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Preparation methods for azlocillin sodium and azlocillin sodium freeze-dried powder for injection

A technology of azlocillin sodium and azlocillin acid, which is applied in the directions of freeze-drying delivery, medical preparations containing active ingredients, and pharmaceutical formulations, can solve the problem that the step control process is not very standardized, the quality of azlocillin sodium is unstable, Insufficient parameter control and other problems, to achieve the effect of improving the safety of clinical use, suitable for promotion, and simple operation

Active Publication Date: 2015-04-01
HAINAN GENERAL & KANGLI PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] There are many preparation methods of azlocillin sodium, but in the preparation methods of the prior art, some steps are more complicated, some auxiliary materials or additives are many, some step control processes are not very standardized, and the parameter control is not accurate enough. As a result, the quality of the obtained azlocillin sodium is unstable, and the shelf life therefore has a large fluctuation range, and the risk of clinical use is relatively high

Method used

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  • Preparation methods for azlocillin sodium and azlocillin sodium freeze-dried powder for injection
  • Preparation methods for azlocillin sodium and azlocillin sodium freeze-dried powder for injection
  • Preparation methods for azlocillin sodium and azlocillin sodium freeze-dried powder for injection

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Embodiment 1

[0043] The preparation method of azlocillin sodium of the present invention comprises step S1 preparing azlocillin acid and step S2 preparing azlocillin sodium, wherein,

[0044] The step S1 prepares azlocillin acid, comprising the following steps:

[0045] S1-1: Material preparation: 40g of ampicillin trihydrate, 532g of dichloromethane, 11.6g of triethylamine, 16g of imidazole chloride;

[0046] S1-2: Add ampicillin trihydrate and dichloromethane into the reaction vessel, and stir evenly;

[0047] S1-3: Cool the liquid medicine in the reaction vessel to 10-13°C, add triethylamine, and stir until all the solids are dissolved;

[0048] S1-4: Control the temperature of the liquid medicine at 3-5°C, add imidazole chloride, adjust the pH to 7-8.5, and react for 1-1.5 hours;

[0049] S1-5: filtering and extracting the reaction liquid;

[0050] S1-6: Cool to 3-5°C, adjust the pH to 3-4, and precipitate the precipitate;

[0051] S1-7: The precipitate was taken out, washed and dr...

Embodiment 2 Embodiment 3

[0069] Referring to Table 1, the difference between Embodiment 2 and Embodiment 3 and Embodiment 1 is that the addition content of ampicillin trihydrate, dichloromethane, triethylamine and imidazole chloride in the material preparation of the step S1-1 is replaced For the parts by weight shown in Table 1, the other steps are the same as in Example 1.

[0070] Table 1 The amount of different components added in the material preparation of step S1-1

[0071]

[0072]

Embodiment 4

[0073] Embodiment four and embodiment five

[0074] Referring to Table 2, the difference between Embodiment 4 and Embodiment 5 and Embodiment 1 is that the cooling temperature and heat preservation time in the steps S3-1 to S3-5, the first heating temperature and heat preservation time, the second time The heating temperature and holding time, the third heating temperature and holding time, and the degree of vacuum are replaced by the values ​​shown in Table 2, and the other steps are the same as in Example 1, and the stability study of the resulting finished product is continued at room temperature , the results are as shown in Table 2. Compared with the prior art, the method of the present invention adopts a vacuum low-temperature freeze-drying process to prepare medicines in airtight containers to ensure that the medicines are not easy to oxidize and deteriorate, and overcome the problem of decomposition of medicines caused by high temperatures in the production process. Pr...

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Abstract

The invention provides preparation methods for azlocillin sodium and an azlocillin sodium freeze-dried powder for injection. The preparation methods are simple to operate and suitable for popularization. The obtained azlocillin sodium is high in yield, high in quality, good in stability and high in clinic usage safety. The provided preparation method for the azlocillin sodium freeze-dried powder for injection precisely controls warm-keeping temperature, warm-keeping time, pressure and other parameters, controls multi-layer filtering, and controls other things, so that the obtained azlocillin sodium freeze-dried powder is good in stability, and is improved in clinic usage safety.

Description

technical field [0001] The invention relates to the field of pharmacy, in particular to a preparation method of azlocillin sodium and azlocillin sodium freeze-dried powder for injection. Background technique [0002] Azlocillin sodium, English name: AzlocillinSodium aliases: Alexin, benzazole penicillin, Kang Enbei, azidocillin. This product is white to slightly gray-yellow powder, easily soluble in water, the aqueous solution is transparent, colorless to gray-yellow, pH6.0-8.0. This product is a penicillin antibiotic, the third-generation broad-spectrum semi-synthetic penicillin, effective against G+ bacteria, G- bacteria and anaerobic bacteria, and can strongly fight against Pseudomonas aeruginosa. It is suitable for infections caused by Gram + bacteria, Gram - bacteria and anaerobic bacteria. The antibacterial spectrum of this product is similar to mezlocillin sodium. This product is not resistant to penicillinase of Staphylococcus aureus and β-lactamase produced by En...

Claims

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Application Information

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IPC IPC(8): C07D499/68C07D499/04C07D499/16
CPCA61K9/19A61K31/431C07D499/04C07D499/16C07D499/68
Inventor 王志涛林小雪张丽华
Owner HAINAN GENERAL & KANGLI PHARMA
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