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Macrolide antibiotic long-circulation emulsion and preparation method thereof

A macrolide and antibiotic technology, applied in the field of pharmacy, can solve the problems of inability to kill intracellular surviving bacteria, difficult to achieve intracellular enrichment, low effective utilization rate, etc., so as to improve effective utilization rate and reduce clinical dosage. , the effect of high biocompatibility

Inactive Publication Date: 2020-07-03
GUANGZHOU HANFANG PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] The purpose of the present invention is to overcome the traditional way of administration of macrolide antibiotics ① rapid metabolism in the body, less infection sites, and low effective utilization rate; ② large dose, long-term administration, serious adverse reactions ; ③ Difficult to achieve intracellular enrichment, unable to kill intracellular surviving bacteria; ④ Problems such as antibiotic resistance

Method used

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  • Macrolide antibiotic long-circulation emulsion and preparation method thereof
  • Macrolide antibiotic long-circulation emulsion and preparation method thereof
  • Macrolide antibiotic long-circulation emulsion and preparation method thereof

Examples

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Effect test

Embodiment 1

[0039] In a kind of macrolide antibiotic long circulation emulsion of the present embodiment, every 1000mL emulsion contains:

[0040]

[0041] The preparation method of a kind of macrolide antibiotic long circulation emulsion of the present embodiment is:

[0042] (1) Weigh the prescribed amount of refined egg yolk lecithin, azithromycin palmitate, and PEGylated phospholipids, add an appropriate amount of ethanol, stir at 60°C to dissolve the emulsifier, after it is completely dissolved, add the prescribed amount of refined soybean oil, and evaporate through rotary evaporation Ethanol was removed to give an oily phase.

[0043] (2) Weigh the prescription amount of stearylamine, glycerin and polysorbate 80, add appropriate amount of water for injection, heat and stir at 60°C to dissolve or disperse evenly, and use it as the water phase for later use.

[0044] (3) Add the oil phase to the water phase, shear at 5000 rpm / min for 10 min, and the shear temperature is 60° C. to ...

Embodiment 2

[0052] In a kind of macrolide antibiotic long circulation emulsion of the present embodiment, every 1000mL emulsion contains:

[0053]

[0054] The preparation method of a kind of macrolide antibiotic long circulation emulsion of the present embodiment is:

[0055] (1) Weigh the prescribed amount of refined soybean lecithin, azithromycin laurate, and PEGylated to synthesize phospholipids, add an appropriate amount of ethanol, stir at 70°C to dissolve the emulsifier, after completely dissolving, add the prescribed amount of refined soybean oil and medium chain oil, And the ethanol was removed by rotary evaporation to obtain an oil phase.

[0056] (2) Weigh the prescribed amount of DOTAP, glycerin and poloxamer 188, add an appropriate amount of water for injection, heat and stir at 70°C to dissolve or disperse evenly, and use it as the water phase for later use.

[0057] (3) Add the oil phase to the water phase, shear at 7000 rpm / min for 15 min, and the shear temperature is ...

Embodiment 3

[0064] In a kind of macrolide antibiotic long circulation emulsion of the present embodiment, every 1000mL emulsion contains:

[0065]

[0066] The preparation method of a kind of macrolide antibiotic long circulation emulsion of the present embodiment is:

[0067] (1) Weigh egg yolk phosphatidylcholine, azithromycin caprylate, PEG to synthesize phospholipids, add appropriate amount of ethanol, stir at 75°C to dissolve the emulsifier, after complete dissolution, add refined soybean oil and medium chain oil, and Ethanol was removed by rotary evaporation to give an oil phase.

[0068] (2) Weigh the prescription amount of stearylamine, glycerin and polysorbate 80, add an appropriate amount of water for injection, heat and stir at 75°C to dissolve or disperse evenly, and use it as the water phase for later use.

[0069] (3) Add the oil phase to the water phase, shear at 8000 rpm / min for 20 min, and the shear temperature is 75° C. to obtain colostrum.

[0070] (4) The prepared...

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Abstract

The invention belongs to the technical field of foods, and discloses a macrolide antibiotic long-circulation emulsion and a preparation method thereof. The macrolide antibiotic long-circulation emulsion comprises the following components in percentage by mass of 0.1%-1% of macrolide antibiotics, 10-30% of an oil solvent, 0.5-5% of an emulsifying agent, 0.2-5% of a co-emulsifier, 0.3-5% of a potential adjusting agent, 1-5% of an osmotic pressure adjusting agent and the balance water for injection. The emulsifying agent comprises synthesis phospholipid of PEG. According to the macrolide antibiotic long-circulation emulsion and the preparation method thereof, the problems of adverse reactions and drug tolerance caused by an administration route of traditional macrolide antibiotics are solved,and besides, the antibacterial effect of the macrolide antibiotics in part of strains can be increased.

Description

technical field [0001] The invention relates to the technical field of pharmacy, in particular to a macrolide antibiotic long-circulation emulsion and a preparation method thereof. Background technique [0002] Macrolides are weak alkaline antibiotics produced by Streptomyces, containing a 14- or 16-membered ring with a lactone structure, and have a strong inhibitory effect on Streptococcus pneumoniae. Its main mechanism of pharmacological action is to act on the 50S subunit of bacterial ribosomes, block bacterial protein synthesis and messenger ribonucleic acid translocation, and have good effects on atypical pathogenic bacteria such as Chlamydia, Mycoplasma, Legionella and Helicobacter pylori antibacterial effect. At present, the formulations of macrolide antibiotics on the market are mostly granules, dispersible tablets, sustained-release tablets, and dry suspensions. In addition, due to the poor solubility and low absorption and utilization rate of macrolide antibiotic...

Claims

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Application Information

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IPC IPC(8): A61K9/107A61K31/704A61K47/54A61K47/24A61P31/04
CPCA61K9/0019A61K9/1075A61K31/704A61K47/24A61K47/542A61P31/04
Inventor 李遥刘春芳袁诚唐顺之许文东牛亚伟傅玉萍彭万才王国财牟肖男满兴战莫嘉伟
Owner GUANGZHOU HANFANG PHARMA
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