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Pharmaceutical composition containing a tetrahydrofolic acid

A technology of tetrahydrofolate and composition, which is applied in the direction of drug combination, medical preparation containing active ingredients, pharmaceutical formula, etc.

Active Publication Date: 2009-07-15
BAYER IP GMBH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The preparation of stable pharmaceutical compositions comprising low doses of tetrahydrofolate is a challenging task in itself, as stability issues are exacerbated when incorporated into pharmaceutical compositions at low concentrations

Method used

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  • Pharmaceutical composition containing a tetrahydrofolic acid
  • Pharmaceutical composition containing a tetrahydrofolic acid
  • Pharmaceutical composition containing a tetrahydrofolic acid

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0098] Example 1 - Direct Compression; Microcrystalline Cellulose

[0099] 80 mg tablet cores with the following composition are prepared by direct compression:

[0100]

[0101] To test the stability of calcium 5-methyl-(6S)-tetrahydrofolate during storage under various conditions. The following stability data were obtained upon storage at 25°C / 60%RH and 40°C / 75%RH respectively (see Tables 1 and 2 below). Stability was tested in open and closed containers.

[0102] Table 1: Percentage of total degradation products

[0103]

[0104] Table 2: Amount (%)

[0105]

[0106] It can be seen that satisfactory stability of calcium 5-methyl-(6S)-tetrahydrofolate was obtained at 25°C even under conditions that allowed the tablets to be exposed to open air. In addition, satisfactory stability was obtained at 40°C (closed container), while 5-methyl-(6S)-tetrahydrofolate calcium was seen when the tablets were stored at 40°C while being exposed to open air. Significantly degr...

Embodiment 2

[0108] Embodiment 2-direct compression tablet; (Lactose Monohydrate / Cellulose Powder)

[0109] 80 mg tablet cores with the following composition are prepared by direct compression:

[0110]

[0111] To test the stability of calcium 5-methyl-(6S)-tetrahydrofolate during storage under various conditions. The following stability data were obtained upon storage at 25°C / 60%RH and 40°C / 75%RH respectively (see Tables 3 and 4 below). Stability was tested in open and closed containers.

[0112] Table 3: Sum of decomposition products (%)

[0113]

[0114] Table 4: percentage amount

[0115]

[0116] It can be seen that satisfactory stability of calcium 5-methyl-(6S)-tetrahydrofolate was obtained at 25°C. However, like Example 1, the dissolution rate of drospirenone was unsatisfactorily slow.

Embodiment 3

[0117] Embodiment 3 - direct compression tablet; (lactose monohydrate)

[0118] 80 mg tablet cores with the following composition are prepared by direct compression:

[0119]

[0120] The stability of calcium 5-methyl-(6S)-tetrahydrofolate was found to be unsatisfactory when stored at 25°C / 60%RH and 40°C / 75%RH, respectively. Like Examples 1 and 2, the dissolution rate of drospirenone was unsatisfactorily slow.

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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.

Description

field of invention [0001] The present invention relates to solid pharmaceutical compositions, especially oral contraceptives, comprising tetrahydrofolate, such as calcium 5-methyl-(6S)-tetrahydrofolate. The composition provided by the present invention allows a good stability of said tetrahydrofolate in storage while still ensuring a fast and reliable release of the estrogen and progestogen present in said composition. Background of the invention [0002] In pregnant women, correction of low folate serum levels takes at least two months, whereas reserves last only as short as a few weeks. According to public health service recommendations, all women of potential pregnancy should therefore consume 400 μg / day of folic acid to reduce the risk of birth defects (MMWR Morb.Mortal.Wkly.Rep.1992;41(RR-14):1-7) . Folic acid supplementation immediately before stopping oral contraceptive use or immediately after a positive pregnancy test has already been obtained may not be sufficien...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K31/585A61K31/567A61K31/525A61P15/18
CPCA61K9/2018A61K9/2054A61P15/00A61P15/18A61P5/30A61P5/34A61K31/525A61K31/57A61K31/585A61K9/20A61K31/567A61K31/565
Inventor K·金
Owner BAYER IP GMBH
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