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Clarithromycin ion pair lipidosome injection and preparation method thereof

A technology of clarithromycin and liposome, which is applied in the field of preparing clarithromycin ion-pair liposome injection, can solve the problems of clarithromycin irritation, poor water solubility, low solubility, etc. Toxicity, the effect of enhancing antibacterial activity

Active Publication Date: 2014-12-03
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0021] 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 liposome injection

Method used

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  • Clarithromycin ion pair lipidosome injection and preparation method thereof
  • Clarithromycin ion pair lipidosome injection and preparation method thereof
  • Clarithromycin ion pair lipidosome injection and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0095] Example 1 Formula 1 clarithromycin content 250mg: 100ml

[0096] Based on 100ml injection

[0097]

[0098]

[0099] The rest is water for injection;

[0100] Preparation of clarithromycin ion-pair liposome injection:

[0101] Step 1: Na 2 HPO 4 12H 2 O0.29g, NaH 2 PO 4 2H 2 O0.13g, KH 2 PO 4 Disperse 0.02g, 0.8g of NaCl, and 0.02g of KCl in 100mL of water for injection, dissolve them all, and prepare the water phase, keep it warm at 60°C for later use;

[0102] Step 2: Dissolve egg yolk lecithin 4.5g, clarithromycin 0.25g, cholesterol succinate monoester 0.325g, and MPEG-DSPE 0.5g with an appropriate amount of absolute ethanol, remove the ethanol by rotary evaporation, and blow dry with nitrogen; The phospholipid dry film was hydrated with the aqueous phase prepared in step 1 at 60°C for 30 minutes to obtain the clarithromycin liposome coarse dispersion system, which was set aside;

[0103] Step 3: Transfer the liposome coarse dispersion system to a hi...

Embodiment 2

[0106] Example 2 Formula 2 clarithromycin content 100mg: 100ml;

[0107] Based on 100ml injection

[0108]

[0109] The rest is water for injection;

[0110] Preparation of clarithromycin ion-pair liposome injection:

[0111] Step 1: Na 2 HPO 4 12H 2 O0.29g, NaH 2 PO 4 2H 2 O0.13g, KH 2 PO 4 Disperse 0.02g, 0.8g of NaCl, and 0.02g of KCl in 100mL of water for injection, dissolve them all, and prepare the water phase, keep it warm at 60°C for later use;

[0112] Step 2: Dissolve egg yolk lecithin 4.5g, clarithromycin 0.1g, cholesterol succinate monoester 0.13g, and MPEG-DSPE 0.5g with an appropriate amount of absolute ethanol, remove the ethanol by rotary evaporation, and blow dry with nitrogen; The phospholipid dry film was hydrated with the aqueous phase prepared in step 1 at 60°C for 30 minutes to obtain the clarithromycin liposome coarse dispersion system, which was set aside;

[0113] Step 3: Transfer the liposome coarse dispersion system to a high-pressure h...

Embodiment 3

[0116] Example 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 liposome injection:

[0121] Step 1: Na 2 HPO 4 12H 2 O0.29g, NaH 2 PO 4 2H 2 O0.13g, KH 2 PO 4 Disperse 0.02g, 0.8g of NaCl, and 0.02g of KCl in 100mL of water for injection, dissolve them all, and prepare the water phase, keep it warm at 60°C for later use;

[0122] Step 2: Dissolve egg yolk lecithin 4.5g, clarithromycin 0.5g, cholesterol succinate monoester 0.65g, and MPEG-DSPE 0.5g with an appropriate amount of absolute ethanol, remove the ethanol by rotary evaporation, and blow dry with nitrogen; The phospholipid dry film was hydrated with the aqueous phase prepared in step 1 at 60°C for 30 minutes to obtain the clarithromycin liposome coarse dispersion system, which was set aside;

[0123] Step 3: Transfer the liposome coarse dispersion system to a high-pressure homo...

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Abstract

The invention relates to a method for preparing clarithromycin ion pair lipidosome injection from cholesteryl hemisuccinate (CHEMS). Every 100ml of injection comprises 0.05-0.8g of clarithromycin, 0.3-1.0g of cholesteryl hemisuccinate, 0.8-5g of high-purity yolk lecithin, 0.05-0.5g of MPEG-DSPE, 0.2-0.4g of Na2HPO4.12H2O, 0.1-0.2g of NaH2PO4.2H2O, 0.01-0.03g of KH2PO4, 0.7-0.9g of NaCl, 0.01-0.03g of KCl and 70-90g of injection water. The physicochemical property of clarithromycin ion pair lipidosome injection meets the vein medicine requirements. Meanwhile the method adopts an ion pair technique to prepare nano preparations in the world for the first time, the transmembrane capability of clarithromycin is improved, bacterial drug resistance is degraded, and the medicine effect is improved. A sample prepared by using the method is good in physical and chemical stability after being stored for a long time, irritation to blood vessels is small, the patient compliance is improved, and the curative effect is improved.

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 liposome 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, chlamydia an...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K31/7048A61K47/34A61K47/48A61P31/04
Inventor 唐星耿思聪张宇何海冰林霞张岩黄成龙
Owner SHENYANG PHARMA UNIVERSITY
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