Abstract
Digoxin is one of the most important drugs in clinical therapeutics. Due to narrow therapeutic range, fine dose adjustment is indispensable, especially in pediatric patients, in the aged and in patients with renal failure. In order to dispense the dose more precisely and easily, 0.01% digoxin powder (0.01% powder) was prepared and the pharmaceutical property was examined. The 0.01% digoxin powder was prepared by diluting the commercial 0.1 % digoxin powder preparation with fine lactose. The bioavailability of 0.01% powder was obtained by comparing area under the curve (AUC) after oral administration of the 0.01% powder 5.0g (as digoxin 0.5mg) with AUC after intravenous administration in 4 healthy normal volunteers.
Our data showed the good content uniformity and rapid solubility (91.3% at 60 minutes) of 0.01% powder. The mean peak plasma concentration was 3.19 ng/ml at 41.3 minutes after oral administration. The bioavailability obtained from AUC time 0 through 8 hours and time 0 through 24 hours was 55.3% and 65.1%, respectively. The mean steady state plasma concentration after oral administration of 0.25 mg/day for 10 days did not show any significant difference between the 0.01% powder and a commercially available tablet.
We conclude the 0.01% powder is a safe and effective alternative of current preparations.
