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Year : 1999  |  Volume : 31  |  Issue : 4  |  Page : 294-298

Comparative in-vivo evaluation of diltiazem hydrochloride following oral and transdermal administration in rabbits

Correspondence Address:
Rao P Rama

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Source of Support: None, Conflict of Interest: None

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Objective: To evaluate the in-vivo performance of orally and transdermally delivered diltiazem hydrochloride in rabbits. Methods: Transdermal patches of diltiazem hydrochloride (DLT) were formulated employing ethyl cellulose and polyvinylpyrrolidone as film formers. The pharmacodynamic and pharmacokinetic performance of diltiazem hydrochloride after transdermal administration was compared with that of oral administration. This study was carried out in a randomized cross over design in male New Zealand albino rabbits. Results: The pharmacokinetic parameters such as maximum serum concentration (C max ), time for peak serum concentration (t max ), mean residence time (MRT) and area under the curve (AUC0-() were significantly (p <0.01) different following transdermal administration compared to oral administration. The terminal elimination half life of transdermally delivered diltiazem was found to similar that of oral administration. A sustained therapeutic activity was observed over a study period of 24 hrs after transdermal administration compared to oral administration. The skin irritation studies indicated that there is no recognisable changes on skin surface after the removal of polymeric films. Conclusions: The relative bioavailability of diltiazem hydrochloride and its therapeutic activity were increased about five fold after transdermal administration compared to oral route.


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