Preparation method of ceftiofur acid long-acting injection

A technology for ceftiofur and injection, which can be applied to medical preparations with non-active ingredients, medical preparations containing active ingredients, and pharmaceutical formulas, etc., and can solve the problems of reduced production economic benefits, high viscosity of preparations, and difficulty in injection. , to achieve the effects of low production and treatment costs, long half-life of intramuscular injection, and simple preparation process

Inactive Publication Date: 2013-08-07
QINGDAO AGRI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Clinical routine preparations mainly include ceftiofur sodium freeze-dried powder, which needs to be injected once a day. The stress caused by frequent injections has a certain impact on the therapeutic effect, and the growth of animals is inhibited to varying degrees, resulting in economic benefits. Reduced; the existing domestic ceftiofur long-acting suspension injection Using solid dispersion technology and using hydrogenated castor oil as a slow-release carrier, the long-acting preparation of ceftiofur hydrochloride was prepared by emulsification of organic reagents. The addition of organic reagents enhances the toxicity of the preparation, and the preparation is layered. Shake well before use, which may easily lead to uneven injection ; Imported ceftiofur long-acting preparations are mostly used by Pfizer Animal Health of the United States This product uses ceftiofur acid to prepare ceftiofur crystalline free acid. Although it overcomes the short half-life of ceftiofur intramuscular injection, the preparation has local irritation, and the single point injection should not exceed 2mL. Shake well before use, and the preparation has a high viscosity , injection is relatively difficult, and its price is high, reducing the economic benefits of production

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0012] The concrete process steps of present embodiment preparation ceftiofuric acid long-acting injection are:

[0013] (1) Put 0.50 g of ceftiofur acid and 1.40 g of 2-hydroxypropyl-β-cyclodextrin into a ball mill and mix them evenly, grind them at room temperature for 15 minutes, mix well and sieve to obtain ceftiofur acid inclusion compound ;

[0014] (2) Dissolve 0.01g of sodium alginate in 6g of sterile water, add 2.00g of poloxamer 407 and 0.25g of poloxamer 188, store in a refrigerator at 4°C for 24 hours to completely dissolve, and then autoclave at 121°C. Cool in an ice bath to obtain a transparent solution;

[0015] (3) Magnetically stir the transparent solution at 4°C and 150r / min, add 1.90g of ceftiofur acid inclusion compound to fully disperse the ceftiofur acid inclusion compound, and add sterile water after the dispersion is uniform. Make up to 10mL.

[0016] The percentage by weight of each component of the ceftiofuric acid injection prepared in this exampl...

Embodiment 2

[0018] The preparation process of this embodiment is the same as that of Example 1, and the weight percentages of each component in the product injection are 10% for ceftiofuric acid, 20% for 2-hydroxypropyl-β-cyclodextrin, and 20% for poloxamer. 407 is 25%, poloxamer 188 is 4%, sodium alginate is 0.3%, and the rest is sterile water, the total is 100%.

[0019] Pharmacokinetic studies of the ceftiofuric acid long-acting injection prepared in this example after intramuscular injection in the neck triangle of Laoshan dairy goats showed that, with 5 mg / kg body weight of ceftiofuric acid long-acting injection The half-life is 17.13h, and the minimum bactericidal blood concentration of 0.2μg / mL can be maintained for at least 48h. Ceftiofuric acid long-acting injection has a long elimination half-life and bactericidal maintenance time, and high bioavailability; pharmacodynamic test on clinical pullorum of piglets It shows that the prepared ceftiofur acid long-acting injection 5mg / kg...

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Abstract

The invention belongs to the technical field of preparation of medicines and in particular relates to a preparation method of ceftiofur acid long-acting injection. The preparation method comprises the followings steps of: adding ceftiofur acid and 2-hydroxypropyl-beta-cyclodextrin in a molar ratio of 1:(1-2) to a ball mill for uniformly mixing; sufficiently grinding under the room temperature, and sufficiently uniformly and sieving to obtain a ceftiofur acid clathrate compound; dissolving sodium alginate in sterile water and adding poloxamer 407 and poloxamer 188, storing for 12-24 hours under the temperature condition of 4 DEG C, so that the poloxamer 407 and the poloxamer 188 are completely dissolved and sterilized under the temperature of 121 DEG C, carrying out ice-bath cooling to obtain a transparent solution; magnetically stirring under the temperature condition of 4 DEG C and the rotation speed condition of 150r/min; adding the ceftiofur acid clathrate compound in a weight ratio of the sodium alginate to the ceftiofur acid clathrate compound of (0.1-0.3):(5-10), so that the ceftiofur acid clathrate compound is sufficiently dispersed uniformly to obtain the ceftiofur acid long-acting injection. According to the preparation method of the ceftiofur acid long-acting injection, the preparation process is simple, the product intramuscular injection half-life period is long, the dissolution degree of the ceftiofur acid is high, the production and treatment cost is low, the cure rate is high and the environment is friendly.

Description

Technical field: [0001] The invention belongs to the technical field of medicine preparation, and relates to a preparation method of ceftiofuric acid long-acting injection, which adopts the combination of cyclodextrin inclusion technology and temperature-sensitive in-situ gel slow-release technology to provide a new type of cefotaxime The production process of Fu long-acting injection. Background technique: [0002] Ceftiofur is a third-generation antibiotic for animals. The prototype of ceftiofur is ceftiofur acid, which is insoluble in water. Ceftiofur sodium salt is easily soluble in water. It has poor stability after dissolution and needs to be used immediately for injection. It is prepared now and has a short half-life after injection, so frequent administration is required; ceftiofur hydrochloride, namely ceftiofur hydrochloride, is insoluble in water and is often used to prepare ceftiofur hydrochloride long-acting suspension injection. Clinical routine preparations m...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/08A61K47/40A61K47/34A61K47/36A61K31/546A61P31/04
Inventor 刘焕奇高存帅曲志娜刘萌萌赵思俊
Owner QINGDAO AGRI UNIV
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