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
CN104771362BActive Publication Date: 2018-01-02SHENYANG PHARMA UNIVERSITY
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
SHENYANG PHARMA UNIVERSITY
Publication Date
2018-01-02

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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.
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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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