A kind of fluoroquinolone pharmaceutical composition

A fluoroquinolone and composition technology, which is applied in the field of veterinary fluoroquinolone pharmaceutical compositions, can solve the problems of difficult preparation, complex preparation process, necrosis of injection sites, etc., and achieves simple and easy operation of the preparation method, increased therapeutic effect, and drug content. improved effect

A fluoroquinolone and composition technology, which is applied in the field of veterinary fluoroquinolone pharmaceutical compositions, can solve the problems of difficult preparation, complex preparation process, necrosis of injection sites, etc., and achieves simple and easy operation of the preparation method, increased therapeutic effect, and drug content. improved effect

CN103830240BActive Publication Date: 2016-07-06LUOYANG HUIZHONG ANIMAL MEDICINE

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  • A kind of fluoroquinolone pharmaceutical composition
  • A kind of fluoroquinolone pharmaceutical composition
  • A kind of fluoroquinolone pharmaceutical composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment approach

[0017] The enrofloxacin used in the present invention was purchased from Zhejiang Guobang Pharmaceutical Co., Ltd., with a content of 98.5%, and batch number 120222-1; the enrofloxacin hexahydrate was prepared by Luoyang Huizhong Veterinary Medicine Co., Ltd. according to CN101961335A Example 1, with a content of 75.0%, batch number 20120102; Ciprofloxacin was purchased from Zhejiang Guobang Pharmaceutical Co., Ltd., with a content of 96.7%, batch number 111020-21.

[0018] Examples 1-15 prepared according to the technical solution of the present invention are shown in Table 1:

[0019] Table 1

[0020]

[0021]

[0022]

[0023] Note: The content of enrofloxacin hexahydrate is calculated by enrofloxacin.

[0024] Preparation:

[0025] Add the prescribed amount of enrofloxacin (or enrofloxacin hexahydrate, ciprofloxacin), co-solvent, water and antioxidants to an appropriate amount of organic solvent according to the above prescriptions, stir until completely dissolv...

Embodiment 16

[0026] Embodiment 16 comparative example composition

[0027] According to the Chinese patent CN101810569A, Example 1 discloses a preparation method of enrofloxacin injection comprising the following steps:

[0028] (1) Add 20 grams of enrofloxacin into 60ml of aqueous sodium hydroxide solution with a concentration of 0.4mol / l, and stir until the enrofloxacin is completely dissolved;

[0029] (2) Continue to add sodium hydroxide aqueous solution with a concentration of 0.4mol / l to adjust the pH value to 12;

[0030] (3) Add 20ml of acidulant lactic acid. During the addition of acidulant, enrofloxacin will first crystallize. With the addition of acidulant, when the pH value reaches neutral, enrofloxacin will completely dissolve;

[0031] (4) Add 0.5g sodium thiosulfate antioxidant to the neutral solution;

[0032] (5) Continue to add 0.5g of EDTA chelating agent;

[0033] (6) After step (5) is completed, dilute to 100ml with purified water, and filter the dilute solution thr...

Embodiment 17、15

[0036] Embodiment 17, 15% enrofloxacin injection

[0037] Enrofloxacin injection, each 100ml injection consists of the following ingredients: 15.2g enrofloxacin, an appropriate amount of 4% (w / v) sodium hydroxide aqueous solution, add water to 100ml.

[0038] Preparation method: Weigh 15.2g of enrofloxacin, suspend it in 50ml of water, add dropwise an appropriate amount of 4% (w / v) sodium hydroxide aqueous solution while stirring, adjust the pH value to 10, and dilute the water to 100ml.

[0039] The 15% enrofloxacin injection prepared in this example was placed at room temperature for 3 hours, and crystals were precipitated.

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Abstract

The invention provides a fluoroquinolone pharmaceutical composition, each 100ml pharmaceutical composition contains: fluoroquinolone 10g-30g, cosolvent 0.1g-20g, water 0g-60g, and the balance is an organic solvent, wherein the cosolvent is A pharmaceutically acceptable acidic cosolvent. The fluoroquinolone drug content in the fluoroquinolone pharmaceutical composition provided by the invention is greatly improved, greatly increasing the therapeutic effect of a single administration; using an organic solvent as the main solvent, compared with conventional enrofloxacin injection, it reduces the intramuscular injection irritation; the prepared fluoroquinolone pharmaceutical composition has stable properties and no crystallization during long-term storage; the preparation method is simple and easy to operate, and is easy to realize industrialized large-scale production.

Description

technical field [0001] The invention relates to a veterinary fluoroquinolone pharmaceutical composition. Background technique [0002] Fluoroquinolones have obvious after-drug effects on Gram-positive bacteria and Gram-negative bacteria, and it is concentration-dependent, that is, the higher the drug concentration, the longer the after-drug effect. With the increasing dosage of clinical use, the concentration of enrofloxacin injection has gradually developed from the initial 0.5% (g / ml) to the current 10% (g / ml). Because enrofloxacin has very little solubility in water and is easily soluble in sodium hydroxide solution, the prior art mainly adopts the method of adding co-solvent sodium hydroxide to increase the concentration of enrofloxacin in the preparation of enrofloxacin injection. Solubility in water, taking into account the stability of the product and the best conditions for enrofloxacin to produce bactericidal effect, control the pH value to 9.5-10.5 (Chinese Veteri...

Claims

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Application Information

Patent Timeline
06 Jul 2016
Publication
CN103830240B
IPC
A61K31/496; A61K9/08; A61K47/10; A61K47/08; A61P31/04
Inventors
张许科; 刘兴金