OCELLA

OCELLA — drospirenone and ethinyl estradiol
Physicians Total Care, Inc.

PHYSICIAN LABELIN G

Rx only

PATIENTS SHOULD BE COUNSELED THAT THIS PRODUCT DOES NOT PROTECT AGAINST HIV INFECTION (AIDS) AND OTHER SEXUALLY TRANSMITTED DISEASES.

Description

OCELLA provides an oral contraceptive regimen consisting of 21 active film coated tablets each containing 3 mg of drospirenone and 0.03 mg of ethinyl estradiol and 7 inert film coated tablets. The inactive ingredients are lactose monohydrate NF, corn starch NF, modified starch NF, povidone 25000 USP, magnesium stearate NF, hydroxylpropylmethyl cellulose USP, macrogol 6000 NF, talc USP, titanium dioxide USP, ferric oxide pigment, yellow NF. The inert film coated tablets contain lactose monohydrate NF, corn starch NF, povidone 25000 USP, magnesium stearate NF, hydroxylpropylmethyl cellulose USP, talc USP, titanium dioxide USP.

Drospirenone (6R,7R,8R,9S,10R,13S,14S,15S,16S,17S)-1,3′,4′,6,6a,7,8,9,10,11,12,13, 14,15,15a,16-hexadecahydro-10,13-dimethylspiro-[17H-dicyclopropa-6,7:15,16] cyclopenta[ a]phenanthrene-17,2′(5H)-furan]-3,5′(2H)-dione) is a synthetic progestational compound and has a molecular weight of 366.5 and a molecular formula of C24 H30 O3 . Ethinyl estradiol (19-nor-17α-pregna 1,3,5(10)-triene-20-yne-3,17-diol) is a synthetic estrogenic compound and has a molecular weight of 296.4 and a molecular formula of C20 H24 O2 . The structural formulas are as follows:

Structural Formula
(click image for full-size original)

CLINICAL PHARMACOLOGY

PHARMACODYNAMICS

Combination oral contraceptives (COCs) act by suppression of gonadotropins. Although the primary mechanism of this action is inhibition of ovulation, other alterations include changes in the cervical mucus (which increases the difficulty of sperm entry into the uterus) and the endometrium (which reduces the likelihood of implantation).

Drospirenone is a spironolactone analogue with antimineralocorticoid activity. Preclinical studies in animals and in vitro have shown that drospirenone has no androgenic, estrogenic, glucocorticoid, and antiglucocorticoid activity. Preclinical studies in animals have also shown that drospirenone has antiandrogenic activity.

PHARMACOKINETICS

Absorption

The absolute bioavailability of drospirenone (DRSP) from a single entity tablet is about 76%. The absolute bioavailability of ethinyl estradiol (EE) is approximately 40% as a result of presystemic conjugation and first-pass metabolism. The absolute bioavailability of OCELLA which is a combination tablet of drospirenone and ethinyl estradiol has not been evaluated. Serum concentrations of DRSP and EE reached peak levels within 1–3 hours after administration of OCELLA. After single dose administration of OCELLA , the relative bioavailability, compared to a suspension, was 107% and 117% for DRSP and EE, respectively.

The pharmacokinetics of DRSP are dose proportional following single doses ranging from 1–10 mg. Following daily dosing of OCELLA , steady state DRSP concentrations were observed after 10 days. There was about 2 to 3 fold accumulation in serum Cmax and AUC (0–24h) values of DRSP following multiple dose administration of OCELLA (see TABLE I).

For EE, steady-state conditions are reported during the second half of a treatment cycle. Following daily administration of OCELLA serum Cmax and AUC(0–24h) values of EE accumulate by a factor of about 1.5 to 2.

TABLE I TABLE OF MEAN PHARMACOKINETIC PARAMETERS OF OCELLA (Drospirenone 3 mg and Ethinyl Estradiol 0.03 mg )
*
NA = Not available

Drospirenone

Mean (%CV) Values

Cycle /

Day

No. of

Subjects

Cmax

(ng/mL)

T max

(h)

AUC(0–24h)

(ng•h/mL)

t1/2

(h)
1/1 12 36.9 (13) 1.7 (47) 288 (25) NA *
1/21 12 87.5 (59) 1.7 (20) 827 (23) 30.9 (44)
6/21 12 84.2 (19) 1.8 (19) 930 (19) 32.5 (38)
9/21 12 81.3 (19) 1.6 (38) 957 (23) 31.4 (39)
13/21 12 78.7 (18) 1.6 (26) 968 (24) 31.1 (36)

Ethinyl Estradiol

Mean (%CV) Values

Cycle /

Day

No. of

Subjects

Cmax

(pg/mL)

Tmax

(h)

AUC(0–24h)

(pg•h/mL)

t1/2

(h)
1/1 11 53.5 (43) 1.9 (45) 280.3 (87) NA *
1/21 11 92.1 (35) 1.5 (40) 461.3 (94) NA *
6/21 11 99.1 (45) 1.5 (47) 346.4 (74) NA *
9/21 11 87 (43) 1.5 (42) 485.3 (92) NA *
13/21 10 90.5 (45) 1.6 (38) 469.5 (83) NA *
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