Comparative pharmacokinetic evaluation of compressed suppositories of diclofenac sodium in humans.
Diclofenac sodium (CAS 15307-79-6) suppositories were formulated using polyethylene glycol 4000 as the base by dispersing the drug in the molten base, congealing the mass, followed by pulverization, sieving and subsequent compression of the resultant granules. These suppositories were evaluated with respect to their pharmacokinetic behaviour in 12 healthy, male human volunteers. The results were compared with those obtained after oral administration of a commercial enteric coated tablet. Bioequivalence between rectal suppositories and commercial tablets was observed with respect to AUC0-infinity and Cmax. However, tmax differed significantly (p < 0.05) in case of rectal administration (0.625 +/- 0.065 h) compared to oral tablet (1.58 +/- 0.06 h). The relative rectal bioavailability was 107.19 +/- 3.2.
Ramakrishna
S
S
Pharmacology Division, Indian Institute of Chemical Technology, Hyderabad, India.
Fadnavis
N W
NW
Diwan
P V
PV
D000284:Administration, Oral; D000285:Administration, Rectal; D000328:Adult; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000008:administration & dosage / Q000493:pharmacokinetics*; D001682:Biological Availability; D004008:Diclofenac / Q000008:administration & dosage* / Q000493:pharmacokinetics*; D006207:Half-Life; D006801:Humans; D008297:Male; D013488:Suppositories; D013810:Therapeutic Equivalency
D000894:Anti-Inflammatory Agents, Non-Steroidal; D013488:Suppositories; D004008:Diclofenac