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...

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Problems solved by technology

[0007] The laboratory research of long-acting injections has continuously made breakthroughs, such as microspheres (Microsphere), liposomes (Liposome), emulsions (Emulsion), etc. However, due to the high cost of excipients, the preparation process is complicated and the process is uncontrollable, etc. restricted in production

Most of the long-acting injections on the market currently use polyvinylpyrrolidone (Povidone) to increase the viscosity of the preparation and reduce the diffusion area of ​​the preparation at the administration site, which can delay the release of the drug to a certain extent. Needle (Syringeability) is reduced, the use of large needles may lead to drug outflow from the needle, resulting in reduced dosage, inconvenient clinical medication; Tetracycline injections are usually complexed with metal ions, such as magnesium chloride, magnesium oxide, etc. , to achieve a long-term effect while also improving the stability of the preparation; Suspension (Suspension) is a commonly used dosage form clinically, the drug is dispersed in water, oil or organic solvent, and a drug reservoir can be formed locally after administration , slow release, delaying the absorption process, such as penicillin suspension, etc.; made into salts or esters with low solubility, such as perphenazine made into enanthate and caprate, which significantly increased the maintenance time of effective blood drug concentration, Ed Shi Laboratory Company (CN02819284.2) greatly prolongs the release time of the drug and reduces the toxicity by making tilmicosin into a fatty acid salt

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