Amorphous cloxacillin sodium compound without hygroscopicity

A cloxacillin sodium and compound technology, applied in the field of amorphous cloxacillin sodium compounds, can solve the problems of serious moisture absorption, inconvenience in production, packaging, storage, and hygroscopicity, and achieve high solubility, good for drug absorption, high dispersive effect

Inactive Publication Date: 2012-12-12
TIANJIN SONGRUI MEDICAL TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0021] During the research process, repeating the method of the patent document prepared above, the crude product of cloxacillin sodium obtained has hygroscopicity and serious hygroscopicity, which brings great inconvenience to production, packaging and storage

Method used

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  • Amorphous cloxacillin sodium compound without hygroscopicity
  • Amorphous cloxacillin sodium compound without hygroscopicity
  • Amorphous cloxacillin sodium compound without hygroscopicity

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0054] Put 100g of crude product, 1L of deionized water and 20g of activated carbon in a reaction flask, adjust pH=2 with concentrated hydrochloric acid while stirring at 60-70℃, keep it warm and stir for 1 hour, while hot, wash the filter cake with deionized water at 70℃ , Combine the filtrate and washing liquid, adjust to pH=7 with 40% sodium hydroxide solution while stirring at 65-70°C, cool to room temperature, and precipitate solids. Wash the filter cake with deionized water and dry to obtain cloxacillin sodium The white powder is 89.5g, the yield is 89%, the chemical purity is as high as 99.9%, the total impurities are less than 0.08%, and the moisture measured by Karl Fischer method is 0.15%.

[0055] See the infrared spectrum of the compound figure 2 , Use KBr to press tablets when measuring.

[0056] The X-ray diffraction pattern of the compound is shown in image 3 . Instrument model and measurement conditions: Rigaku D / max 2500 diffractometer; CuKa 40Kv 100mA; 2θ scanni...

Embodiment 2

[0058] Put 100g of the crude product, 1L of deionized water and 20g of activated carbon in the reaction flask, adjust pH=1 with concentrated hydrochloric acid while stirring at 60-70℃, keep the temperature and stir for 1 hour, while it is hot, wash the filter cake with deionized water at 70℃ , Combine the filtrate and washing liquid, adjust to pH=7 with 40% sodium hydroxide solution while stirring at 65-70°C, cool to room temperature, and precipitate solids. Wash the filter cake with deionized water and dry to obtain cloxacillin sodium The white powder is 87.5g, the yield is 87%, the chemical purity is as high as 99.9%, the total impurities are less than 0.08%, and the moisture measured by Karl Fischer method is 0.25%.

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Abstract

The invention belongs to the technical field of medicines, and particularly relates to an amorphous cloxacillin sodium compound without hygroscopicity, and the compound has the characteristic of high dispersity, is beneficial to medicament absorption, and can be used for improving the clinical adaptability. The cloxacillin sodium compound provided by the invention is high in purity and good in stability, and is not obvious in moisture absorption and weight increment even under the condition of high humidity, so that related substances are not increased; and compared with cloxacillin sodium with other crystalline states, the amorphous cloxacillin sodium compound has high solubility.

Description

Technical field [0001] The invention relates to medicines in the field of medicine, in particular to an amorphous cloxacillin sodium compound without hygroscopicity. Background technique [0002] Cloxacillin sodium is suitable for the treatment of penicillinase-producing staphylococcal infections, including sepsis, endocarditis, pneumonia and skin and soft tissue infections. [0003] Cloxacillin Sodium [0004] English name: Cloxacillin Sodium; [0005] Chemical name: (2S,5R,6R)-3,3-dimethyl-6-[5-methyl-3-(2-chlorophenyl)-4-isoxazolecarboxamido)-7-oxy 4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylate sodium salt; [0006] Molecular formula: C 19 H 17 ClN 3 NaO 5 S; [0007] Molecular weight: 457.87; [0008] Chemical properties: white powder or crystalline powder; slightly odor, bitter taste, and hygroscopic. Easily soluble in water, soluble in ethanol, almost insoluble in ethyl acetate. [0009] Structural formula: [0010] Indications: Suitable for the treatment of penicillinase-produci...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D499/76C07D499/18
Inventor 张昊
Owner TIANJIN SONGRUI MEDICAL TECH
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