Pharmaceutical composition containing a tetrahydrofolic acid
AssigneeBayer Intellectual Property GmbH
InventorKristina King
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Abstract
The present invention relates to solid pharmaceutical compositions, in particular to oral contraceptives, comprising a progestogen, such as drospirenone; an estrogen, such as ethinylestradiol; a tetrahydrofolic acid or a pharmaceutically acceptable salt thereof, such as calcium 5-methyl-(6S)-tetrahydrofolate; and at least one pharmaceutical acceptable excipient or carrier. The compositions of the invention provide good stability of the tetrahydrofolic acid upon storage while still ensuring a fast and reliable release of the estrogen and the progestogen present in the composition.
Claims11
A tablet core comprising a solid pharmaceutical composition comprising,
- particles comprising 3 mg of micronized drospirenone, 0.02 or 0.03 mg of ethinyl estradiol, 25-36 wt % (based on tablet core total weight) of microcrystalline cellulose, 52-63 wt % (based on tablet core total weight) of lactose monohydrate, and 0.42-0.49 mg of an alkaline earth metal salt of 5-methyl-(6S)-tetrahydrofolic acid,
- wherein the in vitro dissolutions of drospirenone and the salt of 5-methyl-(6S)-tetrahydrofolic acid individually are such that at least 85% of each is dissolved from the composition within 30 minutes, as determined by the USP XXIX Paddle Method II using water (for drospirenone) and a 0.03% ascorbic acid aqueous solution (adjusted to pH 3.5 with 0.05 M phosphate buffer (for the salt of 5-methyl-(6S)-tetrahydrofolic acid) at 37° C. as the dissolution media and 50 rpm as the stirring rate, and
- wherein the stability of the salt of 5-methyl-(6S)-tetrahydrofolic acid is such that at least 90% of said amount thereof is present in the composition after storage in a closed container for 12 months at 25° C. and 60% relative humidity.
Dependencies are inferred from the claim text.