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Tylonolide liposome and preparation method thereof

A technology of Tedirosin and liposomes, which is applied in liposome delivery, pharmaceutical formulations, medical preparations of non-active ingredients, etc., can solve problems such as difficulty in encapsulation efficiency, achieve good encapsulation efficiency, and improve drug efficiency. Concentration and bioavailability, the effect of not easy to lose

Active Publication Date: 2014-02-19
HENAN SOAR VETERINARY PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the local action time and effect of specific drugs are related to the preparation method of liposomes and the components of liposomes; and for different drug active ingredients, especially for tedirosin, it is necessary to improve the encapsulation of liposomes. rate is also a problem

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] Co-dissolve 500mg soybean lecithin, 100mg cholesterol and 11mg vitamin C palmitate in ethanol, and form a film by rotary evaporation in a water bath at 50°C; dissolve 300mg poloxamer 188 in 10ml of PBS buffer at pH=6 Then, dissolve 100 mg of Tedirosin in the buffer solution; add the prepared solution into the above film, vortex and disperse to obtain a liposome suspension; finally add Zhan soybean into the liposome suspension Sodium bisulfite 0.1% by total weight of lecithin and cholesterol.

[0031] The particle size of the obtained tedirosin liposome is measured by a particle size analyzer to be between 200 and 300 nm; the product is determined to have an encapsulation efficiency of 60% by an ultrafiltration centrifugation method.

Embodiment 2

[0033] 900mg of egg yolk lecithin, 90mg of cholesterol and 6.3mg of vitamin E were co-dissolved in ethanol, and formed into a film by rotary evaporation in a water bath at 30°C; 100mg of poloxamer 188 was dissolved in 5ml of PBS buffer at pH 7.3, Dissolve Tedirosin 180 mg in the buffer solution; then add the prepared solution to the above membrane, vortex and mix, then magnetically stir and homogenize for 1 hour to obtain a liposome suspension; finally in the liposome suspension Add 0.1% sodium sulfite accounting for the total weight of egg yolk lecithin and cholesterol in the liquid.

[0034] The obtained tedirosin liposome particle size is between 80 and 200nm; the encapsulation efficiency of the product is determined to be 70% by ultrafiltration and centrifugation.

Embodiment 3

[0036] A total of 5 mg of soybean lecithin and synthetic phosphatidylserine (weight ratio 20:1), 0.5 mg of cholesterol, and 0.21 mg of vitamin E were dissolved in chloroform, and a film was formed by rotary evaporation in a water bath at 40 ° C; 100 mg of spit Wen 80 was dissolved in 2ml of PBS buffer solution with a pH of 6.5, and then 1 mg of Tedirosin was dissolved in the buffer solution; the prepared solution was added to the above-mentioned film, oscillated to disperse and then stirred and homogenized for 1 hour to obtain lipid body suspension; finally add 0.1% sodium thiosulfate accounting for soybean lecithin, synthetic phosphatidylserine and cholesterol total weight in liposome suspension.

[0037] The obtained tedirosin liposome particle size is between 100-300nm; the encapsulation efficiency measured by the ultrafiltration centrifugation method is 80%.

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Abstract

The invention belongs to the technical field of veterinary drug preparation and discloses a tylonolide liposome and a preparation method thereof. The tylonolide liposome comprises components in parts by weight as follows: 5-10 parts of phospholipid, 0.5-2 parts of cholesterol, 1-2 parts of tylonolide and 0.5-100 parts of an emulsifier. The invention further provides a preparation method of the tylonolide liposome, such as an injection method, an ultrasonic dispersion method, a reverse-phase evaporation method or a film dispersion method. The particle size of a product ranges from 80 nm to 500 nm, so that tylonolide has better light and ordinary temperature stability. The liposome, particularly the product prepared with the film dispersion method, has a better encapsulation efficiency; besides, the drug tylonolide is packed the liposome with specific components, accordingly, the liposome has a better adhesion to a biological film, the drug is not prone to loss and maintains a high concentration locally, the drug concentration and bioavailability of tylonolide are improved, pursuantly, an anti-bacterial effect is enhanced effectively, and the action time of the drug is prolonged due to increase of the retention volume of the drug.

Description

Technical field [0001] The present invention is the field of veterinary drug preparation technology, which involves a new lipid body and its preparation method. Background technique [0002] Tyedo New, English product name: Tylonolide, CAS number is 328898-40-4, the molecular structure is: [0003] , Molecular formula C 41 H 71 N 3 O 8 , Molecular weight 734.02, the melting point is 192 ° C, dissolved in polar organic solvents (such as methanol, acetone, etc.), and the water is slightly soluble.It is the latest animal -dedicated large -cycle beext -alignable antibiotics developed by foreign companies, which are derivatives of Tyladine.On March 8, 2011, the EU Beast Pharmaceutical Committee (CVMP) allowed Inteve's market license applications for Sterilizers (product name Zuprevo) with Tydroxin as the main ingredient, and will subsequently in the EUThe state has been approved to be listed one after another.At present, the high incidence and mortality of respiratory diseases are t...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K31/706A61K47/34A61P31/04
Inventor 孙江宏管倩岳旭龙
Owner HENAN SOAR VETERINARY PHARMA
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