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A quinolone and injection technology, which is applied in the field of preparation of quinolone long-acting injection, can solve the problems of inconvenient clinical medication, reduced dosage of administration, and reduced acupuncture, and can solve the phenomenon of peaks and troughs of blood drugs and prolong the release time. , the effect of prolonging the dosing cycle
Active Publication Date: 2010-04-07
PU LIKE BIO ENG
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[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
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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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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...
Claims
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Application Information
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