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Captopril zinc complexe and its preparation method and preparation

A technology for zinc complexes and preparations, which is applied in the field of captopril zinc complexes and their preparation methods and preparations, which can solve the problems of unstable drug effects, large differences in peak and valley concentrations, and increased side effects, and reduce volatility , prolonged residence time, and reduced side effects

Inactive Publication Date: 2015-07-15
SUN YAT SEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

After clinical administration 2-3 times a day, there is a large difference in the peak concentration in the plasma, which makes the drug effect unstable or the side effects increase.

Method used

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  • Captopril zinc complexe and its preparation method and preparation
  • Captopril zinc complexe and its preparation method and preparation
  • Captopril zinc complexe and its preparation method and preparation

Examples

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preparation example Construction

[0039] A preparation method of captopril zinc complex, comprising the steps of:

[0040] 1) Add excess captopril and zinc oxide or zinc hydroxide into water or an organic solvent according to the reaction formula, and fully stir;

[0041] 2) Filtrating the generated precipitate and drying under reduced pressure to obtain the captopril zinc complex.

[0042] Because the solubility of zinc oxide itself is extremely small, in order to make the reaction more complete and to make the impurities in the product easy to remove, captopril should be added in excess so that the molar weight of captopril is greater than that of zinc oxide . Preferably, the molar ratio of captopril to zinc oxide is (2-3):1.

[0043] In the above reaction, the organic solvent is preferably a polar organic solvent. Preferably, the organic solvent is miscible with water and can dissolve a certain amount of zinc oxide or zinc hydroxide. In particular, the organic solvent is selected from methanol, acetone, ...

Embodiment 1

[0056] Weigh 217 mg of captopril and 41 mg of zinc oxide, add 2 mL of methanol, stir and react at 60°C for 8 hours to obtain a white suspension, filter, and dry under reduced pressure to obtain 130 mg of a white powdery solid with a yield of 93%.

Embodiment 2

[0058] Weigh 217 mg of captopril and 27 mg of zinc oxide, add 2 mL of water, stir and react at room temperature for 12 hours to obtain a white suspension, filter, and dry under reduced pressure to obtain 89 mg of a white powdery solid with a yield of 96%.

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Abstract

The invention discloses a captopril zinc complexe and its preparation method and preparation. The captopril zinc complexe is prepared by combining captopril and zinc ions in a molar ratio of 1:1, the captopril zinc complexe is small in blood concentration fluctuation and easy to prepare. The preparation method related in the invention has the advantages of simple operation, mild reaction condition and easy control, and elemental analysis and XRPD (X-ray powder diffraction) analysis results show that the prepared captopril zinc complexe is high in purity and low in content of impurities.

Description

technical field [0001] The present invention relates to a compound complex and its preparation method and preparation, in particular to captopril zinc complex and its preparation method and preparation. Background technique [0002] Captopril is an orally effective angiotensin converting enzyme inhibitor, its chemical name is: 1-[(2S)2-methyl-3-mercapto-1-oxypropyl]-L-proline acid, which has the molecular formula C 9 h 13 NO 3 S, the chemical structural formula is as follows [0003] [0004] Captopril is recorded in the second part of the "Chinese Pharmacopoeia" 2010 edition. It is one of the first-choice drugs for renal parenchymal and renovascular hypertension and congestive heart failure, and is widely used at home and abroad. Captopril is metabolized quickly in the body, with a half-life of about 2 to 3 hours, and it is absorbed rapidly after oral administration, with a short peak time (less than 1 hour), high peak concentration, and side effects such as tachycar...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D207/16A61K31/401A61P9/12A61P9/04
CPCC07D207/16
Inventor 陈嘉媚姚加鲁统部
Owner SUN YAT SEN UNIV