Absorption and bioavailability of diclofenac after rectal administration of diclofenac-Na gel preparation in rat and man

In order to evaluate diclofenac-Na (DC-Na) micro-enema, DC-Na gel preparations were administered to rats and man. When DC-Na gel preparations were rectally administered at various pH (pH 5- 8) to rats, their bioavailability increased at higher pH. The bioavailability of DC-Na gel preparations (pH 8....

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Bibliographic Details
Published in:Pharmaceutical research 1985-07, Vol.2 (4), p.166-170
Main Authors: MORIMOTO, K, IWAMOTO, Y, KATASHIMA, T, TAKEEDA, Y, NAKAMOTO, Y, MORISAKA, K
Format: Article
Language:English
Subjects:
Biological and medical sciences
General pharmacology
Medical sciences
Pharmacokinetics. Pharmacogenetics. Drug-receptor interactions
Pharmacology. Drug treatments
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Summary:In order to evaluate diclofenac-Na (DC-Na) micro-enema, DC-Na gel preparations were administered to rats and man. When DC-Na gel preparations were rectally administered at various pH (pH 5- 8) to rats, their bioavailability increased at higher pH. The bioavailability of DC-Na gel preparations (pH 8.0) in rats was significantly higher than that with conventional suppository bases, Witepsol H-15 and polyethylene glycol 1000 (PEG 1000). In man, the DC-Na gel preparation showed higher Cmax and higher bioavailability than commercial suppository made with an oily base. DC-Na gel preparations containing 10% v/v oleic acid showed a prolonged action. The irritative effect of DC-Na gel preparation on rectal mucosa in rats was weaker than that of PEG 1000, but similar to that of Witepsol H-15. Therefore, the present results suggest that gel preparation is a favorable form for rectal administration of diclofenac-Na.
ISSN:0724-8741
1573-904X
DOI:10.1023/A:1016383921320