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Compound gentamicin sulphate in-situ gel for injection and preparation method thereof

A technology of gentamicin sulfate and in-situ gel, which is applied to medical preparations with non-active ingredients, medical preparations containing active ingredients, and pharmaceutical formulas, etc. Taking medicine, time-consuming and troublesome problems, etc., to achieve good pharmacological effects, reduce the number of administrations, and simple preparation process

Inactive Publication Date: 2013-10-09
NANJING AGRICULTURAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Since most medicines have a certain taste, the administration of drinking water or ingredients (orally) is limited to a certain extent, and due to illness, the animal's appetite and drinking desire decrease or even refuse to eat and drink, which affects the oral intake of medicine, and then affects the curative effect; Conventional injection preparations often need to be administered several times in a course of treatment. Frequent injections and holding animals are time-consuming and troublesome, and can easily cause animal stress and aggravate the condition, or even cause new diseases, affecting the efficacy of the drug and the outcome of the disease.

Method used

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  • Compound gentamicin sulphate in-situ gel for injection and preparation method thereof
  • Compound gentamicin sulphate in-situ gel for injection and preparation method thereof
  • Compound gentamicin sulphate in-situ gel for injection and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0029] Compound gentamicin sulfate in situ gel for injection (each mL contains gentamicin 90,000 units, TMP60mg)

[0030]

[0031] Preparation method: Take propylene glycol, add appropriate amount of water for injection, heat to 50-60°C, add TMP, dissolve with appropriate amount of lactic acid, then add gentamicin sulfate, sodium benzoate, sodium bisulfite, stir to dissolve; the selected gel Sprinkle the matrix and sodium carboxymethyl cellulose on the above liquid surface, refrigerate at 4°C for more than 24 hours, until a clear, lump-free, uniformly dispersed solution is obtained, dilute to volume with water for injection, stir evenly, filter through micropores, and dispense .

[0032] The prepared in situ gel was evaluated in vitro, including gelation temperature, gelation time, thermal reversibility, release rate, viscosity, pH value, etc. The measurement methods of each item are as follows, the measurement results are shown in Table 1, and the in vitro release results...

Embodiment 2

[0040] Compound gentamicin sulfate in situ gel for injection (each mL contains gentamicin 90,000 units, TMP60mg)

[0041]

[0042] Preparation method: Take propylene glycol, add appropriate amount of water for injection, heat to 50-60°C, add TMP, add appropriate amount of lactic acid to dissolve, add gentamicin sulfate, sodium benzoate, sodium metabisulfite, stir to dissolve; the selected gel matrix and poly Sprinkle vitamin K-30 on the above-mentioned liquid surface, refrigerate at 4°C for more than 24 hours, until a clear, lump-free, uniformly dispersed solution is obtained, dilute to volume with water for injection, stir evenly, filter through micropores, and divide into packages. The in vitro performance evaluation method is the same as that in Implementation 1. The results are shown in Table 1, and the in vitro release results are shown in the accompanying drawings.

Embodiment 3

[0044] Compound gentamicin sulfate in situ gel for injection (each mL contains gentamicin 90,000 units, TMP60mg)

[0045]

[0046]

[0047] Preparation method: Take propylene glycol, add appropriate amount of water for injection, heat to 50-60°C, add TMP, add appropriate amount of lactic acid to dissolve, add gentamicin sulfate, sodium benzoate, sodium pyrosulfite, stir to dissolve; sprinkle the selected gel base on On the above liquid surface, refrigerate at 4°C for more than 24 hours until a clear, lump-free, uniformly dispersed solution is obtained, dilute to volume with water for injection, stir evenly, filter through micropores, and divide into packages. The in vitro performance evaluation method is the same as that in Implementation 1. The results are shown in Table 1, and the in vitro release results are shown in the accompanying drawings.

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Abstract

The invention belongs to the field of animal pharmaceutical preparations, and relates to a compound gentamicin sulphat in-situ gel preparation for injection and a preparation method thereof. The in-situ gel preparation disclosed by the invention comprises the following components in parts by weight: 9.0 parts of gentamicin (9 million units), 6.0 parts of TMP (Trimethoprim), 15.5-30.5 parts of P407, 0.5-10.5 parts of P188, 30.0-90.5 parts of water, 0.01-10.0 parts of polymer blocker, 5.0-45.0 parts of solubilising stabilizer, 0.01-3.0 parts of preservative, 0.01-5.0 parts of antioxygen and a proper amount of pH adjustor. The in-situ gel preparation disclosed by the invention is freely moveable liquid at room temperature and forms semi-solid gel after drug delivery through intramuscular injection or subcutaneous injection; drug delivery is only carried out once during a treatment course; the in-situ gel preparation has the advantages of steady property, long drug delivery duration, exact curative effect, strong animal adaptation, no toxic and side effects and adverse reaction and the like, and is simple to operate and convenient for drug delivery; the in-situ gel preparation disclosed by the invention has broad-spectrum antibacterial activity and can be used as a medicine for preventing and treating diseases of pigs, sheep, dogs, cats, cattle and the like.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations for animals, and relates to a compound gentamicin sulfate in-situ gel for injection with a suitable phase transition temperature and a preparation method thereof. Background technique [0002] C obtained from the culture medium of Micromonospora gentamicin (Gentamicin) 1 、C 1a and C 2 The antibacterial activity and toxicity of the three components of the complex were basically the same. Gentamicin Sulfate is white or off-white powder; odorless; hygroscopic; easily soluble in water, insoluble in ethanol, acetone, chloroform or ether; pH value of 4% aqueous solution is 4.0-6.0. [0003] Gentamicin sulfate is an aminoglycoside antibiotic, which has a strong inhibitory effect on a variety of Gram-negative bacteria and positive bacteria. It has a strong effect on negative bacteria such as Pseudomonas aeruginosa, Escherichia coli, Proteus, Shigella, Haemophilus, Pseudomonas aeruginosa, Sal...

Claims

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Application Information

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IPC IPC(8): A61K31/7036A61K9/06A61K47/34A61P31/04A61K31/505
Inventor 余祖功耿智霞郭凡溪李会敏
Owner NANJING AGRICULTURAL UNIVERSITY
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