Percutaneous absorption of 2',3'-dideoxyinosine in rats.

摘要: This study explored the topical route for administering of 2′,3′-dideoxyinosine (ddI), a nucleoside analog used treating patients with acquired immunodeficiency syndrome. A dose ddI (∼180 mg/kg) dispersed in ~1 g ointment base was applied, or without occlusion, to back high follicular density (HFD) and low (LFD) rats. The systemic clearance determined using concomitant administration an intravenous tracer [3H]ddI. At 24 hr, experiment terminated skin sections at application site were removed. After application, average plateau plasma levels about 0.6 µg/ml achieved within 1 2 hr maintained hr. Occlusion gave more uniform profile but did not increase bioavailability. bioavailability HFD LFD rats same 33%. In addition, depot 16% recovered by rinsing area extracting drug from excised site. These data indicate that 50% dermal penetrated barrier similar further suggests unimportant role transfollicular absorption ddI. effect mixture penetration enhancers, Azone propylene glycol (5:95), studied Coadministration enhancers However pre-treatment coadministration significantly increased 62%, which is conservative estimate because level still when summary, transdermal exceeded 15% oral found previous studies than 3 folds pretreatment enhancers. as attractive route.