Veterinary valnemulin, novel liposome formulation of the salt thereof and preparation method thereof
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A technology of warnimulin and liposomes, which is applied in the direction of liposome delivery, active ingredients of esters, antibacterial drugs, etc., can solve the problems of lack of drug liposome preparations, and the number of varieties is too small, so as to reduce the dosage The effect of drug frequency, improvement effect, and prolongation of action time
Active Publication Date: 2012-01-11
BEIJING DABEINONG ANIMAL HEALTH TECH +1
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Problems solved by technology
However, there are few related studies on veterinary liposome preparations at home and abroad, and the research on veterinary liposome preparations is mainly based on anti-parasites, trace elements, and nutritional drugs, and the number of varieties is relatively small, especially the lack of antibiotics. and digestive system drug liposome preparations
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Embodiment 1
[0030] The preparation of embodiment 1 warnemulin hydrochloride liposome
[0031] 1) Dissolve 1000mg of lecithin and 100mg of cholesterol in 20ml of chloroform, place in a round bottom flask,
[0032] On a rotary evaporator, dry by vacuum evaporation until a dry thin layer;
[0033] 2) Dissolve 150mg of warnemulin hydrochloride in 25ml of PBS;
[0034] 3) Add warnemulin hydrochloride PBS solution into the flask, shake and hydrate to obtain warnemulin hydrochloride liposomes.
Embodiment 2
[0035] The preparation of embodiment 2 warnimulin liposomes
[0036] 1) Dissolve 2000mg of lecithin and 100mg of cholesterol in 20ml of chloroform-ether (1:1, V / V), and place in a round bottom flask;
[0037] 2) Dissolve 40mg of warnemulin in 20ml of PBS solution;
[0038] 3) Add the PBS solution of Vernemulin into the flask, carry out ultrasonic emulsification for 3min, and then evaporate under reduced pressure. After reaching the colloidal state, add 5ml of PBS solution dropwise, and continue to evaporate under reduced pressure, that is, the liposome of Vernemulin .
Embodiment 3
[0039] The preparation of embodiment 3 warney muulin phosphate liposomes
[0040] 1) Dissolve 1000mg of soybean lecithin and 150mg of cholesterol in 30ml of ether and place in a beaker;
[0041] 2) Dissolving 2000mg of warnemulin phosphate in 25ml of PBS solution;
[0042] 3) Under heating and stirring at 60°C, inject the PBS solution of warnemulin phosphate, and continue stirring until the diethyl ether is completely evaporated to obtain the warnemulin phosphate liposome.
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Abstract
The invention relates to veterinary valnemulin, a novel liposome formulation of the salt thereof and a preparation method thereof, which belongs to the field of veterinary antibiotic preparations. In the preparation, valnemulin and the salt thereof serve as the main components, phospholipid and cholesterol serve as membranes, and the common liposomes, the lung targeting liposomes or the long circulating liposomes of valnemulin or valnemulin salt can be prepared. The valnemulin and the liposomes of the salt thereof have better tissue selectivity compared with the common preparation, are effective to the bacterial and mycoplasma infection in cells, and can reduce the toxic and side effect. The lung targeting liposomes targets the medicine to the lung, and has significant effect to the mycoplasma infection of the lung, bacterial infection and the like, and reduces the toxic and side effect. The long circulating liposomes significantly improves the circulation time of the liposomes in thebody, so that the medicines displays the efficacy for a longer time more effectively, so s to reduce the delivery times and the dosage.
Description
technical field [0001] The invention belongs to the field of veterinary antibiotic preparations, and relates to a new liposome dosage form of warnemulin and its salt and a preparation method thereof. Background technique [0002] Valnemulin and its salts are a new bag of pleuromutilin semi-synthetic antibiotics, which belong to diterpenes and belong to the same class of drugs as tiamulin. They are animal-specific antibiotics and are mainly used to prevent and treat pigs, Mycoplasmosis and Gram-positive bacterial infections in cattle, sheep and poultry. In 1999, it was approved by the European Community for the prevention and treatment of swine dysentery caused by Brachyspira hyodysenteriae infection and swine enzootic pneumonia caused by Mycoplasma pneumoniae infection. It is the first veterinary drug premix approved in Europe. Classified as a prescription drug for veterinary use. [0003] Ordinary preparations of warnemulin, such as: premixes, injections, etc. After admin...
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