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Sitafloxacin fumarate injection and preparation method thereof

A technology of sitafloxacin and fumaric acid, which is applied in the direction of pharmaceutical formulations, medical preparations containing no active ingredients, medical preparations containing active ingredients, etc., can solve the problem of content decline, dark yellow color of liquid medicine, and pH value. Stability and other issues, to achieve the effect of maintaining stability, the best effect, and improving drug solubility

Active Publication Date: 2016-07-20
NANJING YOUKE BIOLOGICAL MEDICAL RES +2
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0010] According to the above, there are a series of unstable factors in sitafloxacin fumarate in aqueous solution, especially under high temperature and light conditions, it is easy to produce oxidation and photodegradation impurities. Problems with stability and content decline

Method used

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  • Sitafloxacin fumarate injection and preparation method thereof
  • Sitafloxacin fumarate injection and preparation method thereof
  • Sitafloxacin fumarate injection and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0050] Example 1 Each 50mg / 20mL, 1000

[0051] Sitafloxacin fumarate 0.25% (calculated as sitafloxacin)

[0052] Aspartic Acid 1%

[0053] Appropriate amount of histidine, adjust pH5.5~6.5

[0054] Methionine 0.5%

[0055] Sorbitol 0.1%

[0056] The balance of water for injection.

[0057] Preparation:

[0058] (1) Weigh aspartic acid and methionine according to the ratio and dissolve them in water for injection to prepare a concentrated solution with a total weight of 20-30% (w / w), keep warm at 45°C-55°C, stir and dissolve, then add For sitafloxacin fumarate, stir to completely dissolve, add 70% of the prescription amount with water for injection to dilute, then add sorbitol, stir to dissolve, and cool to room temperature;

[0059] (2) Dissolve histidine in an appropriate amount of water for injection, slowly add it dropwise to the above solution, adjust the pH to 5.5-6.5, and replenish the water for injection to the full amount;

[0060] (3) Add 0.05% (g / ml) activated...

Embodiment 2

[0062] Example 2 Each 100mg / 20mL, 1000

[0063] Sitafloxacin fumarate 0.5% (calculated as sitafloxacin)

[0064] Aspartic Acid 1.5%

[0065] Appropriate amount of histidine, adjust pH5.5~6.5

[0066] Methionine 0.8%

[0067] Sorbitol 0.1%

[0068] The balance of water for injection.

[0069] Preparation:

[0070] (1) Weigh aspartic acid and methionine according to the ratio and dissolve them in water for injection to prepare a concentrated solution with a total weight of 20-30% (w / w), keep warm at 45°C-55°C, stir and dissolve, then add For sitafloxacin fumarate, stir to completely dissolve, add 70% of the prescription amount with water for injection to dilute, then add sorbitol, stir to dissolve, and cool to room temperature;

[0071] (2) Dissolve histidine in an appropriate amount of water for injection, slowly add it dropwise to the above solution, adjust the pH to 5.5-6.5, and replenish the water for injection to the full amount;

[0072] (3) Add 0.05% (g / ml) activat...

Embodiment 3

[0074] Example 3 Each 50mg / 20mL, 1000

[0075] Sitafloxacin fumarate 0.25% (calculated as sitafloxacin)

[0076] Citric acid 0.6%

[0077] Appropriate amount of sodium citrate, adjust pH5.5~6.5

[0078] Methionine 0.3%

[0079] Sorbitol 0.1%

[0080] The balance of water for injection.

[0081] Preparation:

[0082] (1) Weigh citric acid and methionine according to the ratio and dissolve them in water for injection to prepare a concentrated solution with a total weight of 20-30% (w / w), keep warm at 45°C-55°C, stir and dissolve, then add fuma Acid sitafloxacin, stir to make it completely dissolved, add 70% of the prescription amount with water for injection to dilute, then add sorbitol, stir to dissolve, and cool to room temperature;

[0083] (2) Dissolve sodium citrate in an appropriate amount of water for injection, slowly add it dropwise to the above solution, adjust the pH to 5.5-6.5, and add water for injection to the full amount;

[0084] (3) Add 0.05% (g / ml) activ...

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Abstract

The invention discloses a sitafloxacin fumarate injection. Additive composition of the injection is simple. But stability is obviously raised under high temperature sterilization and high-light exposure, and the preparation can be effectively avoided from being precipitated out under a low-temperature condition during the storage process. The injection is composed of the following ingredients: sitafloxacin fumarate and methionine are used as main drugs; a cosolvent is one ingredient selected from aspartic acid, citric acid and lactic acid; a pH regulator is one ingredient selected from histidine, sodium citrate or disodium hydrogen phosphate; D-sorbitol is used as an antifreezing agent capable of greatly preventing low-temperature crystallization; and water for injection is also included. The injection can be applied in the form of a small-volume injection, a large-volume infusion or freeze-dried powder injection. During the preparation process of the injection, a specific addition order is applied such that dosage of the cosolvent for dissolving the main drug sitafloxacin fumarate is minimized as much as possible; and with addition of methionine and sorbitol, stability of the injection during high temperature sterilization, high-light exposure and low-temperature storage is raised. The preparation technology of the injection can completely meet industrial production and quality requirements.

Description

technical field [0001] The invention belongs to the technical field of medicines, and relates to a novel fluoroquinolone antibacterial preparation, in particular to a sitafloxacin fumarate injection and a preparation method thereof. Background technique [0002] Sitafloxacin (sitafloxacin) is a broad-spectrum quinolone antibacterial drug developed by Daiichi Sankyo Co., Ltd. (Daiichi Sankyo). Bacteria, mycoplasma and chlamydia all have strong antibacterial activity. [0003] The chemical name of sitafloxacin is 7-[4(S)-amino-6-azaspiro[2,4]heptan-6-yl]-8-chloro-6-fluoro-1-[(1R, 2S)-2-fluorocyclopropyl]-4-oxo-1,4-dihydroquinoline-3-carboxylic acid has the chemical structure shown in the following formula. Since the compound has a cis (1R,5R)-2-fluorocyclopropylamine group in its chemical structure, it has good pharmacokinetic properties and few adverse reactions [0004] . [0005] Studies on the in vitro antibacterial activity of sitafloxacin show that this product has...

Claims

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Application Information

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IPC IPC(8): A61K9/08A61K31/4709A61K47/18A61K47/12A61K47/10A61P31/04
Inventor 闵涛杨勇车晓明朱素华薛峪泉张峰
Owner NANJING YOUKE BIOLOGICAL MEDICAL RES
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