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A 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: 2018-01-02
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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  • A clarithromycin ion-pair lipid microsphere injection and preparation method thereof
  • A clarithromycin ion-pair lipid microsphere injection and preparation method thereof
  • A clarithromycin ion-pair lipid microsphere injection and preparation method thereof

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0093] Embodiment 1 formula 1 clarithromycin content 250mg: 100ml

[0094] Based on 100ml injection

[0095]

[0096] Preparation of clarithromycin ion-pair lipid microsphere injection:

[0097] Step 1: Disperse 2.25g of glycerin for injection and 0.2g of pluronic F-680 in an appropriate amount of water for injection, heat it to 60°C in a magnetic stirrer, and dissolve them completely to obtain an aqueous phase, and keep it warm at 60°C for later use;

[0098] 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;

[0099] Step 3: Preheat 10gMCT at 60°C and use it as the oil phase for later use;

[0100] Step 4:...

Embodiment 2

[0103] Embodiment 2 formula 2 clarithromycin content 100mg: 100ml;

[0104] Based on 100ml injection

[0105]

[0106] Preparation of clarithromycin ion-pair lipid microsphere injection:

[0107] Step 1: Disperse 2.25g of glycerin for injection and 0.2g of pluronic F-680 in an appropriate amount of water for injection, heat it to 60°C in a magnetic stirrer, and dissolve them completely to obtain an aqueous phase, and keep it warm at 60°C for later use;

[0108] 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;

[0109] Step 3: Preheat 10gMCT at 60°C and use it as the oil phase for later use;

[0110] Step 4: ...

Embodiment 3

[0113] Embodiment 3 formula 3 clarithromycin content 500mg: 100ml

[0114] Based on 100ml injection

[0115]

[0116] Preparation of clarithromycin ion-pair lipid microsphere injection:

[0117] Step 1: Disperse 2.25g of glycerin for injection and 0.2g of pluronic F-680 in an appropriate amount of water for injection, heat it to 60°C in a magnetic stirrer, and dissolve them completely to obtain an aqueous phase, and keep it warm at 60°C for later use;

[0118] 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;

[0119] Step 3: Preheat 10gMCT at 60°C and use it as the oil phase for later use;

[0120] Step 4: u...

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Abstract

The invention relates to a method for preparing clarithromycin ion-pair lipid microsphere injection by using cholesterol succinate monoester (CHEMS). Based on 100ml injection, it contains: clarithromycin 0.05g-0.5g; cholesterol succinate monoester 0.3g-0.6g; medium-chain fatty acid triglyceride 10g-20g; soybean oil for injection 0-10g; egg yolk lecithin 0.2g~4g; soybean lecithin 0g~4g; Pluronic F‑68 0.2g~1g; glycerin 2g~5g; water for injection 70g~90g. The physical and chemical properties of the clarithromycin ion-pair lipid microsphere injection of the present invention meet the requirements for intravenous administration, and can withstand high-pressure steam sterilization at 121° C. for 10 minutes. At the same time, this study is the first in the world to apply ion-pairing technology to the preparation of nano-preparations, which improves the transmembrane ability of clarithromycin, reduces bacterial drug resistance, and improves drug efficacy. The samples prepared in this study have good physical and chemical stability in long-term storage, and have little vascular irritation, which can improve patient compliance and curative 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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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/127A61K31/7048A61K47/28A61K47/24A61K47/10A61K47/14A61P31/04
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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