Lg. Gisclon et al., Bioequivalence of a newly developed 17 beta-estradiol tablet versus an identical reference formulation, ARZNEI-FOR, 50(10), 2000, pp. 910-914
Two open-label, randomized studies determined the bioequivalence of a test
preparation (Prefest(TM)) of micronized 17 beta -estradiol (E-2, CAS 50-28-
2) tablets as compared with a reference preparation of micronized E-2 table
ts in healthy postmenopausal women. In Study 1, 36 fasting subjects receive
d 4 test preparation 0.5-mg E-2 tablets in one period and 4 reference prepa
ration 0.5-mg E-2 tablets in the other period. In Study 2, 36 fasting subje
cts received 1 test preparation 3-mg E-2 tablet in one period and 1 referen
ce preparation 2-mg E-2 tablet in the other period. Blood samples were coll
ected before and after dosing to determine serum concentrations of E-2, est
rone, and estrone sulfate. The 90% confidence intervals for the ratios of m
ean C-max and AUC values (test preparation/reference preparation) for all t
hree analytes were within the prescribed 80%-125% range of bioequivalence.
In conclusion, the test preparation 0.5-mg and 2-mg micronized E-2 tablets
are bioequivalent to the respective strength reference preparation microniz
ed E-2 tablets.