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High-purity and/or high-content penicillin sodium salt solid powder and preparing method

A solid powder and solid technology, which is applied in the fields of active ingredients of heterocyclic compounds, anti-infective drugs, organic chemistry, etc. It can solve the problems of affecting product quality, easy decomposition, and many impurities in freeze-dried powder.

Inactive Publication Date: 2007-11-14
马启明
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] At present, the preparation of the solid powder of the compound of formula II is to convert the compound of formula I into the compound of formula II in an aqueous solution and then obtain it by freeze-drying (US Patent 4,066,664). Sensitive, easy to decompose, difficult to prepare by conventional solvent method for preparing solid sodium salt of β-lactam antibiotics
The freeze-drying method is usually used because the impurities in the aqueous solution are difficult to be removed during the transformation, and all the impurities are precipitated together with the product after freeze-drying, resulting in many impurities and low purity in the freeze-dried powder, which affects the quality of the product

Method used

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  • High-purity and/or high-content penicillin sodium salt solid powder and preparing method
  • High-purity and/or high-content penicillin sodium salt solid powder and preparing method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] Example 1 Preparation of ticarcillin disodium solid powder with content of 98.7% and purity of 99.68%

[0027] Add 2 mL of water to an ethyl acetate solution containing 0.02 mol of ticarcillin (formula I, Ar is thiophen-3-yl), add sodium bicarbonate at 5-10°C to adjust the pH to 6.5, and separate the water layer. The aqueous layer was slowly added dropwise to 100 mL of isopropanol, filtered with suction, washed the filter cake with a small amount of isopropanol, and vacuum-dried to obtain 7.9 g of ticarcillin disodium white powdery solid, with a yield of 93%. Purity 99.68% (HPLC), content 98.7%.

Embodiment 2

[0028] Example 2 Preparation of ticarcillin disodium solid powder with content of 98.5% and purity of 99.25%

[0029] Add 2 mL of water to the ethyl acetate solution containing 0.02 mol of ticarcillin, add sodium carbonate at 5-10°C to adjust the pH to 6.5, and separate the water layer. The water layer was slowly added dropwise to 100 mL of tert-butanol, filtered with suction, washed the filter cake with a small amount of tert-butanol, and vacuum-dried to obtain ticarcillin disodium as a white powdery solid with a purity of 99.25% and a content of 98.5%.

Embodiment 3

[0030] Example 3 Preparation of ticarcillin disodium solid powder with content of 99.0% and purity of 99.82%

[0031] Add 2 mL of water to the ether solution containing 0.02 mol of ticarcillin, add sodium bicarbonate at 5-10°C to adjust the pH to 6.5, and separate the water layer. The aqueous layer was slowly added dropwise to 500 mL of acetone, filtered with suction, washed with a small amount of acetone, and dried in vacuum to obtain ticarcillin disodium as a white powdery solid with a purity of 99.82% and a content of 99.0%.

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Abstract

This invention relates to a high-purity and / or high-content sodium benzylpenicillin sodium solid powder and their medicine combination, as well as preparation method. Such as: sodium salt of Ticarcillin and carbenicillin carboxybenzyl penicillin.

Description

field of invention [0001] The invention relates to high-purity and / or high-content penicillin sodium salt solid powder, a pharmaceutical composition containing them and a preparation method thereof. Wherein said penicillin sodium salt is exemplified: the sodium salt of ticarcillin and carbenicillin. Background technique [0002] Ticarcillin and carbenicillin are broad-spectrum semi-synthetic penicillin antibiotics belonging to carbenicillin, as shown in formula I, wherein Ar is thiophen-3-yl (ticarcillin) or phenyl (carbenicillin). Clinically, its disodium salt (formula II, Ar is thiophen-3-yl or phenyl) and β-lactamase inhibitors, such as potassium clavulanate, are mainly used to make compound preparations for various bacteria Infection treatment. [0003] [0004] Formula II Formula I [0005] At present, the preparation of the solid powder of the compound of formula II is to convert the compound of formula I into the compound of formula II in an aqueous solution and...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D499/72C07D499/04A61K31/43A61K31/431A61P31/00
CPCC07D499/16C07D499/18A61P31/00
Inventor 马启明
Owner 马启明
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