Premarin

[Conjugated Estrogens]

TABLE 1. PHARMACOKINETIC PARAMETERS FOR PREMARIN
Pharmacokinetic Profile of Unconjugated Estrogens Following a Dose of 2 x 0.3 mg
PK Parameter
Arithmetic Mean (% CV)
Cmax
(pg/ mL)
tmax
(h)
t1/ 2
(h)
AUC
(pgh/ mL)
Estrone 82 (33) 7.8 (27) 54.7 (42) 5390 (50)
Baseline-adjusted estrone 58 (42) 7.8 (27) 21.1 (45) 1467 (41)
Equilin 31 (47) 7.2 (28) 18.3 (110) 652 (68)

Pharmacokinetic Profile of Conjugated Estrogens Following a Dose of 2 x 0.3 mg
PK Parameter
Arithmetic Mean (% CV)
Cmax
(ng/ mL)
tmax
(h)
t1/ 2
(h)
AUC
(ngh/ mL)
Estrone 2.5 (32) 6.5 (29) 25.4 (22) 61.0 (43)
Baseline-adjusted total estrone 2.4 (32) 6.5 (29) 16.2 (34) 40.8 (36)
Equilin 1.6 (40) 5.9 (27) 11.8 (21) 22.4 (42)

Pharmacokinetic Profile of Unconjugated Estrogens Following a Dose of 2 x 0.45 mg
PK Parameter
Arithmetic Mean (% CV)
Cmax
(pg/ mL)
tmax
(h)
t1/ 2
(h)
AUC
(pgh/ mL)
Estrone 92 (32) 8.7 (28) 56.4 (68) 6344 (56)
Baseline-adjusted estrone 65 (40) 8.7 (28) 20.3 (38) 1940 (40)
Equilin 35 (49) 7.6 (33) 21.9 (113) 849 (60)

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Pharmacokinetic Profile of Conjugated Estrogens Following a Dose of 2 x 0.45 mg
PK Parameter
Arithmetic Mean (% CV)
Cmax
(ng/ mL)
tmax
(h)
t1/ 2
(h)
AUC
(ngh/ mL)
Total estrone 2.8 (46) 7.1 (27) 27.6 (35) 77 (34)
Baseline-adjusted total estrone 2.6 (46) 7.1 (27) 14.7 (42) 48 (38)
Total equilin 1.9 (53) 5.9 (32) 11.8 (32) 29 (55)

Pharmacokinetic Profile of Unconjugated Estrogens Following a Dose of 2 x 0.625 mg
PK Parameter
Arithmetic Mean (% CV)
Cmax
(pg/ mL)
tmax
(h)
t1/ 2
(h)
AUC
(pgh/ mL)
Estrone 139 (37) 8.8 (20) 28.0 (30) 5016 (34)
Baseline-adjusted estrone 120 (41) 8.8 (20) 17.4 (37) 2956 (39)
Equilin 66 (42) 7.9 (19) 13.6 (52) 1210 (37)

Pharmacokinetic Profile of Conjugated Estrogens Following a Dose of 2 x 0.625 mg
PK Parameter
Arithmetic Mean (% CV)
Cmax
(ng/ mL)
tmax
(h)
t1/ 2
(h)
AUC
(ngh/ mL)
Total estrone 7.3 (41) 7.3 (24) 15.0 (25) 134 (42)
Baseline-adjusted total estrone 7.1 (41) 7.3 (24) 13.6 (23) 122 (38)
Total equilin 5.0 (42) 6.2 (26) 10.1 (26) 65 (44)

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