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Injectable naproxen preparation and application thereof

A naproxen and injection technology, applied in the field of injectable naproxen preparations, can solve problems such as turbid insoluble matter, reduce the rapid bioavailability of active ingredients, avoid secondary pollution, facilitate large-scale production, The effect of using less material

Pending Publication Date: 2021-12-03
艾迈华创(武汉)科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Since the solubility of naproxen in water is as low as 14 mg / L, most of the clinically used injections in the market are prepared from naproxen sodium, and the pH of naproxen sodium injection is generally 8.0-9.5, which is different from that of blood. The difference of pH value 7.4 reaches 2 points. After intravenous injection, a part of naproxen sodium obtains protons to form naproxen in the environment of lower pH value, and precipitates crystal naproxen precipitate, which reduces the rapid bioavailability of active ingredients. May also be one of the causes of burning sensation at the injection site
And some injection preparations even have turbid insoluble matter before injection

Method used

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  • Injectable naproxen preparation and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] The preparation method of described injectable naproxen preparation, comprises the steps:

[0039] S1. Accurately weigh 2.48g sodium phosphate dodecahydrate and add it to 800mL water for injection to dissolve, then add 5.00g naproxen to continue dissolving, then add 7.5g sodium chloride to dissolve to obtain a mixed solution;

[0040] S2, using 1.0mol / L sodium hydroxide, 1.0mol / L potassium hydroxide or 1.0mol / L hydrochloric acid to adjust the pH value of the mixed solution obtained in step S1 to 7.4, and then adding water for injection to dilute to 1000g to obtain a diluted solution;

[0041] S3. After filtering the diluted solution obtained in step S2, sub-package, and obtain a colorless and clear injectable naproxen preparation with a naproxen concentration of 250 mg / 50 ml after sterilization.

Embodiment 2

[0043] The preparation method of described injectable naproxen preparation, comprises the steps:

[0044] S1. Accurately weigh 1.88g sodium phosphate dodecahydrate and add it to 800mL water for injection to dissolve, then add 2.5g naproxen to continue dissolving, then add 8.0g sodium chloride to dissolve to obtain a mixed solution;

[0045] S2, using 1.0mol / L sodium hydroxide, 1.0mol / L potassium hydroxide or 1.0mol / L hydrochloric acid to adjust the pH value of the mixed solution obtained in step S1 to 7.2, and then adding water for injection to dilute to 1000g to obtain a diluted solution;

[0046] S3. After filtering the diluted solution obtained in step S2, sub-package, and obtain a colorless and clear injectable naproxen preparation with a naproxen concentration of 250 mg / 100 ml after sterilization.

Embodiment 3

[0048] The preparation method of described injectable naproxen preparation, comprises the steps:

[0049] S1. Accurately weigh 4.13g sodium phosphate dodecahydrate and add it to 800mL water for injection to dissolve, then add 2.50g naproxen to continue dissolving, then add 7.0g sodium chloride to dissolve to obtain a mixed solution;

[0050] S2, using 1.0mol / L sodium hydroxide, 1.0mol / L potassium hydroxide or 1.0mol / L hydrochloric acid to adjust the pH value of the mixed solution obtained in step S1 to 6.8, and then adding water for injection to dilute to 1000g to obtain a diluted solution;

[0051] S3. After filtering the diluted solution obtained in step S2, sub-package, and obtain a colorless and clear injectable naproxen preparation with a naproxen concentration of 250 mg / 100 ml after sterilization.

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Abstract

The invention discloses an injectable naproxen preparation. The injectable naproxen preparation comprises at least one of phosphate or citrate, wherein the phosphate or the citrate is tribasic acid salt, the phosphate (sodium salt or potassium salt) or the citrate (sodium salt or potassium salt) is alkaline after dissolving in water and is a solubilizing agent, the dissolving property of naproxen in a neutral pH value buffer aqueous solution can be improved, and the balance distribution ratio of the content of the effective component naproxen to the content of precursor sodium salt in the solution is obviously improved; and besides the three forms of the phosphate or the citrate also play a role of a stabilizer, so that the storage time of the injectable naproxen preparation can be remarkably prolonged. When the phosphate or the citrate is used together, a pH buffer system formed by the phosphate and the citrate is more stable through the synergistic effect of the phosphate and the citrate. The stable injection with the neutral pH value is expected to be capable of reducing or eliminating untoward effects such as burning sensation generated at injection positions of clinical injections and along veins.

Description

technical field [0001] The invention belongs to the technical field of biomedicine, and in particular relates to an injectable naproxen preparation and application thereof. Background technique [0002] Naproxen, also known as (+)-α-methyl-6-methoxy-2-naphthaleneacetic acid, is a non-steroidal drug widely used in the treatment of pain, fever, inflammation, and can inhibit prostaglandin Synthesizing and exerting anti-inflammatory and analgesic effect, its effect is stronger than aspirin, absorbs rapidly and completely, reaches the highest blood concentration in 2 hours, is suitable for rheumatoid arthritis, osteoarthritis, acute ventilation, etc., and its effect is good and It has less side effects and is one of the best-selling over-the-counter drugs in the world. Tablets, capsules, and suppositories are the main products that have been widely used clinically in the market for a long time. [0003] In recent years, some naproxen injections have appeared, mainly the patent ...

Claims

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Application Information

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IPC IPC(8): A61K9/08A61K31/192A61K47/02A61K47/12A61P19/02A61P19/06A61P29/00
CPCA61K31/192A61K9/08A61K9/0019A61K47/12A61K47/02A61P29/00A61P19/06A61P19/02
Inventor 成博成尚理
Owner 艾迈华创(武汉)科技有限公司
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