Synthetic progestogens and pharmaceutical compositions comprising the same
Described herein are synthetic progestogens, such as 6β,7β:15β,16β-Dimethylene-3-oxo-17α-pregn-4-ene-21,17-carbolactone, as well as pharmaceutical compositions comprising the same. Also described are methods of use.
1. A method of providing effective contraception in a female patient, the method comprising:
orally administering to the patient a daily pharmaceutical composition for 24 consecutive days, followed by orally administering to the patient a daily placebo dosage unit for 4 consecutive days,
wherein the pharmaceutical composition comprises from 2 mg to 6 mg drospirenone and is formulated such that:
(1) when orally administered under fasting conditions, the pharmaceutical composition provides a pharmacokinetic profile for the drospirenone comprising:
(i) a mean T max ranging from 2.2 hours to 6 hours;
(ii) a mean C max which is less than 30 ng/ml; and
(iii) a mean AUC 0h-tlast of at least 300 ng*h/ml; and
(2) no more than 50% of the drospirenone initially present in the pharmaceutical composition is dissolved within 30 minutes if subjected to an in vitro dissolution test according to the USP XXIII Paddle Method; and
wherein the pharmaceutical composition does not comprise estrogen.
2. The method of claim 1 , wherein the mean T max ranges from 3 hours to 4 hours.
3. The method of claim 1 , wherein the mean C max ranges from 15 ng/ml to less than 30 ng/ml.
4. The method of claim 1 , wherein the mean AUC 0h-tlast is at least 350 ng*h/ml.
5. The method of claim 1 , wherein the pharmaceutical composition is formulated such that at least 55% of the drospirenone initially present in the pharmaceutical composition is dissolved within 4 hours if subjected to the in vitro dissolution test according to the USP XXIII Paddle Method.
6. The method of claim 1 , wherein the amount of the drospirenone present is 3.5 mg.
7. The method of claim 1 , wherein the amount of the drospirenone present is 4.0 mg.
8. The method of claim 1 , wherein the amount of the drospirenone present ranges from 3.0 mg to 4.5 mg.
9. The method of claim 1 , wherein the amount of the drospirenone present ranges from 3.0 mg to 3.5 mg.
10. The method of claim 1 , wherein the amount of the drospirenone present ranges from 3.5 mg to 4.5 mg.