Doramectin injection and preparation method thereof

A doramectin and injection technology, which can be used in pharmaceutical formulations, medical preparations with non-active ingredients, and medical preparations containing active ingredients, etc., can solve the problems of unstable preparations, difficult application, poor water solubility, etc. Improve solubility, broad application prospects, and the effect of not easy precipitation

Inactive Publication Date: 2015-04-08
SHANGHAI TONGREN PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Doramectin is currently an excellent antiparasitic drug, and the research on its preparation has also made some progress. However, due to its poor water solubility, it is often added with strong irritating organic solvents such as cosolvents when producing injections. , so there is a certain irritation in clinical application
And its formulation is also unstable, and has certain difficulties in application

Method used

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  • Doramectin injection and preparation method thereof
  • Doramectin injection and preparation method thereof
  • Doramectin injection and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] Weigh each raw material with the following mass percentage (take the total amount as 100mL as an example):

[0025]

[0026] Take the prescribed amount of ethyl oleate, glyceryl triacetate, benzyl benzoate and 20% injection oil, heat to 60°C, and purging with nitrogen at the same time; add the prescribed amount of doramectin and BHA, stir to dissolve, quickly Cool to room temperature; add the prescribed amount of phenol, stir evenly, add soybean oil to the prescribed amount, and stir evenly.

Embodiment 2

[0028] Weigh each raw material with the following mass percentage (take the total amount as 100mL as an example):

[0029]

[0030] Take the prescribed amount of ethyl oleate, glyceryl triacetate, benzyl benzoate and 20% oil for injection, heat to 60°C, and purging with nitrogen at the same time; add the prescribed amount of doramectin and BHT, stir to dissolve, and quickly Cool to room temperature; add the prescribed amount of phenol, stir evenly, add castor oil to the prescribed amount, and stir evenly.

Embodiment 3

[0032] Weigh each raw material with the following mass percentage (take the total amount as 100mL as an example):

[0033]

[0034] Take the prescribed amount of ethyl oleate, glyceryl triacetate, benzyl benzoate and 20% injection oil, heat to 60°C, and purging with nitrogen at the same time; add the prescribed amount of doramectin and BHA, stir to dissolve, quickly Cool to room temperature; add the prescribed amount of benzyl alcohol, stir evenly, add soybean oil to the prescribed amount, and stir evenly.

[0035] Observe the appearance of the doramectin injection obtained in the above examples, and carry out the determination of moisture and content, and the results are shown in Table 1.

[0036] Table 1

[0037] Example

character

Moisture (%)

Content (%)

1

Light yellow clear oily liquid

0.46

100.5

2

Light yellow clear oily liquid

0.51

99.9

3

Light yellow clear oily liquid

0.49

101.3

...

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PUM

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Abstract

The invention relates to a doramectin injection. The doramectin injection is characterized by comprising the following ingredients in percentage by mass: 0.1% of doramectin, 10-40% of ethyl oleate, 2-5% of glycerol triacetate, 5-10% of benzyl benzoate, 1-10% of preservative, and 0.005-0.5% of antioxidant, wherein injection oil is added to 100%. The invention further provides a preparation method of the doramectin injection. With the adoption of the doramectin injection and the preparation method disclosed by the invention, ethyl oleate and the injection oil are used as a solvent of doramectin; meanwhile, glycerol triacetate and benzyl benzoate are added as a mixed solvent, thus improving the solubility of doramectin and enabling doramectin to be not easy to separate out. The problems that the prepared injection is easy to separate out and not stable enough are avoided, and the improvement of the stability of a medicine preparation is promoted; moreover, the injection is simple in preparation process, cheap and easily available in raw materials, and suitable for industrialized mass production, thus having a wide application prospect.

Description

technical field [0001] The invention relates to the field of veterinary medicine, in particular to veterinary drugs, in particular to a doramectin injection and a preparation method thereof. Background technique [0002] Doramectin is a new generation of macrolide anti-parasitic drug developed in the 1990s. It uses cyclohexanecarboxylic acid (Cyclohexanecarboxylic acid) as a precursor, and through genetic recombination of Streptomyces avermitilis ( Streptomycete avermitilis) is an avermectin antibiotic fermented by a new strain of ivermectin. It has the same deworming mechanism as ivermectin, and it is achieved by strengthening the effect of γ-aminobutyric acid (GABA). GABA is a An inhibitory neurotransmitter. In the brain, GABA mainly inhibits post-synaptic nerve conduction. The increase in GABA release increases the normal resting potential of postsynaptic cells, making it difficult for nerves to transmit stimulation to muscles, making muscles unable to contract, and causi...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/08A61K31/7048A61K47/14A61P33/10A61P33/14A61P33/00
Inventor 何林华方玮秦佳琪
Owner SHANGHAI TONGREN PHARM CO LTD
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