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Crystal for oral solid drug and oral solid drug for dysuria treatment containing the same

A technology for dysuria and solids, which can be used in drug combinations, pharmaceutical formulations, urinary system diseases, etc., and can solve the problems of unreported KMD-3213 crystalline polymorphic methods, unreported and mentioned which types of crystalline forms exist, preparation methods and its nature

Inactive Publication Date: 2005-11-09
KISSEI PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] Namely, so far, no method for preparing KMD-3213 crystalline polymorphs has been reported
In addition, there is no report or mention of what type of crystal form exists, its preparation method and its properties, etc.

Method used

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  • Crystal for oral solid drug and oral solid drug for dysuria treatment containing the same
  • Crystal for oral solid drug and oral solid drug for dysuria treatment containing the same
  • Crystal for oral solid drug and oral solid drug for dysuria treatment containing the same

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0051] Preparation of Form α

[0052] To 1 g of crude crystals of KMD-3213 was added 3 ml of ethyl acetate, and the mixture was heated to dissolve. After filtering off insoluble materials, the filtrate was left standing at room temperature. After the resulting crystals were completely precipitated, 10 ml of ethyl acetate was added thereto. The resulting crystals were collected by filtration and dried under vacuum at 50°C for 16 hours to yield 930 mg of Form α.

Embodiment 2

[0054] Preparation of Form β

[0055] To 1 g of crude crystals of KMD-3213 was added 0.4 ml of methanol, and the mixture was heated to dissolve. After filtering off the insoluble matter, 20 ml of petroleum ether was added thereto and vigorously shaken. The resulting crystals were collected by filtration and dried under vacuum at 50°C for 16 hours to yield 930 mg of Form α.

Embodiment 3

[0057] Preparation of Crystal Formsγ

[0058] To 1 g of crude crystals of KMD-3213 was added 4 ml of toluene, and the mixture was heated to dissolve. After filtering off insoluble materials, the filtrate was left standing at room temperature. After the resulting crystals were completely precipitated, 10 ml of toluene was added thereto. The resulting crystals were collected by filtration and dried under vacuum at 50°C for 16 hours to yield 970 mg of Form α.

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PUM

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Abstract

A crystal for oral solid drug comprised of indoline compound (KMD-3213) which exerts alpha1-adrenaline receptor shielding activity, is useful as a therapeutic agent for dysuria and is represented by the formula: (I) wherein in the powder X-ray diffraction pattern, the compound is characterized by main peaks of 5.5 DEG +- 0.2 DEG , 6.1 DEG +- 0.2 DEG , 9.8 DEG +- 0.2 DEG , 11.1 DEG +- 0.2 DEG , 12.2 DEG +- 0.2 DEG , 16.4 DEG +- 0.2 DEG , 19.7 DEG +- 0.2 DEG and 20.0 DEG +- 0.2 DEG as 2theta. There is further provided an oral solid drug for dysuria treatment containing the crystal as an active ingredient.

Description

technical field [0001] The invention relates to a crystal for oral solid medicine. More specifically, the present invention relates to crystals for oral solid medicine of indoline represented by the following general formula (hereinafter referred to as KMD-3213): [0002] [0003] it plays alpha 1 - Adrenergic receptors (α 1 -AR) blocking effect, and used as a therapeutic agent for dysuria; and relates to an oral solid medicament for treating dysuria comprising said crystal as an active ingredient. [0004] The present invention also relates to an oral solid drug comprising KMD-3213 crystals for oral solid drug as active ingredients and α 1 - at least one of an AR blocker, an anticholinergic, a 5α-reductase inhibitor, a sex hormone, an anxiolytic, a cholinomimetic, a cholinesterase inhibitor, an anti-inflammatory, and an antibacterial. [0005] Furthermore, the present invention relates to a medicine for treating dysuria, which comprises a medicine comprising KMD-3213 c...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K9/48A61K31/404A61K45/00A61K47/02A61P13/02C07D209/08
CPCC07D209/08A61K31/404A61P13/02A61P13/12C07D209/14A61K45/06A61K2300/00C07B2200/13
Inventor 靏荣治户田道雄平田一满
Owner KISSEI PHARMA
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