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Azithromycin liposome composition medicine and its prepn process

A kind of technology of azithromycin lipid and azithromycin, which is applied in the field of azithromycin liposome combination medicine and preparation thereof

Inactive Publication Date: 2007-01-03
刘祥华 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] In view of the above-mentioned adverse reactions of existing azithromycin, the present invention provides a combination drug of azithromycin liposome

Method used

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  • Azithromycin liposome composition medicine and its prepn process
  • Azithromycin liposome composition medicine and its prepn process
  • Azithromycin liposome composition medicine and its prepn process

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] The formula used in this embodiment is as follows:

[0041] Azithromycin 1;

[0042] Any ratio mixture of hydrogenated soybean lecithin and egg yolk lecithin

[0043] Mixture 10 with a molar ratio of 8:1 to cephalin;

[0044] A mixture of soybean sterol and cholesterol at a molar ratio of 1:1 10;

[0045] Vitamin E 1;

[0046] PEG2000 0.1;

[0047] α-Mercaptopropionylglycine 0.1;

[0048] The above-mentioned combination medicine uses vitamin C as an excipient, and its added amount is 4% of the total formula.

[0049] Wherein, the azithromycin can be one of azithromycin dihydrogen citrate sodium citrate, azithromycin dihydrogen phosphate, azithromycin lactobionate, azithromycin hydrochloride, azithromycin maleate, azithromycin aspartate, azithromycin sulfate or any combination thereof, which is in the formula The moles of azithromycin are all based on azithromycin.

[0050] The preparation method is as follows:

[0051] 1) A mixture composed of a mixture of hydrogenated soyb...

Embodiment 2

[0061] The formula used in this embodiment is as follows:

[0062] Azithromycin 0.8;

[0063] Any ratio mixture of hydrogenated soybean lecithin and egg yolk lecithin

[0064] Mixture 12 with a molar ratio of 8:1 to cephalin;

[0065] A mixture of soybean sterol and cholesterol at a molar ratio of 1:2 8;

[0066] Vitamin E 1.2;

[0067] PEG2000 0.2;

[0068] α-Mercaptopropionylglycine 0.2;

[0069] The above-mentioned combination medicine uses vitamin C as an excipient, and its addition amount is 8% of the total formula.

[0070] Wherein the azithromycin can be one or any combination of azithromycin dihydrogen citrate sodium citrate, azithromycin dihydrogen phosphate, azithromycin lactobionate, azithromycin hydrochloride, azithromycin maleate, azithromycin aspartate, azithromycin sulfate, and any combination thereof. The number of moles is based on azithromycin.

[0071] The preparation method is as follows:

[0072] 1) A mixture composed of a mixture of hydrogenated soybean lecit...

Embodiment 3

[0081] The formula used in this embodiment is as follows:

[0082] Azithromycin 1.2;

[0083] Any ratio mixture of hydrogenated soybean lecithin and egg yolk lecithin

[0084] Mixture 8 with cephalin 8:1 molar ratio;

[0085] A mixture of soybean sterol and cholesterol at a molar ratio of 1:2 12;

[0086] Vitamin E 0.8;

[0087] PEG2000 0.1;

[0088] α-Mercaptopropionylglycine 0.2;

[0089] The above-mentioned combination medicine uses vitamin C as an excipient, and its added amount is 5% of the total formula.

[0090] Wherein the azithromycin can be one or any combination of azithromycin dihydrogen citrate sodium citrate, azithromycin dihydrogen phosphate, azithromycin lactobionate, azithromycin hydrochloride, azithromycin maleate, azithromycin aspartate, azithromycin sulfate, and any combination thereof. The number of moles is based on azithromycin.

[0091] The preparation method is as follows:

[0092] 6) The mixture of hydrogenated soy lecithin and egg yolk lecithin in any ra...

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Abstract

The present invention relates to azithromycin liposome composition medicine and its preparation process. The azithromycin liposome composition medicine consists of azithromycin 0.8-1.2 (in molar portions, the same below), mixture of hydrogenated soybean lecithin and / or yolk lecithin in 8 to 1 molar ratio 8-12, mixture of soyasterol and cholesterol in 1 to 1-2 molar ratio 8-12, vitamin E 0.8-1.2, PEG2000 0.1-0.2, and alpha-mercapto glycin 0.1-0.2; and has vitamin C in the amount of 4-8 % added as excipient. The present invention also provides the preparation process of the azithromycin liposome composition medicine. The medicine of the present invention has high and stable curative effect and less adverse reactions.

Description

Technical field [0001] The invention relates to an azithromycin liposome combination medicine and a preparation method thereof. Background technique [0002] Azithromycin belongs to the second-generation synthetic derivatives of macrolides, with fast oral absorption and wide tissue distribution. It is characterized by high intracellular concentration and long half-life, and its antibacterial effect on Gram-negative bacteria is stronger than that of erythromycin. The antibacterial effect of Gram-positive bacteria is slightly worse than that of erythromycin. The effect on Mycoplasma pneumoniae is the best among macrolides. It also has a stronger effect on N. burgdorferi than erythromycin. [0003] However, the existing azithromycin preparation products have the following adverse reactions: nausea, vomiting, abdominal pain, diarrhea, etc. of the gastrointestinal tract. Its incidence is related to dose. Skin erythema, pain, and swelling at the injection site may occur during intraven...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K31/7052A61K31/685A61K31/355A61K47/34A61P31/04A61K47/10A61K47/24A61K47/28
Inventor 蔡海德
Owner 刘祥华
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