Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

Tulathromycin liposome and preparation method thereof

The technology of tyramectin lipid and tyramectin is applied in the field of tyramectin liposome and its preparation, and can solve the problems of hindering the popularization and application of tyramectin, low bioavailability and the like

Active Publication Date: 2014-08-27
HENAN SOAR VETERINARY PHARMA
View PDF3 Cites 6 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, telamectin is insoluble in water, and its bioavailability is low, which hinders the popularization and application of telamectin

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0018] Embodiment 1: Determination of basic process conditions

[0019] (1) Preparation of blank liposomes (film method)

[0020] Take the lipid material and add absolute ethanol, stir and dissolve in a 65°C water bath, remove the ethanol by rotary evaporation to form a thin film; add citrate-sodium citrate buffer solution with a pH value of 4.0 for hydration, and stir at 65°C for 20 minutes to obtain a blank lipid The primary product of the liposome; after the blank liposome product was ultrasonically treated for 8min (200w×2min, 400w×6min), it was passed through the microporous membranes of 0.8μm, 0.45μm and 0.22μm in turn to obtain the blank Liposome suspension (control the final mass concentration of phospholipids to be 50 mg / mL).

[0021] (2) Prepare gradient liposomes and incubate drug loading

[0022] Take 1.0 mL of the above blank liposome suspension, add sodium phosphate solution (alkali, pH gradient regulator) with a concentration of 500 mmol / L, adjust the pH ...

Embodiment 2

[0031] Embodiment 2: the influence of ethanol residual amount on liposome

[0032] Lipid material composition: Distearoylphosphatidylcholine 3g

[0033] Cholesterol l g

[0034] Distearoylphosphatidylglycerol modified with polyethylene glycol 1000 0.5g

[0035] Dihydrocholesterol 0.5g

[0036] Weighed 8 groups of the above-mentioned lipid materials and dissolved them in absolute ethanol. The amount of ethanol in each group was 2.5%, 5.0%, 10%, 15%, 20%, 25%, 30% and 40% medium volume ratio); add 300 mmol / L citrate-sodium citrate buffer solution with pH=4.0, the final mass concentration of phospholipids is 50 mg / mL, stir in 65°C water bath for 20 min, and obtain blank liposome primary product; After the primary probe was sonicated for 8 min (200 w × 2 min, 400 w × 6 min), it was passed through 0.8 μm, 0.45 μm, and 0.22 μm microporous membranes in sequence to obtain a blank liposome suspension.

[0037] Adopt laser particle size me...

Embodiment 3

[0040] Example 3 Preparation of Tyramectin Liposomes by Spray Drying

[0041] 3.1 Preparation of lipid material mixed powder: mix HSPC, CHOL and PEG2000-DSPE according to the mass ratio of 3:1, dissolve with ethanol to obtain a clear solution, and obtain lipid powder after spray drying (tert-butanol can also be used to dissolve each lipid Components, lipid powder obtained by freeze-drying method).

[0042] 3.2 Prepare blank liposomes: hydrate the above-mentioned lipid powder with 300mM ammonium sulfate solution at 50-65°C, shear and disperse to obtain multilocular liposomes with uneven particle sizes; add different amounts of absolute ethanol, and use Microfluidic equipment reduces the particle size of liposomes (approximately 80nm) and prepares liposomes containing different concentrations of ethanol.

[0043] 3.3 Preparation of gradient liposomes: the ammonium sulfate in the outer water phase of the liposomes is removed by ion exchange resin / fiber.

[0044] 3.4 Drug load...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

PropertyMeasurementUnit
Particle sizeaaaaaaaaaa
Molecular weightaaaaaaaaaa
Login to View More

Abstract

The invention belongs to the technical field of pharmacy, and provides a tulathromycin liposome which comprises tulathromycin and a lipid material; the lipid material comprises phospholipid, and the weight ratio of the tulathromycin to the phospholipid is 1:1-20. The invention also provides a corresponding preparation method which comprises the following steps: 1) dissolving the lipid material in ethanol, and preparing a blank liposome suspension by a film dispersion method, an injection method, a reverse evaporation method, or a spray-drying method; 2) preparing gradient liposome; 3) adding an ethanol solution of tulathromycin, controlling the ethanol content of the system to be less than 15 V%, performing incubation at 45-75 DEG C for 2-60 min to obtain a tulathromycin-containing liposome suspension. Liposome is encapsulated by tulathromycin, which effectively improves the bioavailability of tulathromycin. The ethanol content is controlled in the preparation method, which contributes to the acquisition of higher encapsulation efficiency and appropriate particle size.

Description

technical field [0001] The invention belongs to the technical field of pharmacy, and in particular relates to telamectin liposome and a preparation method thereof. Background technique [0002] Tyramectin is a macrolide super antibiotic, which is currently on the market in the United States, the European Union, and many countries in Asia and Latin America. Due to its excellent pharmacokinetic model, telamectin can provide long-term drug effects, which provides a revolutionary method and method for veterinarians and producers to control respiratory diseases in nursery and fattening pigs in pig production. A whole new standard. However, telamectin is insoluble in water and its bioavailability is low, which hinders the popularization and application of telamectin. [0003] Liposome is a new type of pharmaceutical preparation with targeted drug delivery function. In general, liposomes are formed by the aggregation of phospholipid molecules suspended in aqueous solution. The ...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
IPC IPC(8): A61K9/127A61K9/19A61K9/14A61K31/7052A61P31/04
Inventor 孙江宏蒋增海郭建军张军强
Owner HENAN SOAR VETERINARY PHARMA
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com