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New active clindamycin phosphate compound and medicinal composition thereof

A technology of clindamycin phosphate and compounds, which is applied in the field of medicine, can solve the problems of unguaranteed quality, low crystal yield, and poor reproducibility of the preparation method, and achieve simple and feasible preparation methods, simple preparation methods, The effect of stability improvement

Active Publication Date: 2012-10-17
南城第二医院
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The stability of the clindamycin phosphate crystals obtained in the above application has been improved, but the reproducibility of the preparation method is not strong. The method of recrystallization after dissolving the clindamycin phosphate and then natural evaporation or rotary evaporation is adopted. The yield of the obtained crystals is Low, quality can not be guaranteed

Method used

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  • New active clindamycin phosphate compound and medicinal composition thereof
  • New active clindamycin phosphate compound and medicinal composition thereof
  • New active clindamycin phosphate compound and medicinal composition thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0048] The preparation of embodiment 1 clindamycin phosphate compound

[0049] (1) Take the crude clindamycin phosphate and fully dissolve it in a mixed solution of isopropanol and n-butanol to obtain a clindamycin phosphate solution. The ratio of isopropanol to n-butanol in the mixed solution is 4 :3, the mass volume ratio of clindamycin phosphate and Virahol is 1:3;

[0050] (2) Add a mixture of ether and acetone dropwise to the solution obtained in step 1 under an ultrasonic field of 0.5KW. In the mixture, the amount of ether and acetone is 4:5, and the mass of clindamycin phosphate and the mixture The volume ratio is 3:7; the dropping speed is 8ml / min; the stirring is continued at a speed of 12rmp during the dropping process;

[0051] (3) Continue ultrasonication for 20 minutes at a stirring speed of 4rmp and an ultrasonic field power of 0.25kw, let the solution stand and cool down to 15°C at a speed of 0.06°C / min, grow crystals for 6 hours, filter, and use 2 times the am...

Embodiment 2

[0053] The preparation of embodiment 2 clindamycin phosphate compounds

[0054] (1) Take the crude product of clindamycin phosphate and fully dissolve it in a mixed solution of isopropanol and n-butanol to obtain a clindamycin phosphate solution. The ratio of isopropanol to n-butanol in the mixed solution is 2 :3, the mass volume ratio of clindamycin phosphate and Virahol is 1:1.5;

[0055] (2) Add a mixture of ether and acetone dropwise to the solution obtained in step 1 under an ultrasonic field of 0.4KW. In the mixture, the amount of ether and acetone is 2:5, and the mass of clindamycin phosphate and the mixture The volume ratio is 3:4; the dropping speed is 5ml / min; the stirring is continued at a speed of 10rmp during the dropping process;

[0056] (3) Continue ultrasonication for 10 minutes at a stirring speed of 2rmp and an ultrasonic field power of 0.2kw, let the solution stand and cool down to 12℃ at a speed of 0.02℃ / min, grow crystals for 4 hours, filter, and use 1 t...

Embodiment 3

[0058] The preparation of embodiment 3 clindamycin phosphate compounds

[0059] (1) Take the crude product of clindamycin phosphate and fully dissolve it in a mixed solution of isopropanol and n-butanol to obtain a clindamycin phosphate solution. The ratio of isopropanol to n-butanol in the mixed solution is 5 : 3, the mass volume ratio of clindamycin phosphate and Virahol is 1: 4.5;

[0060] (2) Add a mixture of ether and acetone dropwise to the solution obtained in step 1 under an ultrasonic field of 0.6KW. In the mixture, the amount of ether and acetone is 6:5, and the mass of clindamycin phosphate and the mixture The volume ratio is 3:11; the dropping speed is 10ml / min; the stirring is continued at a speed of 16rmp during the dropping process;

[0061] (3) Continue ultrasonication for 25 minutes at a stirring speed of 5rmp and an ultrasonic field power of 0.3kw, let the solution stand and cool down to 18°C ​​at a speed of 0.1°C / min, grow crystals for 8 hours, filter, and ...

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Abstract

The invention relates a new active clindamycin phosphate compound and a medicinal composition of the compound. When the clindamycin phosphate compound is determined by using powder X-ray diffraction, characteristic diffraction peaks appear at the angels of 4.85 degrees, 5.73 degrees, 6.64 degrees, 9.12 degrees, 11.98 degrees, 13.51 degrees, 17.37 degrees, 19.61 degrees, 21.76 degrees, 22.23 degrees, 23.46 degrees, 26.82 degrees, 28.16 degrees, 33.68 degrees and 34.29 degrees in a X-ray diffraction pattern represented in 2theta + / -0.2 degree diffraction angles. The stability of the clindamycinphosphate compound provided by the invention is improved remarkably; the influences on the appearance, content and other aspects of the clindamycin phosphate compound caused by long-term storage can be ignored, thereby ensuring the drug safety for patients. In addition, the new clindamycin phosphate compound is suitable to be popularized and applied to various clindamycin phosphate preparations.

Description

technical field [0001] The invention relates to the field of medicine, in particular to a new active clindamycin phosphate compound and a pharmaceutical composition thereof. Background technique [0002] Clindamycin phosphate is a derivative of clindamycin, which is inactive in vitro. When injected into the body, it is rapidly hydrolyzed into clindamycin to exert pharmacological effects and inhibit bacterial protein synthesis. Clindamycin phosphate has the same antibacterial spectrum and antibacterial activity as clindamycin, and has antibacterial activity against Gram-positive bacteria such as Staphylococcus aureus, Streptococcus pneumoniae and hemolytic streptococcus and most anaerobic bacteria. [0003] Clindamycin phosphate is a lactone compound, which is easy to degrade in water, and its hydrolyzed products are highly toxic. In addition, the structure and pharmacological properties of many degradation products are still unclear, which affects the safety of clinical medi...

Claims

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Application Information

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IPC IPC(8): C07H15/16A61K31/7056A61P31/04
Inventor 夏智红
Owner 南城第二医院
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