Evaluation of The Food Effect On a Drospirenone Only Contraceptive Containing 4 mg Administered With and Without High-Fat Breakfast
Abstract Background:The objective of the present trial was to assess the difference in pharmacokinetics of an oral test preparation containing 4 mg drospirenone. under fasting conditions compared to food intake after single dose administration.Methods:Open label, single centre, two-treatment, two-sequence, crossover study in 24 healthy female volunteers, with duration of 1 day per sequence and with a real wash-out period of 14 days to investigate the relative bioavailability of DRSP with both forms of administration. The 90% confidence intervals were calculated for the intra-individual ratio (test with food vs. without food) of the pharmacokinetic endpoints AUC(0-72h) and Cmax of drospirenone. Results:The 90% CI calculated by means of ANOVA-log for the endpoint, intra-individual ratio (Test ‘A’ = with food intake) vs. Test ‘B’ = without food intake) of AUC(0-72h) of drospirenone was between 104.72% and 111.36%. The 90% CI calculated by means of ANOVA- log for the endpoint intra-individual ratio (Test ‘A’ vs. Test ‘B’) of Cmax of drospirenone was between 118.58% and 141.10%.The mean relative bioavailability of the Test with food ‘A’ compared to the Test without food ‘B’ after single dose administration based on the endpoints AUC(0-72h) was 107.99%; for the endpoint Cmax it was 129.35%.Conclusions:The rate of absorption, based on the endpoint Cmax of drospirenone was increased by about 30% under fed conditions which differs to a COC containing 0,02 mg EE and 3 mg drospirenone in a 24/4 regimen where the rate of absorption was reduced by about 40% for both components. Implications: Our results suggest that the food intake has no impact on the absorption of 4 mg drospirenone in the management for contraception.This raises up the contraceptive efficacy as no interference with food is expected in real life use when consuming the oral formulation