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Doramectin O/W type injection taking water as matrix and preparation method thereof

A doramectin and injection technology, which is applied in the directions of non-active ingredients medical preparations, medical preparations containing active ingredients, and pharmaceutical formulas, can solve the problems of insoluble in water, poor stability, etc., and achieve fluidity Good, reduced pain, good safety

Active Publication Date: 2013-12-04
LANZHOU INST OF ANIMAL SCI & VETERINARY PHARMA OF CAAS
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This method solves the shortcomings of doramectin, which is extremely difficult to dissolve in water and has poor stability, and at the same time reduces the toxic and side effects of traditional oil agents

Method used

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  • Doramectin O/W type injection taking water as matrix and preparation method thereof

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] Embodiment 1: the preparation of the O / W type doramectin injection that content is 0.1%~5%:

[0028] 1) Weigh each drug component: 37.5 grams of OP emulsifier, 12.5 grams of PEG400, 10.0 grams of ethyl oleate, 5.0 grams of doramectin, and place them in a brown triangular flask. Stir for 0.2h until the doramectin is completely dissolved and the system is uniform, transparent and clear.

[0029] 2) Slowly add water for injection into the solution under stirring conditions. With the increase of the amount of water for injection, the solution system first becomes relatively viscous. When the water for injection reaches 25g, the system suddenly becomes thinner and the fluidity increases. It is completely transparent. When the amount of water for injection reaches 35 grams, the content of doramectin is 5% O / W type doramectin injection. At this time, the content of other various excipients is also as high as 60%. The content is high, the toxic and side effects are large, and ...

Embodiment 2

[0032] Embodiment 2: Determination of 1% O / W type doramectin injection

[0033]The content of the prepared 1% O / W doramectin injection was determined by HPLC, using Waters high performance liquid chromatography series; Luna C18 (3μm) 4.6 mm × 150 mm chromatography; Waters510 type infusion Pump; TM480 type fluorescence detector; U6 K type injection valve; AST type data processor; 3800 type printer. The mobile phase is acetonitrile: methanol: glacial acetic acid (64:32:4), flow rate 1 mL / min; column temperature (30.0 ± 0.5) ℃; excitation wavelength 383 nm, emission wavelength 447 nm, injection volume: 20 μl.

[0034] Preparation of reference substance solution: Accurately weigh doramectin reference substance: 0.0100 g, dissolve it in mobile phase and configure it to a concentration of 100.0 μg / ml as a stock solution. Precisely measure 0.2, 0.6, 1.0, 3.0, 6.0, 10.0 μl of the above stock solutions, put them in 10ml volumetric flasks respectively, add mobile phase to constant vol...

Embodiment 3

[0038] Embodiment 3: acute toxicity test result

[0039] (1) Acute toxicity test results of 0.1% O / W doramectin injection

[0040] 30 Kunming mice and 30 Wistar rats (clean grade), male and female, were purchased from the Experimental Animal Center of Lanzhou University, license number: SCXK (Gan) 2009-0004; After intraperitoneal injection of 0.1% O / W type doramectin injection with the content of doramectin original drug (10mg / kg) body weight dose, continuous observation for 7 days, no toxic and side effects were found, and the large and small mice had smooth coat and moved freely , normal diet, and no death during the test period. The test results show that 0.1% O / W doramectin injection has the maximum tolerated dose of LD for intraperitoneal injection in mice and mice. 0 That is to say, if the dose is greater than 10g / kg body weight without death, then its half lethal dose LD 50 The value must be greater than the dose, that is, greater than 10g / kg body weight. Therefore, a...

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Abstract

The invention discloses a doramectin O / W (oil in water) type injection taking water as the matrix and a preparation method thereof. The O / W type injection is composed of OP emulsifier, PEG 400, ethyl oleate, doramectin, and injection water. The key point of the invention is the determination of formula of the injection and the content of each component. The injection mainly takes water as the matrix, comprises a little organic solvent, reduces affection of organic solvent on livestock, poultry and environment, does little harm to producers and users, is safer in storage and transportation, has little by-effect on livestock and poultry, and solves the problems of harms to livestock and poultry and pollution to environment, which are generated during the production and use processes of the conventional dosage form (oil dosage).

Description

[0001] technical field [0002] The invention belongs to the field of veterinary medicines, and relates to medicines for treating nematodes and arthropods outside livestock and poultry, in particular to a water-based doramectin O / W injection and a preparation method thereof. [0003] Background technique [0004] Doramectin (DOR for short) is a new macrolide antibiotic, the third-generation derivative of Avermectins (ivermectin is the second generation), and it and Ivemectin The deworming mechanism of Bacterin is the same, and they are all realized by strengthening the effect of r-aminobutyric acid (GABA). GABA is an inhibitory neurotransmitter. In the brain, GABA mainly inhibits post-synaptic nerve conduction, and the release of GABA The increase means that the normal resting position of the post-synaptic cells can be improved, it is difficult for the nerves to transmit stimulation to the muscles, the muscles cannot contract, and the parasites are paralyzed and expelled. I...

Claims

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Application Information

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IPC IPC(8): A61K9/107A61K31/7048A61K47/34A61P33/10A61P33/14
Inventor 周绪正张继瑜李冰李剑勇魏小娟牛建荣杨亚军刘希望李金善
Owner LANZHOU INST OF ANIMAL SCI & VETERINARY PHARMA OF CAAS
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