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In-situ gel for ceftiofur injection and preparation method thereof

A technology of ceftiofur and in-situ gel, which is applied in the directions of non-active ingredients medical preparations, active ingredients-containing medical preparations, pharmaceutical formulas, etc. Simple, slow-release effect

Pending Publication Date: 2021-03-19
ZHENGZHOU BARY ANIMAL PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, both ceftiofur hydrochloride injection and ceftiofur injection are oil preparations, which have the disadvantage of being more irritating than water preparations.

Method used

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  • In-situ gel for ceftiofur injection and preparation method thereof
  • In-situ gel for ceftiofur injection and preparation method thereof
  • In-situ gel for ceftiofur injection and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] Ceftiofur solid dispersion prescription:

[0030]

[0031] The preparation of ceftiofur solid dispersion: (1) take stearic acid, soybean lecithin and cholesterol of prescription quantity and melt at 70 ℃, add the ceftiofur of prescription quantity, stir evenly; (2) put in -20 ℃ quickly (3) low-temperature pulverization to obtain ceftiofur solid dispersion.

[0032] In situ gel preparation prescription for injection:

[0033]

[0034]

[0035] The preparation method of in situ gel for ceftiofur injection:

[0036] Step 1: Take the prescribed amount of ceftiofur solid dispersion, methylcellulose and poloxamer 188 and mix evenly, then add 80% of the prescribed amount to water, and stir until the poloxamer 188 is completely dissolved.

[0037] Step 2: Take the prescribed amount of poloxamer 407 and add it to step 1, stir until a lump-free and uniformly dispersed medicinal solution is obtained, add water to make up the volume, and the product is ready.

[0038] I...

Embodiment 2

[0047] Ceftiofur solid dispersion prescription:

[0048]

[0049] The preparation of ceftiofur solid dispersion: (1) take glycerol monostearate, hydrogenated soybean lecithin and cholesterol of prescription quantity and melt at 85 ℃, add the ceftiofur of prescription quantity, stir evenly; (2) place rapidly Cooling and solidification at -20°C; (3) Low-temperature pulverization to obtain a solid dispersion of ceftiofur.

[0050] In situ gel preparation prescription for injection:

[0051]

[0052] Preparation:

[0053] The preparation method of in situ gel for ceftiofur injection:

[0054] Step 1: Take the prescribed amount of ceftiofur solid dispersion, povidone K30 and poloxamer 188, mix evenly, add 80% of the prescribed amount to water, stir until the poloxamer 188 is completely dissolved, and the ceftiofur solid is dispersed The body is evenly dispersed.

[0055] Step 2: Take the prescribed amount of poloxamer 407 and add it to step 1, stir until a lump-free and u...

Embodiment 3

[0058] Ceftiofur solid dispersion prescription:

[0059] Ceftiofur 200.0g

[0060] Glyceryl Palmitate 350.0g

[0061] Soy Sterol 100.0g

[0062] Preparation:

[0063] Preparation of ceftiofur solid dispersion: (1) Take glyceryl palmitate and soy sterol of the prescription amount and melt at 80°C, add the ceftiofur in the prescription amount, and stir evenly; (2) rapidly place at -20°C Cooling and solidification; (3) low-temperature pulverization to obtain a solid dispersion of ceftiofur.

[0064] In situ gel preparation prescription for injection:

[0065]

[0066] The preparation method of in situ gel for ceftiofur injection:

[0067] Step 1: Take the prescribed amount of ceftiofur solid dispersion, hydroxypropyl methylcellulose and poloxamer 188 and mix evenly, add 80% of the prescribed amount to water, stir until the poloxamer 188 is completely dissolved, and the cefotaxime The furan solid dispersion is uniformly dispersed.

[0068] Step 2: Take the prescribed amo...

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Abstract

The invention belongs to the technical field of pharmaceutical preparations for animals, and relates to in-situ gel for ceftiofur injection and a preparation method thereof. The in-situ gel for ceftiofur injection comprises a ceftiofur solid dispersion, a temperature-sensitive in-situ gel matrix, a polymer retardant and water for injection, wherein the temperature-sensitive in-situ gel matrix is composed of poloxamer 407 and poloxamer 188. The in-situ gel for ceftiofur injection specifically comprises the following components in percentage by mass of 4-20 percent of the ceftiofur solid dispersion, 12-28 percent of the poloxamer 407, 0.2-10 percent of the poloxamer 188, 0.05-5 percent of the polymer retardant and the balance of the water for injection. According to the invention, the soliddispersion is combined with the in-situ gel for injection, so that the gelling strength of the in-situ gel is increased, the corrosion of the in-situ gel can be obviously delayed, and the slow releaseeffect is more obvious.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations for animals, and relates to an in-situ gel for ceftiofur injection and a preparation method thereof. Background technique [0002] Ceftiofur is an off-white to light yellow powder. Slightly soluble in acetone, almost insoluble in water or ethanol, its sodium salt is hygroscopic and easily soluble in water; its hydrochloride is white or off-white crystalline powder, in N,N-dimethylacetamide Soluble in medium, slightly soluble in methanol, insoluble in water. [0003] Ceftiofur belongs to the third-generation cephalosporins for animals, which has a spectrum bactericidal effect. It has strong activity against Gram-positive bacteria (including producing β-lactamase) and Gram-negative bacteria. The sensitive bacteria are mainly Pasteurella multocida, Pasteurella hemolyticus, Actinobacillus pleuropneumoniae, Salmonella, Escherichia coli, Streptococcus, Staphylococcus and so on. T...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/06A61K31/546A61K47/26A61P31/04A61P11/00A61P15/14A61K9/127
CPCA61K31/546A61K9/0019A61K47/26A61K9/06A61P31/04A61P11/00A61P15/14A61K9/127Y02A40/70
Inventor 余祖功周衡王亚丽杨亚婷康玉霞路向阳张凤
Owner ZHENGZHOU BARY ANIMAL PHARMA
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