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Tilmicosin liposome preparation and preparation method thereof

A technology of liposome preparation and tilmicosin, which is applied in the direction of liposome delivery, pharmaceutical formulations, medical preparations containing active ingredients, etc., can solve the problems of kidney toxicity, cardiotoxicity, toxic side effects, etc., and achieve stability Good, high encapsulation efficiency, stable drug loading effect

Inactive Publication Date: 2009-05-06
ZHEJIANG KING TECHINA TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although tilmicosin has a very definite curative effect on respiratory diseases of livestock and poultry, as a newly synthesized chemical drug, it has relatively toxic side effects, which may cause cardiotoxicity and renal toxicity

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0042] Weigh 10 mg tilmicosin, 200 mg soybean lecithin (purity>76% phosphatidylcholine) and 50 mg cholesterol, dissolve them in ether, mix them well, place the solution in a ground-mouthed round-bottomed flask, and place it in a constant temperature water bath at 35°C. Use a rotary evaporator to evaporate the organic solvent under the condition of 100rpm and reduced pressure, so that the film-forming materials such as phospholipids form a uniform lipid film at the bottom of the flask; add 20ml of ether to the above lipid film to dissolve, and add 10ml of pH7.4 phosphoric acid Salt buffer solution, ultrasonic emulsification in a water bath, remove the organic solvent with a rotary evaporator at 35°C, until it becomes a milky white liposome suspension, high-pressure emulsification or micro-jet to reduce the particle size. 100 mg of trehalose was dissolved in liposomes, after sterile filtration (membrane filter pore size 0.2 μm), the final dispersion was divided into vials, and th...

Embodiment 2

[0044] Weigh 20mg of tilmicosin, 400mg of soybean lecithin (purity>76% phosphatidylcholine) and 100mg of cholesterol and dissolve them in ether, mix well, place the solution in a ground-mouthed round-bottomed flask, and place it in a constant temperature water bath at 35°C. Use a rotary evaporator to evaporate the organic solvent under the condition of 100rpm and reduced pressure, so that the film-forming materials such as phospholipids form a uniform lipid film at the bottom of the flask; add 20ml of ether to the above lipid film to dissolve, and add 10ml of pH7.4 phosphoric acid Salt buffer solution, ultrasonic emulsification in a water bath, remove the organic solvent with a rotary evaporator at 35°C, until it becomes a milky white liposome suspension, high-pressure emulsification or micro-jet to reduce the particle size. 200 mg trehalose was dissolved in liposomes, after sterile filtration (membrane filter pore size 0.2 μm), the final dispersion was divided into vials, and ...

Embodiment 3

[0046] Weigh 30mg of tilmicosin, 600mg of soybean lecithin (purity>76% phosphatidylcholine) and 150mg of cholesterol and dissolve them in ether, mix well, place the solution in a round-bottomed flask with a constant temperature of 35°C Use a rotary evaporator to evaporate the organic solvent under the condition of 100rpm and reduced pressure, so that the film-forming materials such as phospholipids form a uniform lipid film at the bottom of the flask; add 20ml of ether to the above lipid film to dissolve, and add 10ml of pH7.4 phosphoric acid Salt buffer solution, ultrasonic emulsification in a water bath, remove the organic solvent with a rotary evaporator at 35°C, until it becomes a milky white liposome suspension, high-pressure emulsification or micro-jet to reduce the particle size. 300 mg trehalose was dissolved in liposomes, after sterile filtration (membrane filter pore size 0.2 μm), the final dispersion was divided into vials, and then freeze-dried or spray-dried.

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Abstract

The invention relates to a Tilmicosin lipidosome preparation and a preparation method. The Tilmicosin lipidosome preparation consists of the Tilmicosin lipidosome and the acceptable vector of a medicament; wherein, the Tilmicosin lipidosome contains Tilmicosin, phospholipid and cholesterin with the weight ratio of 1 : 2 to100 : 1 to 15; the acceptable vector of the medicament comprises an internal buffer system, alkali used for regulating pH, and a frozen-dried supporting agent; the adding amount of the frozen-dried supporting agent calculated according to the weight ratio of the phospholipid is as follows: 0.2 to 4 portions of the frozen-dried supporting agent is added into one portion of the phospholipid; the adding amount of the internal buffer system is 5 to 15mL. The invention has the advantages that: the Tilmicosin content in the unit volume of the Tilmicosin lipidosome preparation is high; the envelop rate is high; the stability is good; moreover, the medicament-loading rate is stable. The medicament in the lipidosome is continuously released, thus remarkably improving the concentration of blood medicament and prolonging the circulating time of the medicament in the blood. The Tilmicosin lipidosome preparation improves the curative effect of the medicament and enhances the clinic usability of the medicament.

Description

technical field [0001] The invention relates to a liposome preparation and a preparation method, mainly a tilmicosin liposome preparation and a preparation method. Background technique [0002] Tilmiosin is a macrolide antibiotic for animals semi-synthesized from tylosin, which was originally successfully developed by Eli Lilly and Company of the United States. Due to its unique antibacterial activity and special pharmacokinetic characteristics, it has been approved abroad for infectious diseases caused by sensitive bacteria in pigs, poultry, cattle, sheep and other animals, especially respiratory tract infections in livestock and poultry. Although tilmicosin has a very definite curative effect on respiratory diseases of livestock and poultry, as a newly synthesized chemical drug, it has relatively toxic side effects, which may cause cardiotoxicity and renal toxicity. According to relevant studies, the damage of tilmicosin to the cardiovascular system is mainly due to the d...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K31/706A61P31/04
Inventor 金一王成润朱颖李浙烽
Owner ZHEJIANG KING TECHINA TECH
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