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Semihydrate crystal of silodosin, preparation method thereof and medicinal composition containing semihydrate crystal

A hemihydrate and crystal technology, which is applied in the direction of drug combinations, medical preparations containing active ingredients, and pharmaceutical formulas, to achieve cost-effective, environmentally friendly, low-cost, and easy-to-operate effects

Active Publication Date: 2011-11-02
NANJING HEALTHNICE MEDICAL TECH +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In addition, using silodosin hemihydrate crystals as an active ingredient and adding pharmaceutically acceptable adjuvants or excipients to prepare pharmaceutical preparations for treating dysuria has not been reported yet.

Method used

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  • Semihydrate crystal of silodosin, preparation method thereof and medicinal composition containing semihydrate crystal
  • Semihydrate crystal of silodosin, preparation method thereof and medicinal composition containing semihydrate crystal
  • Semihydrate crystal of silodosin, preparation method thereof and medicinal composition containing semihydrate crystal

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] Implementation example 1: Preparation of hemihydrate crystals of silodosin

[0028] Take 1g of this product and dissolve it with 2ml of ethanol, filter to remove the insoluble matter, slowly add 30ml of water to the mother liquor under stirring until the crystalline solid is completely precipitated, and continue to stir for 30 minutes. The resulting solid was collected by filtration and dried under vacuum at 50° C. for 12 hours to constant weight to obtain 950 mg of crystals with a purity of 99.3%. The obtained crystalline form is characterized by the following powder X-ray diffraction pattern, which is measured by a diffractometer and expressed in terms of interplanar distance d, 2θ angle, intensity and intensity:

[0029]

Embodiment 2

[0030] Implementation example 2: Preparation of hemihydrate crystals of silodosin

[0031] Take 1g of this product and dissolve it with 2ml of ethyl acetate, filter to remove the insoluble matter, slowly add water dropwise to the mother liquor with stirring until the solid precipitates, add 5ml of water after the solid precipitates, and continue stirring for 0.5 hours. The resulting solid was collected by filtration and dried under vacuum at 50° C. for 12 hours to constant weight to obtain 930 mg of crystals with a purity of 99.5%.

[0032] The obtained crystal form is characterized by the following powder X-ray diffraction pattern, which is measured by a diffractometer and expressed in terms of interplanar distance d, 2θ angle, and intensity:

[0033]

[0034]

Embodiment 3

[0035] Embodiment 3: Capsule 1

[0036] formula:

[0037] Silodosin hemihydrate crystals 2.0g

[0038] Mannitol 66.5g

[0039] Pregelatinized starch 30.0g

[0040] Magnesium Stearate 1.0g

[0041] Sodium Lauryl Sulfate 0.5g

[0042] According to the above formula, 1000 capsules containing 2.0 mg of silodosin hemihydrate crystals were prepared in the capsules by conventional methods.

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PUM

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Abstract

The invention relates to semihydrate crystal of silodosin, a preparation method thereof and a medicinal composition containing the semihydrate crystal. The semihydrate crystal is prepared by crystallizing under the combined action of an organic solvent and water. The crystal form of the semihydrate crystal is represented by an X-ray powder diffraction figure of the semihydrate crystal.

Description

technical field [0001] The present invention relates to silodosin or formula (I) 2,3-dihydro-1-(3-hydroxypropyl)-5-[(2R)-2-[2-[2-(2,2,2 - Hemihydrate crystal of trifluoroethoxy)phenoxy]ethylamino]propyl]-1H-indole-7-carboxamide, preparation method and pharmaceutical composition containing it. [0002] Background technique [0003] Silodosin (silodosin), 2,3-dihydro-1-(3-hydroxypropyl)-5-[(2R)-2-[2-[2-(2,2,2-trifluoroethane Oxygen) phenoxy] ethylamino] propyl] -1H-indole-7-carboxamide, is a kind of substituted indoline compound, its molecular structure formula is as follows: [0004] [0005] Silodosin is an alpha 1 - adrenoceptor antagonists, which selectively inhibit the contraction of the smooth machine of the urethra and are useful in the treatment of disorders associated with urethral tissue blockage, neurological disorders of voiding control, functional urethral blockage, and prostatic hypertrophy, Drug compound for dysuria caused by urethral stricture, urethra...

Claims

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Application Information

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IPC IPC(8): C07D209/08A61K31/4045A61P13/00
Inventor 邹巧根
Owner NANJING HEALTHNICE MEDICAL TECH
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