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Pharmaceutical preparation for the alleviation of endometriosis

An endometriosis, drug technology, applied in the field of excipients/carriers, single-phase products

Inactive Publication Date: 2009-11-18
BAYER SCHERING PHARMA OY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Up to 90% of patients report irregular bleeding, but no one reports intolerable bleeding

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] Tablets are prepared with the following composition:

[0030] Dienogest, micronized 2,000mg

[0031] min.99%≤20μm, 100%<30μm

[0032] Lactose monohydrate 62,800mg

[0033] Microcrystalline Cellulose 18,000mg

[0034] Potato Starch 36,000mg

[0035] Povidone K 25 8,100mg

[0036] Magnesium Stearate 1,350mg

[0037] Talc 4,050mg

[0038] Crospovidone 2,700mg

[0039] Dienogest was used, which was micronized to an average particle size of 20 μm and mixed with lactose monohydrate, microcrystalline cellulose and potato starch. Povidone K 25 was sprayed during granulation. After drying and mixing with talc, crospovidone and magnesium stearate, the substance mixture is compressed into tablets having a diameter of 7 mm and a mass of 135 mg.

Embodiment 2

[0041] In clinical studies, 3.75 mg of the GnRH agonist leuprolide acetate (LA) was administered subcutaneously (s.c.) every 4 weeks or the progestogen dienogest (DNG) 2 mg / day orally ), treated 252 women diagnosed with endometriosis by laparoscopy. 128 patients were randomly assigned to the LH group and 124 patients were randomly assigned to the DNG group. Efficacy of various treatments is checked by a pain scale (visual analog scale (VAS)) etc. completed by the patient. At the end of treatment, both comparison groups showed similar pain reductions compared to the beginning of the study (-47.5 mm for DNG; -46.0 mm for LA). Statistical analysis showed no advantage of DNG over LA.

[0042] In addition, common side effects of hormone therapy for endometriosis are documented:

[0043] Menstrual bleeding changes occurred in both treatment groups, usually in the form of missing cycles or in the form of slightly irregular bleeding -- but these only led to discontinuation of treat...

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PUM

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Abstract

A pharmaceutical composition for the treatment of endometriosis without loss of bone density comprises a gestagenic having an antiandrogenic effect, preferably 17a-cyanomethyl-17ss-hydroxy-estra-4,9-diene-3-one (Dienogest), cyproteronacetate or chlormadinonacetate at a daily dosage which is no more than two times the dosage required to suppress ovulation, together with one or a plurality of pharmaceutically acceptable adjuvants / carriers. The pharmaceutical composition according to the invention provides both the alleviation of endometriosis and the lack of a negative affect on bone metabolism and bone density, and is simultaneously able to keep the side effects known from conventional pharmaceuticals (such as hot flashes, acne, negative affects on the lipid profile) within tolerable limits. The pharmaceutical composition is thus suitable for long-term application.

Description

technical field [0001] The present invention relates to a pharmaceutical composition for alleviating endometriosis without reducing bone density, comprising a progestogen with antiandrogenic activity in a daily dose not exceeding twice the dose of ovulation inhibitors, and one or more pharmaceutically Acceptable excipients / carriers. The invention also includes monophasic products, which do not have negative effects on bone metabolism. The product is therefore suitable for long-term use. However, the use of progestogens with antiandrogenic activity in the above doses for the manufacture of medicines makes it possible to keep the known side effects of traditional pharmaceutical compositions - such as hot flashes, acne, changes in lipid profile - within tolerable limits , the medicinal product for preventing and / or treating endometriosis without negatively affecting bone metabolism and thus reducing bone density. Background technique [0002] Endometriosis is a chronic gynec...

Claims

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Application Information

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IPC IPC(8): A61K31/57A61K31/573A61P15/00
CPCA61K31/57A61K31/573A61P15/00A61P19/08A61P19/10
Inventor C·塞茨A·瓦塞弗尔H·齐默尔曼
Owner BAYER SCHERING PHARMA OY
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