Non-irritating clarithromycin freeze-dried powder and preparation method thereof

Abstract

The invention belongs to the technical field of macrolide antibiotic preparation, and particularly relates to non-irritating clarithromycin freeze-dried powder and a preparation method thereof. The clarithromycin freeze-dried powder injection is composed of a clarithromycin liposome and a freeze-drying protective agent, and 18-30 g of the freeze-drying protective agent is added into every 100 mL of a liposome solution; 100 mL of the liposome solution is prepared from the following raw materials: 2.0 g of clarithromycin, 1.8 to 2.2 g of cholesterol sodium sulfate, 6.0 to 6.4 g of lecithin, 0.5to 0.6 g of citric acid, 8 to 20 g of sucrose, 8 to 15 g of glucose and the balance of a phosphate buffer solution. According to the non-irritating clarithromycin freeze-dried powder disclosed by theinvention, the clarithromycin liposome is prepared by adopting the components of the cholesterol sodium sulfate, the lecithin, the citric acid and the clarithromycin, so that the particle size of theliposome can be reduced, the surface charge of the liposome can be increased, the liposome is stable, and the encapsulation efficiency of the liposome is high.

Description

technical field [0001] The invention belongs to the technical field of preparation of macrolide antibiotics, and in particular relates to a non-irritating clarithromycin freeze-dried powder and a preparation method thereof. Background technique [0002] Clarithromycin is a semi-synthetic macrolide antibiotic produced by methylation of the 6-hydroxyl group of erythromycin A. After methylation, clarithromycin can effectively improve its pharmacokinetic properties due to its increased lipid solubility, rapid oral absorption, good cell penetration and wide tissue distribution. The antibacterial mechanism of clarithromycin is to act on the ribosome 50S subunit in the bacterial 70S system, hindering the synthesis of bacterial proteins, and is a long-term antibacterial agent. It has inhibitory effect on Gram-positive bacteria such as Staphylococcus aureus, Streptococcus, pneumococcus, etc., and has inhibitory effect on some Gram-negative bacteria such as Haemophilus influenzae, Bo...

AI Technical Summary

Problems solved by technology

After intravenous injection of clarithromycin common intravenous injection, due to the nature of the drug itself, there is serious vascular irritation, which can cause injection local pain, and in severe cases, it can lead to phlebitis, which makes it difficult for patients to tolerate and affects the clinical application of intravenous injection of the drug. Application and promotion, resulting in the gradual shrinking of the dosage form of some manufacturers

Because clarithromycin is almost insoluble in water, this is a technical problem in the preparation of intravenous injection preparations; in order to solve its solubility problem, the clarithromycin powder injection of Abbott, France uses lactobionic acid and clarithromycin to form a salt to improve its solubility. However, during clinical use, it was found that the incidence of pain at the injection site and phlebitis was high, which greatly limited its clinical application.

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