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|Title:||Pharmaceutical composition containing a tetrahydrofolic acid|
|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.|
|Inventor(s):||King; Kristina (Berlin, DE)|
|Assignee:||Bayer Intellectual Property GmbH (Monheim, DE)|
1. 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.degree. 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.degree. C. and 60% relative humidity.
2. The tablet according to claim 1, wherein the ethinyl estradiol is in the form of an estrogen-.beta.-cyclodextrin complex.
3. The tablet according to claim 1, wherein the ethinyl estradiol is micronized.
4. The tablet according to claim 1, wherein the estrogen-.beta.-cyclodextrin complex is micronized.
5. The tablet according to claim 1, wherein the salt of 5-methyl-(6S)-tetrahydrofolic acid is the calcium salt.
6. The tablet according to claim 5, wherein the calcium salt of 5-methyl-(6S)-tetrahydrofolic acid is in crystalline form.
7. The tablet according to claim 6, wherein the crystalline form is the Type I crystalline form.
8. The tablet according to claim 1, wherein the composition does not contain vitamin B12.
9. The tablet according to claim 1, wherein the composition contains less than 2% polyvinylpyrrolidone (PVP) by weight of the composition.
10. The tablet according to claim 1, wherein the tablet is coated.
11. The tablet according to claim 10, wherein the tablet is film-coated.
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