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Torasemide compound

A technology for torsemide and compounds, applied in the field of medicine, can solve the problems of unreproducible content and crystal form, difficulty in scaling up the pilot scale, low purity of torsemide, etc.

Active Publication Date: 2015-02-25
TIANJIN HANRUI PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, regardless of the method, the obtained torasemide has low purity and high impurity content; the method has poor reproducibility, and it is difficult to scale up to a pilot scale, so that the content and crystal form cannot be reproduced

Method used

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0046] In a 50L reactor, add 3 kg of torasemide (purity 97.3%, HPLC) and 30.3 L of water-acetone-ammonia = 9:0.8:1.1 mixture, heat to 88°C-91°C, add 150 gram of activated carbon, insulated and stirred for 30 minutes, filtered while hot, naturally cooled to room temperature under filtrate stirring, and then incubated for 5.5 hours, crystallization was precipitated, filtered, and vacuum-dried at room temperature to obtain 2.81 kilograms of torasemide crystals. Melting point: 148.5°C-149.6°C, purity 99.95%, single impurity 0.04%, MS: 349.13 (M+H) solvent residue detection meets the requirements.

[0047] Elemental Analysis Results:

[0048]Measured value (calculated value), C: 55.25 (55.16), H: 5.68 (5.79), N: 16.02 (16.08), S9.18 (9.20).

[0049] The X-ray diffraction pattern of the crystal is shown in figure 1 . Instrument model and measurement conditions: Rigaku D / max 2500 diffractometer; CuKa 40Kv 100mA; 2θ scanning range: 0-50 ° .

Embodiment 2

[0051] The injection containing the torasemide crystal of the present invention is prepared by using standard and conventional techniques, the specification: 10 mg / bottle.

[0052] Weigh 5 grams of sodium chloride, add 1800 milliliters of water for injection, and stir to dissolve it. In addition, 10 grams of torasemide crystals of the present invention are weighed, added to the above solution, adjusted to pH 5.5-6.5 with dilute hydrochloric acid under stirring, 1 gram of activated carbon is added, stirred for 30 minutes, filtered and decarburized to make the liquid clear, and added to the injection Water to 2000 ml, stir evenly, filter with microporous membrane, fill 2ml into a vial after the content is qualified, half-stoppered, freeze-dried in a freezer, fully stoppered, and take out the product after the vacuum is released and tie an aluminum cap. Inspect and pack.

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Abstract

The invention belongs to the technical field of medicine, and specifically relates to a torasemide compound and a preparation method thereof. The provided novel torasemide crystal form has the advantages of high purity (the maximal impurity content is less than 0.05%), and good stability. Moreover, the preparation method has a good repeatability, and the purity and crystal form can be well repeated when the preparation method is amplified to a pilot scale. The invention further relates to an application of the novel torasemide crystal form in preparation of drugs for treating medium and heavy edema caused by heart failure, kidney failure, cirrhosis ascites, encephaledema, and the like.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a torasemide compound and a preparation method thereof. The invention also relates to the use of this crystal to manufacture and treat moderate and severe edema caused by heart failure, renal failure, liver cirrhosis, ascites, and cerebral edema. drug. Background technique [0002] Torasemide (torasemide) is a long-acting diuretic that acts on the Henle of the renal tubules. It was first launched in Belgium in 1993, and was subsequently approved for marketing in Italy, Belgium, the United States, the United Kingdom and other countries, and entered my country in December 2003. Compared with other diuretics such as furosemide, this product has strong diuretic effect, high bioavailability, long-lasting effect, less adverse reactions, and good tolerance of patients. research shows. This product exerts diuretic effect by inhibiting the reabsorption of chloride and sodiu...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D213/74A61K31/44A61P7/10
CPCC07D213/74
Inventor 严洁李轩
Owner TIANJIN HANRUI PHARMA
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