|
In the year 1990, the Food and Drugs Administration-FDA of the
United States has formally released the approval of branded medicine
named Diflucan manufactured by the world’s largest pharmaceutical
corporation called Pfizer Inc of the United States. The drug has
been formulated by using Fluconazole as the active pharmaceutical
ingredient. The drug is the first of the latest subclass of
synthetic Triazole anti-fungal agents which is produced in the
tablet form for oral ingest, in the powder form for oral suspension
usage and in the sterile solution for intravenous administration in
glass and plastic containers. The drug is basically chemically
designated as 2, 4-difluoro- α, α1-bis (1H-1, 2,
4-triazole-1-ylmethyl) benzyl alcohol with the empirical formula of
C13H12F2N6O and molecular weight 306.3.
It is the highly selective inhibitor of fungal cytochrome P-450
sterol C-14 alpha-demethylation which is the mammal cell much less
sensitive to Fluconazole inhibition. The pharmacokinetic properties
of Diflucan-Fluconazole are similar following administration by the
intravenous or oral dose routes. In usual volunteers, the
bioavailability of orally given Diflucan-Fluconazole is more than 90
percent as compared to intravenous administration. Bioequivalence
was established between 100mg tablet and both suspension strengths
when administered as the single 300mg dose.
Peak plasma concentrations-Cmax fasted normal participants occur
between 1 and 2 hours with incurable plasma removal half-life of
nearly 30 hours after oral administration. In the fasted general
participants giving of single oral dose of 400mg of
Diflucan-Fluconazole led to the mean Cmax of 6.72µg/mL and after
single oral dose of 50-400mg, Fluconazole plasma concentrations and
area under plasma concentration-time curve are dose proportional.
|
