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Amorphous cephalosporin

An amorphous, cefathiamidine technology, applied in the directions of antibacterial drugs, organic chemistry, organic active ingredients, etc., can solve the problems of increasing freeze-drying cost, prolonging freezing and drying time, etc., to achieve industrialization cost advantage and finished product clarity. Good, low solvent residue effect

Active Publication Date: 2005-03-16
GUANGZHOU BAIYUNSHAN PHARM CO LTD
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The co-melting decomposition point of this multi-component solution may be lower than the co-melting decomposition point of a single component, and the freezing and drying time is correspondingly prolonged, thereby increasing the cost of freeze-drying

Method used

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  • Amorphous cephalosporin
  • Amorphous cephalosporin
  • Amorphous cephalosporin

Examples

Experimental program
Comparison scheme
Effect test

example 1

[0044] Example 1: Preparation of lyophilized cefathiamidine.

[0045]Take by weighing 120 grams of cefathiamidine, add 600ml of pre-cooled water for injection, weigh 0.6g of activated active C after dissolving, decolorize 10mm in an ice bath, and then sterile filter, and the sterile filtrate is placed in a lyophilizer (medical LGJ- LC type freeze dryer), freeze, heat, sublimate and dry according to the freeze-drying curve of cefathiamidine. The obtained white cefathiamidine powder had a content of 95.8%, related substances 1.08%, water content 1.8%, methylene chloride solvent residue 0.01% (pharmacopoeia standard less than 0.06%), and other indicators met the pharmacopoeia standard.

[0046] Differential scanning calorimetry (DSC) curve, it is measured that it exotherms at 147.74 ° C, and its melting decomposition point measured by a melting point instrument is 127 ° C,

[0047] Infrared absorption spectrum of characteristic functional groups (KBr, cm -1 ) are: 1231.8, 1339....

example 2

[0050] Example 2, the preparation of lyophilized cefathiamidine

[0051] Configuration concentration is 60% cefathiamidine aqueous solution, add 0.4gC decolorization, other conditions are the same as example 1, obtain off-white powder, its content 96.02%, related substance 1.10%, moisture 1.7%, dichloromethane solvent residual 0.01%, other The indicators meet the Pharmacopoeia standards.

[0052] Differential scanning calorimetry (DSC) curve, it is measured that it is exothermic at 147.20 ° C, and its melting point is 127 ° C as measured by the melting point instrument.

[0053] Infrared absorption spectrum of characteristic functional groups (KBr, cm -1 ) are: 1231.2, 1338.6, 1392.1, 1607.9, 1774.7.

[0054] X-ray diffraction patterns, proved to be amorphous powder.

[0055] The dissolution rate was measured as in Example 1, and the lyophilized powder was dissolved in 4.3 seconds.

example 3

[0056] Example 3, the preparation of lyophilized cefathiamidine

[0057] A 10% cefathiamidine aqueous solution was prepared, and 0.2 g of C was added for decolorization, and other conditions were the same as in Example 1 to obtain a white powder.

[0058] According to the differential scanning calorimetry (DSC) curve, it was measured that it exothermic obviously at 146.9°C, and the melting point instrument showed that its melting decomposition point was 126~127°C.

[0059] Infrared absorption spectrum of characteristic functional groups (KBr, cm -1 ) are: 1231.9, 1339.5, 1393.9, 1774.6.

[0060] X-ray diffraction patterns, proved to be amorphous powder.

[0061] The dissolution rate was measured as in Example 1, and the lyophilized powder was dissolved in 5 seconds.

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Abstract

The invention discloses an amorphous cefathiamidine solid which is characterized by X-ray diffraction atlas, differential scanning calorimetry (DSC) and infrared spectroscopic data. The solid can be prepared through cryodesiccation, spray drying and precipitation process.

Description

Technical field: [0001] The invention relates to an amorphous cephalosporin, in particular to an amorphous solid of cefathiamidine, its preparation method and its application in the field of pharmacy. Background technique: [0002] Cephalosporins are a class of thermosensitive and hygroscopic β-lactam antibiotics. Cephalosporins for injection are usually prepared by solvent crystallization under sterile conditions. Crystalline cephalosporin products are generally considered to be relatively stable, and the physical form of the product is also related to its bioavailability. For research on crystalline and amorphous aspects, please refer to "solid state chemistry of drug", 1982, PP10-11 and int, J, pharm, VO124, pp1-17. However, the dissolution rate of crystalline products in water is generally slower than that of amorphous products, and their solubility is also poor. Due to their fast dissolution rates, amorphous products show better operability in clinical injection thera...

Claims

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Application Information

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IPC IPC(8): A61K9/08A61K9/19A61K31/545A61P31/04C07D501/02C07D501/28
Inventor 刘学斌许淑文湛燕薇叶放
Owner GUANGZHOU BAIYUNSHAN PHARM CO LTD
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