Preparation method for carbostyril injection

Abstract

The invention relates to a preparation method for a carbostyril injection, in particular to a veterinary medicament. The injection comprises the following components: 1 to 30 percent of a carbostyril medicament or salt and hydrate thereof,, 0.5 to 20 percent of fatty acid, 0 to 30 percent of other medicaments combined to augment antimicrobial spectrum, 0 to 20 percent of one or more than two of blocker, local anesthesia, a stabilizing agent and an antioxidant, and the balance of an organic solvent. The preparation method comprises the following steps of: taking the carbostyril medicament or the salt thereof, the fatty acid and the organic solvent; heating until all the components are dissolved in the process of stirring; cooling to the room temperature; adding the combined antimicrobial medicament; stirring until all the components are dissolved; adding activated carbon; evenly stirring; and carrying out organic film filtration to obtain the carbostyril long-acting injection. A novel composition is formed through the reaction of the carbostyril medicament or the salt and the hydrate thereof with the fatty acid. The medicament release time of the prepared carbostyril long-acting injection is prolonged, and the time of maintaining effective blood concentration of the medicament in vivo is prolonged because the release time is prolonged so as to reduce administration times and stress of the medicament.

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...

AI Technical Summary

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

Images