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 RESEARCH PAPER
Year : 1998  |  Volume : 30  |  Issue : 3  |  Page : 191-194

Comparative pharmacokinetic evaluation of compressed rectal suppositories of diltiazem hydrochloride in rabbits



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Rao P Rama


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Objectives: To evaluate the bioavailability of rectally administered diltiazem hydrochloride in rabbits Methods: Compressed rectal suppositories of diltiazem hydrochloride were formulated employing polyethylene glycol 4000 as base. The bioavailability of diltiazem hydrochloride from rectal suppositories was compared with that of oral administration of same dose of the drug. This study was carried out in a randomized cross over design and various pharmacokinetic parameters were calculated. Results: The maximum serum concentration (Cmax) and area under the curve (AUC0-() were significantly (p<0.05) higher in the case of rectal administration compared to oral administration. However, there was no significant difference in time for peak serum concentration (tmax) and elimination half-life (t1/2) for both rectal and oral route. Conclusions: The relative bioavailability of diltiazem hydrochloride was about 75% greater after rectal administration compared to oral route.This may be due to the avoidance of biotransformation of diltiazem by liver, intestine and lungs.






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