Objective: To determine the relative bioavailability of @entity2082 (EE) and @entity2081 ( @entity5202 ) after application of a novel transdermal contraceptive patch vs. a a standard combined oral contraceptive (COC) pill (study 1), and to evaluate the pharmacokinetics (PK) of EE after application of the @entity5202 compared with an EE/ @entity26169 (NGMN) patch (study 2). Materials: @entity1 were healthy, nonobese @entity1 aged 18 - 45 years (study 1) or 18 - 35 years (study 2). Compositions of study treatments were as follows: 0.55 mg EE/2.1 mg @entity5202 ( @entity5202 ); 0.02 mg EE/0.075 mg @entity5202 (standard COC); 0.6 mg EE/6 mg NGMN (EE/NGMN patch). Methods: In study 1, which consisted of 3 treatment periods (each followed by 7 patch- or pill-free days), treatments were administered in one of two randomized orders: either @entity27300 ( @entity5202 (P) every 7 days for 28 days  >  @entity11718 (M) once-daily for 21 days  >  two 7-day patch-wearing periods followed by one 10-day patch-wearing phase (E)), or the same treatments administered in sequence M-P-E. For study 2, @entity1 received either the @entity5202 or EE/ NGMN patch for seven treatment cycles (one patch per week for 3 weeks followed by a 7-day patch-free interval). Results: In study 1, average daily exposure to EE was similar for treatments P and M; the mean daily area under the concentration-time curve (AUC) ratio of treatment P vs. treatment M for EE was 1.06 (90% confidence interval (CI): 0.964 - 1.16), indicating average daily delivery similar to oral administration of 0.019 - 0.023 mg EE. For unbound @entity5202 , average daily exposure was lower for treatment P vs. treatment M. The mean AUC ratio of treatment P vs. treatment M for unbound @entity5202 was 0.820 (90% CI: 0.760 - 0.885), indicating average daily delivery from the patch of 0.057 - 0.066 mg @entity5202 . Prolonged patch wearing did not result in a distinct decline in @entity5202 and EE serum concentrations. In study 2, AUC at steady state (AUC0-168,ss), average steady-state serum concentration, and maximum steady-state serum concentration for EE was 2.0 - 2.7-fold higher for the EE/NGMN patch vs. the @entity5202 . The @entity5202 was well tolerated in both studies. Conclusions: Based on the 90% CI of the AUC ratio of oral treatment vs. patch application for unbound @entity5202 and EE, the daily doses of @entity5202 and EE released from the @entity5202 over the 7-day application period provided the same systemic exposure as those recorded after daily oral administration of a COC containing 0.02 mg EE and 0.06 mg @entity5202 . The @entity5202 showed reduced EE exposure compared with the EE/NGMN patch. Together with its good tolerability, these properties support the @entity5202 as an effective and well-tolerated alternative to available transdermal and oral contraceptives.

Pharmacokinetic overview of XXXX dose and bioavailability using two transdermal contraceptive systems and a standard combined oral contraceptive.

@entity1 :: ('9606', 'Species') :: ['participants', 'women', 'Participants'] @entity2081 :: ('MESH:C033273', 'Chemical') :: ['gestodene'] @entity5202 :: ('MESH:D057765', 'Disease') :: ['EE/GSD patch', 'GSD'] @entity11718 :: ('CHEBI:28887', 'Chemical') :: ['COC'] @entity2082 :: ('MESH:D004997', 'Chemical') :: ['ethinyl estradiol'] @entity27300 :: ('1476', 'Gene') :: ['P-M-E'] @entity26169 :: ('MESH:C449219', 'Chemical') :: ['norelgestromin']
@entity2082 :: (MESH:D004997,Chemical) :: ['ethinyl estradiol']
