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Clarithromycin ion pair lipid microsphere injection and preparation method thereof

A technology of clarithromycin and lipid microspheres, applied in liposome delivery, pharmaceutical formulations, medical preparations of non-active ingredients, etc., can solve the problems of clarithromycin irritation, low solubility, and difficulty in development, etc. Achieve the effects of reducing vascular irritation, improving antibacterial activity, reducing pain and vascular irritation

Active Publication Date: 2015-07-15
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0015] The technical problem to be solved by the present invention is that clarithromycin itself has poor water solubility, the solubility in water is 1:1000, and has a certain fat solubility; not only that, but its low solubility in oil also determines that it is difficult to develop it into an injection , even if it is made into common injections by a certain process, most of them are unstable; and it has been reported that clarithromycin has a great irritant deficiency during intravenous infusion. Method for ion-pair lipid microsphere injection

Method used

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  • Clarithromycin ion pair lipid microsphere injection and preparation method thereof
  • Clarithromycin ion pair lipid microsphere injection and preparation method thereof
  • Clarithromycin ion pair lipid microsphere injection and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0094] Embodiment 1 formula 1 clarithromycin content 250mg: 100ml

[0095] Based on 100ml injection

[0096]

[0097] The rest is water for injection;

[0098] Preparation of clarithromycin ion-pair lipid microsphere injection:

[0099] Step 1: Disperse 2.25g of glycerin for injection and 0.2g of pluronic F-68 in an appropriate amount of water for injection, heat it to 60°C in a magnetic stirrer to dissolve them all, and prepare the water phase, keep it warm at 60°C for later use;

[0100] Step 2: Dissolve 4 g of egg yolk lecithin, 0.25 g of clarithromycin, and 0.325 g of cholesterol succinate monoester with an appropriate amount of absolute ethanol, remove the ethanol by rotary evaporation, and blow dry with nitrogen. Hydrate the obtained phospholipid dry film with the aqueous phase prepared in step 1 at 60° C. for 30 min to obtain a clarithromycin liposome coarse dispersion system for subsequent use;

[0101] Step 3: Preheat 10gMCT at 60°C and use it as the oil phase f...

Embodiment 2

[0105] Embodiment 2 formula 2 clarithromycin content 100mg: 100ml;

[0106] Based on 100ml injection

[0107]

[0108] The rest is water for injection

[0109] Preparation of clarithromycin ion-pair lipid microsphere injection:

[0110] Step 1: Disperse 2.25g of glycerin for injection and 0.2g of pluronic F-68 in an appropriate amount of water for injection, heat it to 60°C in a magnetic stirrer to dissolve them all, and prepare the water phase, keep it warm at 60°C for later use;

[0111] Step 2: Dissolve 4 g of egg yolk lecithin, 0.1 g of clarithromycin, and 0.13 g of cholesterol succinate monoester with an appropriate amount of absolute ethanol, remove the ethanol by rotary evaporation, and blow dry with nitrogen. Hydrate the obtained phospholipid dry film with the aqueous phase prepared in step 1 at 60° C. for 30 min to obtain a clarithromycin liposome coarse dispersion system for subsequent use;

[0112] Step 3: Preheat 10gMCT at 60°C and use it as the oil phase for...

Embodiment 3

[0116] Embodiment 3 formula 3 clarithromycin content 500mg: 100ml

[0117] Based on 100ml injection

[0118]

[0119] The rest is water for injection;

[0120] Preparation of clarithromycin ion-pair lipid microsphere injection:

[0121] Step 1: Disperse 2.25g of glycerin for injection and 0.2g of pluronic F-68 in an appropriate amount of water for injection, heat it to 60°C in a magnetic stirrer to dissolve them all, and prepare the water phase, keep it warm at 60°C for later use;

[0122] Step 2: Dissolve 4 g of egg yolk lecithin, 0.5 g of clarithromycin, and 0.65 g of cholesterol succinate monoester with an appropriate amount of absolute ethanol, remove the ethanol by rotary evaporation, and blow dry with nitrogen. Hydrate the obtained phospholipid dry film with the aqueous phase prepared in step 1 at 60° C. for 30 min to obtain a clarithromycin liposome coarse dispersion system for subsequent use;

[0123] Step 3: Preheat 10gMCT at 60°C and use it as the oil phase for...

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Abstract

The present invention relates to a method for preparation of a clarithromycin ion pair lipid microsphere injection from cholesteryl hemisuccinate (CHEMS). Every 100 ml of the injection comprises 0.05-0.5g of clarithromycin; 0.3-0.6g of cholesteryl hemisuccinate; 10g-20g of medium chain fatty acid triglyceride; 0-10g of injection soybean oil; 0.2g-4g of egg yolk lecithin; 0-4g of soybean lecithin; 0.2g-1g of Pluronic F-68; 2g-5g of glycerol; and 70g-90g of injection water. The physicochemical properties of the clarithromycin ion pair lipid microsphere injection conform to the requirements of intravenous medication, and the clarithromycin ion pair lipid microsphere injection can tolerate 10 min of high-pressure steam sterilization at 121 DEG C. At the same time, the ion pair technology is used in preparation of a nano preparation for the first time in the world, the clarithromycin transmembrane ability is improved, bacterial drug resistance is reduced, and the drug efficacy is improved. The sample prepared in the study is good in long-term storage physical and chemical stability, and small in vascular irritation, can improve the compliance of patients and improves the therapeutic effect.

Description

Technical field: [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to a method for preparing clarithromycin ion-pair lipid microsphere injection by using cholesterol succinate monoester (CHEMS). Background technique: [0002] The chemical name of clarithromycin (clarithromycin, CLA) is 6-O-methyl erythromycin, so it is also called clarithromycin. Oxygen substituted. Erythromycin is the first successfully developed macrolide antibiotic, and it is also its representative drug. However, erythromycin has a poor effect on Gram-negative bacteria, and it is easy to make these bacteria develop tolerance; it is also unstable under acidic conditions, has low blood and urine drug concentrations, and has large gastrointestinal side effects. In the past ten years, people have realized that erythromycin has a good effect on the increasingly popular Gram-positive bacteria, including drug-resistant Staphylococcus aureus and mycoplasma, chl...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K31/7048A61K47/28A61K47/44A61P31/04
Inventor 唐星耿思聪张宇何海冰林霞张岩刘玉歆
Owner SHENYANG PHARMA UNIVERSITY
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