A kind of preparation method of quinolone injection

Abstract

A preparation method of quinolone injection, which relates to a veterinary drug: the injection comprises the following components: quinolone drug or its salt, hydrate 1-30%; fatty acid 0.5-20%; combined with other drugs to increase the antibacterial spectrum 0-30% 30%; blockers, local anesthetics, stabilizers or antioxidants alone or two or more 0-20%; the balance is organic solvents; take quinolone drugs or their salts, fatty acids and organic solvents, heat during stirring After the ingredients are completely dissolved, cool to room temperature, add the combined antibacterial drug, stir until completely dissolved, add activated carbon, stir evenly, and filter through an organic membrane to obtain quinolone long-acting injection; the present invention uses quinolone drug or its salt, hydrate React with fatty acids to form a new composition. The prepared quinolone long-acting injection prolongs the release time of the drug. At the same time, due to the prolongation of the release time, the effective blood concentration of the drug in the body is prolonged, reducing the number of administrations and the stress of the drug. .

Description

Technical field

[0001] The invention relates to a veterinary drug, in particular to a preparation method of quinolone long-acting injection.

Background technique

[0002] Quinolones refer to a class of drugs with a 4-quinolone ring structure. The first-generation quinolones that were first used clinically in 1962 were Nalidixic Acid; the second-generation representative drugs were Pipemidic Acid synthesized in 1974 and Flumequine for animals; In 1978, Norfloxacin, the first drug of the third generation, was synthesized. Because it has a 6-fluoro-7-piperazine-4-quinolone structure, it is also known as fluoroquinolones. For decades, the research progress of quinolones has been very rapid, and there are more than a dozen commonly used clinically. Chlamydia, etc. all have effects; ② strong bactericidal power, it can show strong antibacterial activity at a very low drug concentration in vitro, and has good clinical curative effect; ③ fast absorption, wide distribution in th...

Examples

Embodiment 1

[0038] Preparation and in vitro evaluation of 10% enrofloxacin laurate injection

[0039] Add 10g of enrofloxacin (purified) and 5.6g of lauric acid into 50mL of propylene glycol, stir for 1h until the solution is clear, set the volume to 100mL with ethanol, add 0.3g of activated carbon, stir for 15min, and filter through a 0.45μm organic membrane to obtain 10% Enrofloxacin laurate injection. Take 1mL of injection and put it in a dialysis bag, dialysis conditions: 500mL of pH7.4PBS, 37°C, 100rpm. Respectively at 1h, 4h, 8h, 12h, 24h, 48h, 72h, 96h, 120h, until the concentration changes little. The drug release percentage-sampling time curve is shown as figure 1 As shown, the fitting results show that the in vitro release law of enrofloxacin laurate injection is best fitted by Higuchi equation, the in vitro release half-life is 27.2h, and the in vitro sustainable release is more than 120h.

Embodiment 2

[0041] Preparation of 30% Norfloxacin Stearate Injection

[0042] Take 40mL glycerin formal and 10mL propylene glycol, mix evenly, add 20g stearic acid, heat to 70°C during the stirring process, cool to room temperature after the stearic acid dissolves, add 30g norfloxacin (pure) in small amounts for several times, stir Until clarification, the volume of propylene glycol was adjusted to 100 mL, 0.3 g of activated carbon was added, stirred for 15 min, and filtered through a 0.45 μm organic membrane to obtain 30% norfloxacin stearate injection.

Embodiment 3

[0044] Preparation of 20% Compound Dafloxacin Oleate Injection

[0045] Add 20g of dafloxacin (purified) and 14.7g of oleic acid to 60mL of NMP, add 30g of sulfathiazole and 9.6g of benzyl alcohol, stir for 1h to a clear solution, set the volume of NMP to 100mL, add 0.3g of activated carbon, stir for 15min, 0.45 The 20% compound danofloxacin oleate injection was obtained by filtering with a μm organic membrane.

Technical field

[0001] The invention relates to a veterinary drug, in particular to a preparation method of quinolone long-acting injection.

Background technique

[0002] Quinolones refer to a class of drugs with a 4-quinolone ring structure. The first-generation quinolones that were first used clinically in 1962 were Nalidixic Acid; the second-generation representative drugs were Pipemidic Acid synthesized in 1974 and Flumequine for animals; In 1978, Norfloxacin, the first drug of the third generation, was synthesized. Because it has a 6-fluoro-7-piperazine-4-quinolone structure, it is also known as fluoroquinolones. For decades, the research progress of quinolones has been very rapid, and there are more than a dozen commonly used clinically. Chlamydia, etc. all have effects; ② strong bactericidal power, it can show strong antibacterial activity at a very low drug concentration in vitro, and has good clinical curative effect; ③ fast absorption, wide distribution in th...

Examples

Embodiment 1

[0038] Preparation and in vitro evaluation of 10% enrofloxacin laurate injection

[0039] Add 10g of enrofloxacin (purified) and 5.6g of lauric acid into 50mL of propylene glycol, stir for 1h until the solution is clear, set the volume to 100mL with ethanol, add 0.3g of activated carbon, stir for 15min, and filter through a 0.45μm organic membrane to obtain 10% Enrofloxacin laurate injection. Take 1mL of injection and put it in a dialysis bag, dialysis conditions: 500mL of pH7.4PBS, 37°C, 100rpm. Respectively at 1h, 4h, 8h, 12h, 24h, 48h, 72h, 96h, 120h, until the concentration changes little. The drug release percentage-sampling time curve is shown as figure 1 As shown, the fitting results show that the in vitro release law of enrofloxacin laurate injection is best fitted by Higuchi equation, the in vitro release half-life is 27.2h, and the in vitro sustainable release is more than 120h.

Embodiment 2

[0041] Preparation of 30% Norfloxacin Stearate Injection

[0042] Take 40mL glycerin formal and 10mL propylene glycol, mix evenly, add 20g stearic acid, heat to 70°C during the stirring process, cool to room temperature after the stearic acid dissolves, add 30g norfloxacin (pure) in small amounts for several times, stir Until clarification, the volume of propylene glycol was adjusted to 100 mL, 0.3 g of activated carbon was added, stirred for 15 min, and filtered through a 0.45 μm organic membrane to obtain 30% norfloxacin stearate injection.

Embodiment 3

[0044] Preparation of 20% Compound Dafloxacin Oleate Injection

[0045] Add 20g of dafloxacin (purified) and 14.7g of oleic acid to 60mL of NMP, add 30g of sulfathiazole and 9.6g of benzyl alcohol, stir for 1h to a clear solution, set the volume of NMP to 100mL, add 0.3g of activated carbon, stir for 15min, 0.45 The 20% compound danofloxacin oleate injection was obtained by filtering with a μm organic membrane.

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