Preparation method of nicorandil for injection

A technology for nicorandil and injection, applied in the field of chemical preparations, can solve the problems of difficult control of moisture content of finished products, poor crystal form, difficult operation, etc., and achieves ideal reconstitution effect, good crystal form, and good freeze-drying effect. Effect

Active Publication Date: 2021-11-05
TIANJIN TASLY ZHIJIAO PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0013] In the existing preparation methods of nicorandil freeze-dried preparations, freeze-drying and low-temperature drying are selected during drying, but this method takes a long time, consumes a lot of energy, and the moisture content of the finished product is not easy to control
Or choose ethanol as a solvent for freeze-drying. Ethanol is flammable and explosive.

Method used

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  • Preparation method of nicorandil for injection
  • Preparation method of nicorandil for injection
  • Preparation method of nicorandil for injection

Examples

Experimental program
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Effect test

Embodiment 1

[0216] Specification 12mg / bottle: Take 0.6g of sodium citrate, add 216g (360 times) of water for injection, dissolve the water at a temperature of 10-15°C, stir, and measure the pH value; take another 1.8g of mannitol, add the above solution to dissolve, and stir; Take 1.2g of Nicorandil, add the above solution, stir ultrasonically to dissolve, and measure the pH value; after dissolving, add 0.05mol / L citric acid (1.05g / 100ml requires about 100ml) to adjust the pH value to 7.5, and the liquid is cooled to Store at 2-5°C. Sterile filtration, filling and subpackaging are carried out according to conventional methods, and each bottle is 3ml.

Embodiment 2

[0218] Specification 48mg / bottle: Take 2.4g of sodium citrate, add 864g (360 times) of water for injection, dissolve the water at a temperature of 10-15°C, stir, and measure the pH value; take another 7.2g of mannitol, add the above solution to dissolve, and stir; Take 4.8g of Nicorandil, add the above solution, stir ultrasonically to dissolve, and measure the pH value; after dissolving, add 0.05mol / L citric acid (1.05g / 100ml requires about 100ml) to adjust the pH value to 7.5, and cool down the liquid Store at 2-5°C. Carry out sterilizing filtration according to the conventional method, fill, sub-package, each bottle is 12ml.

Embodiment 3

[0220] Carry out lyophilization to the subpackage liquid medicine of embodiment 1:

[0221]

[0222]

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Abstract

The invention relates to a preparation method of nicorandil for injection. The nicorandil for injection, disclosed by the invention, is prepared from nicorandil, mannitol, sodium citrate and water for injection through the procedures of liquid preparation and freeze drying, and the weight ratio of all the components is as follows: nicorandil: mannitol: sodium citrate: water for injection is 2: 3: 1: (300-600). The preparation method of the nicorandil for injection, disclosed by the invention, comprises the following steps: step 1, liquid preparation, and step 2, freeze-drying, wherein the freeze-drying step further comprises the following steps: step A, pre-freezing, freeze-thawing, crystallizing and annealing, and step B, sublimation stage.

Description

technical field [0001] The invention belongs to the field of chemical preparations, and in particular relates to a method for preparing a stable solution of nicorandil for injection and a method for preparing nicorandil freeze-dried powder for injection. [0002] technical background [0003] Nicorandil (Nicorandil), drug aliases Nicorandine, Nitonic acid ester, SIGMART, PERISALOL, the translated names in the patent are: Nicorandil, Nicorandil, chemical name N-(2-hydroxyethyl ) nicotinamide nitrate, the structural formula is as follows: [0004] [0005] Nicorandil, as the first potassium ion channel opening drug, has double-layer effects of nitrate ester and potassium ion channel opening, which can not only relieve symptoms but also improve prognosis, significantly reduce the incidence of cardiovascular events in patients with angina pectoris, and fill the dual role of angina pectoris treatment. It is an ideal drug for the treatment of angina pectoris. [0006] Physical...

Claims

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Application Information

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IPC IPC(8): A61K9/08A61K31/4406A61K47/10A61K47/12A61K9/19A61P9/10
CPCA61K9/08A61K31/4406A61K47/10A61K47/12A61K9/19A61P9/10
Inventor 宋丽丽岳洪水郝晓为苏亚芹鞠爱春
Owner TIANJIN TASLY ZHIJIAO PHARMA
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