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Compositions of estrogen-cyclodextrin complexes

A composition and cyclodextrin technology, which can be used in pharmaceutical combinations, non-active ingredients of polymer compounds, and medical preparations containing active ingredients, etc., can solve the lack of chemical stability, lack of physical stability, and bioavailability of free estrogen Degree not realized, etc.

Inactive Publication Date: 2014-01-08
BAYER IP GMBH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] Furthermore, due to the lack of physical stability of cyclodextrin-estrogen complexes and the lack of chemical stability of free estrogen, the improvement in bioavailability achieved by complexing estrogen with cyclodextrins has not been realized.

Method used

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  • Compositions of estrogen-cyclodextrin complexes
  • Compositions of estrogen-cyclodextrin complexes
  • Compositions of estrogen-cyclodextrin complexes

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0102] Example 1 discloses pharmaceutical products according to some embodiments of the invention as well as pharmaceutical products known to those skilled in the art. Table 1.3 shows the performance in terms of stability compared to known formulations after fixation under controlled environmental conditions for prolonged periods of time. The data indicated that direct compression of the powder blend resulted in good stability of ethinylestradiol in the form of a cyclodextrin complex (Product D). Product E is according to the invention does not contain polyvinylpyrrolidone. This product also shows that ethinyl estradiol still has good stability despite being prepared by granulation. However, if the product contains polyvinylpyrrolidone and is manufactured according to Example 3 of US 5,798,338 (tablet A), the stability of the product is poor.

Embodiment 2

[0103] Example 2 illustrates the stability of EE in formulations D and E, compared to other formulations in terms of breakdown products isolated from samples after storage under controlled environmental conditions for a fixed period of time.

Embodiment 3

[0104] Example 3 discloses the content of an embodiment of the invention wherein the composition further comprises drospirenone.

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Abstract

Pharmaceutical compositions comprising low doses of sensitive complexes of an estrogen and a cyclodextrin are provided with improved stability. In specific embodiments the composition comprises a complex between ethinyl estradiol and in a granulate preparation and in yet another embodiment the composition comprises a limited amount of polyvinylpyrrolidone since this excipient was found to degrade ethinyl estradiol. Furthermore, a method for improving the stability of an estrogen in a composition and for manufacturing such a stable composition is provided. Essentially, the granulate preparation are manufactured under careful control of the relative humidity.

Description

technical field [0001] The present invention relates to pharmaceutical compositions and formulations comprising cyclodextrin-estrogen complexes capable of imparting very high chemical stability to estrogens. The present invention improves the physical stability of cyclodextrin-estrogen complexes and the chemical stability of estrogens such as ethinylestradiol during storage. Background technique [0002] In conventional pharmaceutical products, the decomposition of eg ethinyl estradiol is one of the most critical issues with regard to product shelf life. Stabilization of the estrogen can be achieved by packaging the product in a sealed container or, more effectively as in the present invention, by actually stabilizing the drug product. [0003] Pharmaceutical products containing naturally or synthetically derived sex hormones usually consist of low doses of these active ingredients. If the amount of active ingredient required per single dose is small, usually in the range ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/565A61K31/585A61K47/40A61P15/18A61P5/30A61P17/10A61P43/00A61P15/00
Inventor 托马斯·巴肯斯费尔德沃尔夫冈·黑尔拉尔夫·利普
Owner BAYER IP GMBH
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