RESUMEN
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.
RESUMEN
The transport of cephalothin (CET) to the exudate was investigated in croton oil-induced inflammatory rats following the intramuscular administration of CET-aqueous solution, CEt-O/W emulsion, or CET-W/O emulsion. The lymphatic transport of CET was the highest following the administration of W/O emulsion. The exudate level of CET was in a decreasing order of W/O emulsion, O/W emulsion, and aqueous solution. In the rat whose blood vessels at femoral rectus, the site of administration, were ligated, the plasma level was decreased by the administration of aqueous solution, but not by W/O emulsion. The exudate level of CET was significantly higher in case of W/O emulsion. Possible mechanisms involved are discussed.