You’re using a public version of DrugPatentWatch with 5 free searches available | Register to unlock more free searches. CREATE FREE ACCOUNT

Last Updated: April 19, 2024

Claims for Patent: 8,617,597


✉ Email this page to a colleague

« Back to Dashboard


Summary for Patent: 8,617,597
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)
Application Number:11/773,689
Patent Litigation and PTAB cases: See patent lawsuits and PTAB cases for patent 8,617,597
Patent Claims: 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.

Make Better Decisions: Try a trial or see plans & pricing

Drugs may be covered by multiple patents or regulatory protections. All trademarks and applicant names are the property of their respective owners or licensors. Although great care is taken in the proper and correct provision of this service, thinkBiotech LLC does not accept any responsibility for possible consequences of errors or omissions in the provided data. The data presented herein is for information purposes only. There is no warranty that the data contained herein is error free. thinkBiotech performs no independent verification of facts as provided by public sources nor are attempts made to provide legal or investing advice. Any reliance on data provided herein is done solely at the discretion of the user. Users of this service are advised to seek professional advice and independent confirmation before considering acting on any of the provided information. thinkBiotech LLC reserves the right to amend, extend or withdraw any part or all of the offered service without notice.