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Stable hydrochlorothiazide crystalline compound, and composite enalapril maleate pharmaceutical composition thereof

A technology of enalapril maleate and crystal compounds, which is applied in the field of medicine, can solve the problems of slow absorption rate and low solubility, and achieve the effects of small fluctuations, good solubility, and reduced side effects

Inactive Publication Date: 2015-07-01
张旻
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

For domestic and foreign marketed samples, common crystals of hydrochlorothiazide are used, which have low solubility in water and slow absorption rate in the body. It is of great significance to study the structure of its stable crystal form and fast-release compound

Method used

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  • Stable hydrochlorothiazide crystalline compound, and composite enalapril maleate pharmaceutical composition thereof
  • Stable hydrochlorothiazide crystalline compound, and composite enalapril maleate pharmaceutical composition thereof
  • Stable hydrochlorothiazide crystalline compound, and composite enalapril maleate pharmaceutical composition thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0083] First dissolve the hydrochlorothiazide solid in the sodium hydroxide acetone solution, adjust the temperature of the solution to drop a mixed solvent of chloroform and absolute ethanol under the condition of 50° C., the volume ratio of the chloroform and absolute ethanol is 1: 1.5, the feeding speed of the chloroform and dehydrated ethanol is 2ml / min, and the stirring speed is 20 rpm when the described feeding of chloroform and dehydrated ethanol, after the mixed solvent is added dropwise, Continue heat preservation and stirring for 30 minutes, lower the temperature to 30° C., heat preservation and stirring for 30 minutes to obtain crystals: filter, wash the filter cake with chloroform, and vacuum dry for 2-4 hours to obtain hydrochlorothiazide crystal compound.

[0084] X-ray powder diffraction measured by using Cu-Kα rays at 2θ of 11.4°, 13.9°, 14.4°, 17.9°, 20.8°, 21.2°, 24.1°, 24.8°, 25.0°, 26.2°, 28.0°, 38.0 ° shows a characteristic peak, and its X-ray powder diffr...

Embodiment 2

[0086] First dissolve the hydrochlorothiazide solid in the sodium hydroxide acetone solution, adjust the temperature of the solution to drop a mixed solvent of chloroform and absolute ethanol under the condition of 50° C., the volume ratio of the chloroform and absolute ethanol is 1: 1.25, the feeding speed of the chloroform and dehydrated ethanol is 3ml / min, and the stirring speed is 30 rpm when the described chloroform and dehydrated ethanol is added, after the mixed solvent is added dropwise, Continue heat preservation and stirring for 30 minutes, lower the temperature to 30° C., heat preservation and stirring for 30 minutes to obtain crystals: filter, wash the filter cake with chloroform, and vacuum dry for 2-4 hours to obtain hydrochlorothiazide crystal compound.

[0087] X-ray powder diffraction measured by using Cu-Kα rays at 2θ of 11.4°, 13.9°, 14.4°, 17.9°, 20.8°, 21.2°, 24.1°, 24.8°, 25.0°, 26.2°, 28.0°, 38.0 ° shows a characteristic peak, and its X-ray powder diffra...

Embodiment 3

[0089]First dissolve the hydrochlorothiazide solid in the sodium hydroxide acetone solution, adjust the temperature of the solution to drop a mixed solvent of chloroform and absolute ethanol under the condition of 51° C., the volume ratio of the chloroform and absolute ethanol is 1: 1.1, the feeding speed of the chloroform and dehydrated ethanol is 5ml / min, and the stirring speed is 45 rpm when the described feeding of chloroform and dehydrated ethanol, after the mixed solvent is added dropwise, Continue to insulate and stir for 30 minutes, lower the temperature to 31° C., and insulate and stir for 30 minutes to obtain crystals: filter, wash the filter cake with chloroform, and vacuum-dry for 2-4 hours to obtain hydrochlorothiazide crystalline compound.

[0090] X-ray powder diffraction measured by using Cu-Kα rays at 2θ of 11.4°, 13.9°, 14.4°, 17.9°, 20.8°, 21.2°, 24.1°, 24.8°, 25.0°, 26.2°, 28.0°, 38.0 ° shows a characteristic peak, and its X-ray powder diffraction pattern i...

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Abstract

The invention belongs to the technical field of medicines, and provides a stable hydrochlorothiazide crystalline compound, and a composite enalapril maleate pharmaceutical composition thereof, and a preparation method. The method comprises the following steps: dissolving hydrochlorothiazide sold into water; dropwise adding a mixed solvent of absolute ethyl alcohol and trichloromethane; and carrying out heat-preservation stirring, cooling, carrying out heat-preservation stirring, filtering, washing and drying in vacuum to obtain the hydrochlorothiazide crystalline compound. The hydrochlorothiazide crystalline compound is high in yield, high in purity, good in water solubility and stable in quality. The invention further provides a composite enalapril maleate pharmaceutical composition containing the stable hydrochlorothiazide crystalline compound and a preparation method of the composite enalapril maleate pharmaceutical composition. The composite enalapril hydrochlorothiazide pharmaceutical composition prepared by the preparation formula and the preparation technology is stable in quality; and industrialized implementation is easily to realize.

Description

technical field [0001] The invention relates to the field of medicine, in particular to a stable hydrochlorothiazide crystal compound, its compound enalapril hydrochlorothiazide pharmaceutical composition and a preparation method thereof. Background technique [0002] The global prevalence of hypertension is very high, whether in developed or developing countries, essential hypertension affects 25% to 35% of adults, especially in the West, which accounts for 1 / 3 of the adult population, while It accounts for 60% to 70% of people over 70 years old. There are about 1 billion people in the world, and their heart, brain, and kidney are the important target organs damaged by hypertension. Hypertension is not only an important risk factor for cardiovascular and cerebrovascular diseases, but also increases the risk of heart failure, renal failure and left ventricular hypertrophy, and causes serious economic burden to patients. About 30% to 40% of deaths from cardiovascular and ce...

Claims

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Application Information

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IPC IPC(8): C07D285/28A61K38/05A61K31/549A61P9/12
CPCC07D285/28A61K31/549A61K38/05C07B2200/13
Inventor 张旻
Owner 张旻
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