New crystal form cefamandole nafate compound prepared by adopting particle process crystal product molecular assembling and morphology optimizing technology and preparation

A technology of cefamandole sodium and its compound, which is applied in the field of medicine and can solve problems such as poor color, low content, and adverse reactions

Inactive Publication Date: 2016-05-11
HAINAN LINGKANG PHARMA CO LTD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the products obtained by the existing methods and the above-mentioned patents all have defects such as poor purity, poor color, and low content, which affect the quality effect of its preparations
In particular, cefamandole sodium is often used as an injection in clinical practice, and its low purity may even cause unforeseen adverse reactions, thereby limiting the use of the drug

Method used

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  • New crystal form cefamandole nafate compound prepared by adopting particle process crystal product molecular assembling and morphology optimizing technology and preparation
  • New crystal form cefamandole nafate compound prepared by adopting particle process crystal product molecular assembling and morphology optimizing technology and preparation
  • New crystal form cefamandole nafate compound prepared by adopting particle process crystal product molecular assembling and morphology optimizing technology and preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] Embodiment 1: Preparation of Cefamandole Sodium New Crystal Form Compound

[0028] (1) Add 10.5g of 7-ATCA and 100ml of dichloromethane to the reactor successively, and stir for 10min; continue to gradually add BSA15ml into the above solution; react at 25~30℃ for 3h, cool down to -5~-10℃; Add 8.1 g of formylmandelic acid chloride (dissolved in 25 ml of ethyl acetate). After the dropwise addition, the temperature is raised to 0-5° C. for 3 h. Add 100ml of deionized water at about 15°C and 100g of sodium acetate to the above reactor; stir for 30 minutes, let stand for 30 minutes to separate layers; separate the water layer, add 50ml of saturated sodium chloride solution to the organic layer, stir for 15 minutes, and combine the organic layers . Add 15 g of anhydrous magnesium sulfate to the organic layer, stir and dehydrate for 60 minutes; then add 2 g of activated carbon, stir and decolorize for 30 minutes; filter, and vacuum-dry the filtrate at 28° C. to obtain a solid...

Embodiment 2

[0037] Embodiment 2: Preparation of Cefamandole Sodium New Crystal Form Compound

[0038] (1) Add 11.4g of 7-ATCA and 100ml of dichloromethane to the reactor successively, and stir for 10min; continue to gradually add BSA15ml into the above solution; Add 11.4g of formylmandelic acid chloride (dissolved in 35ml of ethyl acetate), and after the dropwise addition, raise the temperature to 0-5°C and react for 3h. Add 100ml of deionized water at about 15°C and 100g of sodium acetate to the above reactor; stir for 30 minutes, let stand for 30 minutes to separate layers; separate the water layer, add 50ml of saturated sodium chloride solution to the organic layer, stir for 15 minutes, and combine the organic layers . Add 13.8g of anhydrous magnesium sulfate to the organic layer, stir and dehydrate for 60min; then add 2g of activated carbon, stir for 30min to decolorize; filter, and vacuum-dry the filtrate at 30°C to obtain a solid-liquid mixture of cefamandroic acid. .

[0039] (2...

Embodiment 3

[0042] Embodiment 3: Preparation of new crystal form compound of cefamandole sodium

[0043] (1) Add 11.4g of 7-ATCA and 100ml of dichloromethane to the reactor successively, and stir for 10min; continue to gradually add BSA15ml into the above solution; Add 20.5g of formylmandelic acid chloride (dissolved in 60ml of ethyl acetate), and after the dropwise addition, raise the temperature to 0-5°C and react for 3h. Add 200ml of deionized water at about 15°C and 200g of sodium acetate to the above reactor; stir for 30 minutes, let stand for 30 minutes to separate layers; separate the water layer, add 50ml of saturated sodium chloride solution to the organic layer, stir for 15 minutes, and combine the organic layers . Add 20.4g of anhydrous magnesium sulfate to the organic layer, stir and dehydrate for 60min; then add 2g of activated carbon, stir for 30min to decolorize; filter, and vacuum-dry the filtrate at 30°C to obtain a solid-liquid mixture of cefamandroic acid. .

[0044]...

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PUM

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Abstract

The invention discloses a new crystal form cefamandole nafate compound and a crystallization preparation method thereof. The new crystal form cefamandole nafate compound is prepared by adopting the particle process crystal product molecular assembling and morphology optimizing technology. The compound has the advantages of being high in purity, low in impurity content and good in fluidity and stability. The invention also discloses a preparation which is prepared from cefamandole nafate, namely cefamandole nafate for injection.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a new crystal form compound of cefamandole sodium and a preparation using particle process crystal product molecular assembly and shape optimization technology. Background technique [0002] Cefamandole sodium (Cefamandolenafate) chemical name is 7-D-(2-formyloxyphenylacetamide)-3-[(1-methyl-1H-tetrazol-5 base)thiomethyl]-3- Cephem-4-carboxylic acid sodium salt, molecular weight 512.5, structural formula: [0003] [0004] Cefamandole sodium is the prodrug of cefamandole, which is rapidly hydrolyzed into the active ingredient cefamandole after intravenous or intramuscular injection. The drug is a second-generation semi-synthetic cephalosporin developed by Eli Lilly and Company in 1972. It was used clinically in 1978, and its trade name is Mandol. At present, the United States Pharmacopoeia, the British Pharmacopoeia, the European Pharmacopoeia, and the Chinese P...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D501/36C07D501/06C07D501/12A61K31/546A61K9/14A61P31/04A61P11/00A61P13/02A61P1/16A61P17/00A61P19/02A61P19/08
CPCC07D501/36C07B2200/13
Inventor 陶灵刚王静康尹秋响郝红勋
Owner HAINAN LINGKANG PHARMA CO LTD
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