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Preparation method of small unilamellar vesicle liposome of ivermectin

A technology of small unilamellar liposomes and ivermectin, which is applied in the field of preparation of ivermectin liposomes, can solve the problems of high toxicity of slow-release giant pills, short validity period, and the need for repeated administration, and achieve increased Effects of drug efficacy, uniform distribution, and reduced dosing frequency

Inactive Publication Date: 2010-03-10
INST OF ANIMAL SCI & VETERINARY TIBET ACADEMY OF AGRI & ANIMAL HUSBANDRY SCI
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0003] The technical problem to be solved by the present invention is to solve the problem that the existing ivermectin preparations have a short validity period, need repeated administration, and the toxicity of ivermectin slow-release boluses is high. Plastid preparation method

Method used

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  • Preparation method of small unilamellar vesicle liposome of ivermectin
  • Preparation method of small unilamellar vesicle liposome of ivermectin
  • Preparation method of small unilamellar vesicle liposome of ivermectin

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specific Embodiment approach 1

[0008] Specific embodiment one: the preparation method of ivermectin small unilamellar liposome in the present embodiment is as follows: one, soybean lecithin and cholesterol are dissolved in organic solvent, then add ivermectin former powder, obtain suspension 2. Place the suspension in the reactor and rotate it under reduced pressure at 35°C, 200hpa air pressure and 70r / min to form a thin film on the inner wall of the reactor, stop the rotary evaporation, and then pass nitrogen gas for 10min 3. Dissolve the film obtained in step 2 in a PBS solution with a pH value of 7.0 and let it stand for 1 hour to obtain a mixed solution, put 4 to 5 glass beads, and then place the mixed solution containing the glass beads in a whirlpool In the device, shake and wash the membrane for 1 hour under the conditions of washing membrane shaking speed of 120r / min and water bath temperature of 30°C, and then rest for 1 hour to obtain a milky multilamellar liposome suspension; 4. Milky multilamella...

specific Embodiment approach 2

[0010] Embodiment 2: This embodiment differs from Embodiment 1 in that the particle size of the glass beads described in step 3 is 2 mm to 5 mm. Others are the same as in the first embodiment.

specific Embodiment approach 3

[0011] Specific embodiment three: the method for the encapsulation efficiency of the small unilamellar liposome of ivermectin obtained in the specific embodiment 1 of the present embodiment test is as follows: Place in the inner tube of a centrifugal ultrafiltration tube (the relative molecular weight cut-off is 10KD), centrifuge at a speed of 3000r / min for 30min, then take 1.0mL of ultrafiltrate, dilute to 10mL with mobile phase, and then filter with a 0.22μm filter membrane Two, measure the filtrate of 10 μ L step one gained, adopt the high-performance liquid chromatograph that the model of U.S. Waters Company to produce is 2695 to filtrate parallel determination 3 times, get average value, get free ivermectin content, namely W free 3. Measure 1.0 mL of the gained ivermectin small unilamellar liposomes in the specific embodiment one, then add 2 mL of Triton-X100 ethanol solution with a mass concentration of 5% for ultrasonic demulsification for 10 min, then settle to 10 mL wi...

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Abstract

The invention discloses a preparation method of small unilamellar vesicle liposome of ivermectin, and relates to a preparation method of ivermectin liposome, which solves the problems that the existing ivermectin preparation has short effective date, and needs to deliver drug repeatedly and the sustained release macro-pill of the ivermectin has high toxicity. The method comprises the following steps of: adding raw ivermectin powder in organic solution of soya bean lecithin and cholesterol, then carrying out pressure reduction, rotation and evaporation to the obtained injectable suspension tilla layer of thin film is formed at the inner wall of a reactor, then dissolving the thin film in PBS solution, adding glass beads into a rotary-type oscillator, shaking to wash the film for 1 hour, then standing for 1 hour, and carrying out ultrasonic oscillation so as to obtain the small unilamellar vesicle liposome of ivermectin. The liposome obtained by the preparation method has similar structure as a biofilm, can be biodegraded in the organism, does not generate toxic substances, and can be slowly and continuously released as embedded drug in a storage mode, thus being capable of prolonging effective horizontal period of the drug and reducing drug delivery frequency; and the packet rate of the small unilamellar vesicle liposome of ivermectin is 89.5%.

Description

technical field [0001] The invention relates to a preparation method of ivermectin liposome. Background technique [0002] Ivermectin (Ivermectin, IVM) is a new type of semi-synthetic macrolactone antibiotic anthelmintic produced by the fermentation of Streptomyces avermitilis. Common preparations of mycocin include tablets, pastes, injections, emulsions, sprays, premixes, powders, etc. These dosage forms have a short validity period and require repeated administration, which not only increases labor costs and stress on animals At the same time, it is also easy to produce drug resistance, and even lead to poisoning. The accumulated residues produced in animal tissues after long-term use have a non-negligible impact on ecological balance, and are also harmful to human health. Therefore, it is necessary to develop long-acting sustained-release and Although the existing ivermectin slow-release bolus only needs to be administered once throughout the grazing season, the auxiliar...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K31/7048A61K47/24A61K47/28A61P33/00
Inventor 佘永新巴桑旺堆董禄德何书海拉巴次旦杨德全色珠陈裕祥赵好信
Owner INST OF ANIMAL SCI & VETERINARY TIBET ACADEMY OF AGRI & ANIMAL HUSBANDRY SCI
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