other Details:
Languages:  eng     Pagination:  446-50     Citation Subset:  IM    
Affiliation:
Department of Veterinary Basic Sciences, Royal Veterinary College, Hatfield Herts, United Kingdom.
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MeSH Terms
Descriptor/Qualifier:
Administration, Oral
Animals
Anti-Inflammatory Agents, Non-Steroidal / administration & dosage,  blood,  pharmacokinetics*,  pharmacology
Biological Availability
Capsules
Chromatography, High Pressure Liquid / veterinary
Cross-Over Studies
Drug Delivery Systems
Female
Food Deprivation
Horses / metabolism*
Injections, Intravenous / veterinary
Intestinal Absorption / drug effects
Ketoprofen / administration & dosage,  blood,  pharmacokinetics*,  pharmacology
Male
Ointments
Stereoisomerism
Chemical
Reg. No./Substance:
0/Anti-Inflammatory Agents, Non-Steroidal; 0/Capsules; 0/Ointments; 22071-15-4/Ketoprofen

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


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