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

A technology of clarithromycin and clarithromycin lipid, applied in the field of macrolide antibiotic preparation, can solve the problems affecting the clinical application and promotion of intravenous injections, high incidence of phlebitis, shrinking dosage form, etc. Insoluble, reduced dosing frequency, stable effect at room temperature

Active Publication Date: 2022-08-02
ZIBO VOCATIONAL INST
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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.

Method used

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

Examples

Experimental program
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Effect test

Embodiment 1

[0027] The non-irritating clarithromycin freeze-dried powder described in this example 1 is composed of clarithromycin liposome and a freeze-drying protective agent, and 25 g of the freeze-dried protective agent is added to each 100 mL of liposome solution; The plastid solution is prepared from the following raw materials: 2.0 g of clarithromycin, 2.0 g of sodium cholesteryl sulfate, 6.0 g of lecithin, 0.6 g of citric acid, 15 g of sucrose, 10 g of glucose, and the balance is phosphate buffer solution.

[0028] The preparation method of the non-irritating clarithromycin freeze-dried powder described in the present embodiment 1, consists of the following steps:

[0029] (1) Dissolve clarithromycin, sodium cholesteryl sulfate, lecithin and citric acid in absolute ethanol to obtain an oil phase, and keep the temperature at 70°C for 30min;

[0030] (2) the dehydrated alcohol in the oil phase is removed by rotary evaporation, and then blown dry with nitrogen to obtain a film;

[0...

Embodiment 2

[0038] The non-irritating clarithromycin freeze-dried powder described in this example 2 is composed of clarithromycin liposome and a freeze-drying protective agent, and 18 g of the freeze-dried protective agent is added to each 100 mL of liposome solution; The plastid solution is prepared from the following raw materials: 2.0 g of clarithromycin, 2.2 g of sodium cholesteryl sulfate, 6.2 g of lecithin, 0.5 g of citric acid, 10 g of sucrose, 8 g of glucose, and the balance is phosphate buffer solution.

[0039] The preparation method of the non-irritating clarithromycin freeze-dried powder described in the present embodiment 2 consists of the following steps:

[0040] (1) Dissolve clarithromycin, sodium cholesteryl sulfate, lecithin and citric acid in absolute ethanol to obtain an oil phase, and keep the temperature at 68°C for 35min;

[0041] (2) the dehydrated alcohol in the oil phase is removed by rotary evaporation, and then blown dry with nitrogen to obtain a film;

[004...

Embodiment 3

[0049]The non-irritating clarithromycin freeze-dried powder described in Example 3 is composed of clarithromycin liposome and a freeze-drying protective agent, and 30 g of a freeze-dried protective agent is added to each 100 mL of liposome solution; The plastid solution is prepared from the following raw materials: 2.0 g of clarithromycin, 2.2 g of sodium cholesteryl sulfate, 6.4 g of lecithin, 0.6 g of citric acid, 20 g of sucrose, 10 g of glucose, and the balance is phosphate buffer solution.

[0050] The preparation method of the non-irritating clarithromycin freeze-dried powder described in the present embodiment 3 consists of the following steps:

[0051] (1) Dissolve clarithromycin, sodium cholesterol sulfate, lecithin and citric acid in absolute ethanol to obtain an oil phase, and keep the temperature at 72°C for 33min;

[0052] (2) the dehydrated alcohol in the oil phase is removed by rotary evaporation, and then blown dry with nitrogen to obtain a film;

[0053] (3) ...

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Abstract

The invention belongs to the technical field of macrolide antibiotic preparation, in particular to a non-irritating clarithromycin freeze-dried powder and a preparation method thereof. It is composed of clarithromycin liposome and freeze-drying protective agent, and the freeze-drying protective agent of 18-30g is added in every 100mL liposome solution; the 100mL liposome solution is made from the following raw materials: clarithromycin 2.0g, Cholesterol sodium sulfate 1.8-2.2g, lecithin 6.0-6.4g, citric acid 0.5-0.6g, sucrose 8-20g, glucose 8-15g, and the balance is phosphate buffer solution. The non-irritating clarithromycin freeze-dried powder of the present invention adopts the formula of cholesterol sodium sulfate, lecithin, citric acid and clarithromycin to prepare clarithromycin liposome, which can not only reduce the particle size of liposome, And increase its surface charge, make liposome stable, and liposome encapsulation efficiency is high.

Description

technical field [0001] The invention belongs to the technical field of macrolide antibiotic preparation, in particular to a non-irritating clarithromycin freeze-dried powder and a preparation method thereof. Background technique [0002] Clarithromycin is a semi-synthetic macrolide antibiotic obtained by methylation of the 6-hydroxyl group of erythromycin A. After methylation, clarithromycin effectively improves 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 that it acts on the 50S subunit of the ribosomal protein in the bacterial 70S system, which hinders the synthesis of bacterial proteins and is a long-term bacteriostatic agent. It has inhibitory effect on Gram-positive bacteria such as Gluconobacter aureus, Streptococcus, Pneumococcus, etc., and has inhibitory effect on some Gram-negative bacteria such as Haemophilus influen...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/19A61K9/127A61K47/28A61K47/24A61K47/12A61K47/26A61K31/7048A61P31/04
CPCA61K9/19A61K9/127A61K9/1277A61K47/28A61K47/24A61K47/12A61K47/26A61K9/0019A61K31/7048A61P31/04
Inventor 张军
Owner ZIBO VOCATIONAL INST
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