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Premature ovulation preventive agent

An inhibitor, premature technology, applied in the direction of pill delivery, medical preparations containing active ingredients, organic active ingredients, etc., can solve problems such as peptide compounds

Inactive Publication Date: 2008-09-24
TAKEDA PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] However, peptide compounds are still problematic in many aspects, such as oral absorbability, administration form, dosage, drug stability, sustainability of action, metabolic stability, etc.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

preparation example 1

[0338] (1) Compound A 1g

[0339] (2) Lactose 197g

[0340] (3) Corn starch 50g

[0341] (4) Magnesium stearate 2g

[0342] (1) and (2) above, and corn starch (20 g) were mixed and granulated with a paste made of corn starch (15 g) and water (25 mL). Cornstarch (15 g) and the above (4) were added thereto, and the mixture was compressed by a tablet machine to obtain tablets (2000 tablets, 3 mm in diameter), each containing 0.5 mg of Compound A.

preparation example 2

[0344] (1) Compound A 2g

[0345] (2) Lactose 197g

[0346] (3) Corn starch 50g

[0347] (4) Magnesium stearate 2g

[0348] In the same manner as in Formulation Example 1, tablets (2000 tablets, 3 mm in diameter) were prepared, each tablet containing 1.0 mg of Compound A.

preparation example 3

[0350] (1) Compound A 5.0 mg

[0351] (2) Lactose 60.0mg

[0352] (3) Corn starch 35.0mg

[0353] (4) Gelatin 3.0mg

[0354] (5) Magnesium stearate 2.0mg

[0355] The above-mentioned mixture of (1), (2) and (3) was granulated with 0.03 ml of 10% gelatin aqueous solution (3.0 mg of gelatin) through a 1 mm mesh sieve. The granules were dried at 40°C and sieved again. The resulting granules were mixed with (5) above and compressed. The resulting tablet cores are coated with an aqueous sugar coating suspension of sucrose, titanium dioxide, talc and gum arabic. The coated tablets were buffed with beeswax to obtain coated tablets.

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Abstract

A preventive agent of premature ovulation which may occur during in vitro fertilization or embryo transplantation, the agent comprising a non-peptide compound having an antagonistic effect on a gonadotropin-releasing hormone. The preventive agent shows a low toxicity, can be administered through an oral route, and has an excellent preventive effect on the premature ovulation during in vitro fertilization or embryo transplantation.

Description

technical field [0001] The present invention relates to the pharmaceutical use of non-peptide compounds having an antagonistic effect on gonadotropin-releasing hormone, and more particularly, the present invention relates to premature ovulation inhibitors (inhibitors) for in vitro fertilization or embryo transfer procedures. Background technique [0002] The secretion of anterior pituitary hormones is regulated by peripheral hormones secreted by various hormone target organs, and hormones secreted by the hypothalamus to promote secretion or inhibit secretion (these hormone families are generally referred to as hypothalamic hormones hereinafter in this specification), and the hypothalamus Is the upper nerve of the anterior pituitary gland. So far, 9 hormones have been confirmed in hypothalamic hormones, for example, thyrotropin-releasing hormone (TRH), gonadotropin-releasing hormone {GnRH: also called luteinizing hormone-releasing hormone (LH-RH)}, etc. These hypothalamic h...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K45/00A61K31/519A61P15/06A61P15/08A61P43/00C07D495/04
CPCC07D495/04A61K31/519A61K9/2059A61P15/06A61P15/08A61P43/00A61K45/00
Inventor 古矢修一日下雅美
Owner TAKEDA PHARMA CO LTD
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