The authors reported the plasma levels and pharmacokinetic parameters of ciclopirox olamine in rabbits after i.v. and intravaginal administrations and in female patients after vaginal administration. Plasma levels of total and free ciclopirox were determined by a HPLC method. In rabbit ciclopirox showed a half-life of 2.22 h and an intravaginal bioavailability of about 2%. In female patients ciclopirox showed low intravaginal absorption; this value might explain the good local and systemic tolerability and also the penetration of drug in deep tissue.
A new ciclopirox olamine vaginal preparation was tested for toxicity after topical vaginal administration for 28 days to rats and rabbits. At the end of the experiments animals were sacrificed for autopsy, the main organs were weighed, hematological, coagulative and biochemical parameters were checked and histological examinations were performed on uterus and vagina. The results demonstrated the good topical and systemic tolerance of this new vaginal formulation in rats and rabbits.
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