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Cefradine compound and capsule preparation method thereof

A cefradine and compound technology, which is applied to the preparation of cefradine capsules and the field of cefradine refining, can solve the problems of residual organic solvent, mixing of water-insoluble impurities, affecting refining effect, etc., and achieve simple refining process, reduce toxic and side effects, and improve product quality Effect

Inactive Publication Date: 2009-10-07
HAINAN MEIDA PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

In this method, adjust alkalinity with triethylamine alone, there will be a large amount of water-insoluble impurities to mix in, affect the effect of refining, and triethylamine is adjusted to 5.4, a little on the high side, affects the yield of cephradine refining, finally with acetone (60 %) washing, the residual organic solvent is serious, which affects the quality of the final preparation product

Method used

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  • Cefradine compound and capsule preparation method thereof
  • Cefradine compound and capsule preparation method thereof
  • Cefradine compound and capsule preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0035] The refining of embodiment 1 cefradine

[0036] Add 1000g of cephradine to 4000ml of water containing 10ml of concentrated hydrochloric acid for hydrolysis, stir at 10°C for 15 minutes, add 13.5g of activated carbon to the water layer for decolorization, filter, and collect the filtrate. Add 25ml of triethylamine to adjust the pH value to 3.0, add 0.1g of seed crystals, and continue to adjust to 5.4 with 15ml of triethylamine. Cool to 5°C and let stand overnight. Crystals were precipitated, washed with 60% acetone solution, and vacuum-dried at 50° C. to obtain 648.4 g of refined cephradine with a purity of 96.8%.

Embodiment 2

[0037] The refining of embodiment 2 cefradine

[0038] Add 1000g of cephradine to 2000g of 0.1mol / L hydrochloric acid solution, dissolve completely in an ice-water bath, add 13.3g of activated carbon for decolorization for 30 minutes, filter for decarbonization, wash the filter cake with 100ml of water, combine the filtrates, and transfer them to a three-necked flask. Stir to constant temperature, slowly add triethylamine / DMF solution with a volume ratio of 1.2:1, control the volume and speed of addition, monitor the pH change of the crystallization solution online with an acidity meter, control the pH value of the crystallization end point to 5.2, and stop adding alkali , the dosage is 300ml, the crystal slurry is lowered to 5°C in 1.5h, filtered after constant temperature, washed with 100ml of 95% ethanol, and dried in vacuum at 45°C to obtain 886.4g of cephradine refined product, and the detection purity is 99.1%.

Embodiment 3

[0039] The refining of embodiment 3 cefradine

[0040] Add 2000g of cephradine into 4000g of 0.5mol / L hydrochloric acid solution, dissolve completely in an ice-water bath, add 28.2g of activated carbon for decolorization for 15 minutes, filter for decarburization, wash the filter cake with 100ml of water, combine the filtrates, and transfer them to a three-necked flask. Stir down to a constant temperature, slowly add 10% sodium bicarbonate solution, control the volume and speed of addition, monitor the pH change of the crystallization solution online through an acidity meter, control the crystallization terminal pH value to 5.1, stop adding alkali, and the dosage is 500ml. The crystal slurry was lowered to 5°C within 1h, filtered after constant temperature, washed with 100ml of 95% ethanol, and vacuum-dried at 45°C to obtain 1684.7g of cephradine refined product with a detection purity of 98.9%.

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Abstract

The invention provides a cefradine compound and a capsule preparation method thereof. The preparation method of the cefradine compound includes the following steps: cefradine is added into an acid solution and dissolves fully in ice water bath; active carbon is added for discoloration and the mixed solution is filtered and the filtrate is combined and then put into a container; the filtrate is stirred at the initial temperature of crystallization to constant temperature; alkaline liquor is gradually added; the magma is filtered after the temperature of the magma reduces to the crystallization end temperature, washed with alcohol and dried in vacuum to obtain the compound. Based on the total weight of capsule, cefradine capsule comprises 20-70wt of cefradine, 0-60wt of filling agent, 0-10wt of disintegrating agent, 1-10wt of adhesive and 0.5-3wt of lubricant.

Description

technical field [0001] The invention relates to a method for refining cephradine, in particular to a method for preparing cephradine capsules, and belongs to the technical field of medicine. Background technique [0002] Cephradine is the first generation of β-lactam antibiotics of the cephem class for injection or oral use. It mainly has a strong bactericidal effect on drug-resistant Staphylococcus aureus and Klebsiella pneumoniae. Pneumococci, Escherichia coli, and some Proteus all have antibacterial effects, and have the advantages of broad antibacterial, strong bactericidal power, small allergic reaction, and high stability to β-lactamase. Clinically, it is mainly used to treat respiratory tract, urinary tract, skin, soft tissue and other infections. [0003] The raw materials of cephradine currently on the market have poor purity and relatively high polymers, resulting in clinically allergic reactions. The main symptoms are rash, urticaria, itching, erythema, and drug ...

Claims

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Application Information

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IPC IPC(8): C07D501/22C07D501/12A61K31/545A61K9/48A61J3/07A61P31/00A61P31/04
Inventor 王明
Owner HAINAN MEIDA PHARMA
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