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Clindamycin phosphate compound and preparation method and pharmaceutical composition thereof

A technology of clindamycin phosphate and compounds, which is applied to the preparation of sugar derivatives, chemical instruments and methods, sugar derivatives, etc., can solve the problems of unsuitability for clinical application and potential safety hazards, and achieve the reduction of stability and good Effects of stability and concentration of particle size distribution

Inactive Publication Date: 2013-09-18
四川省惠达药业有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0011] Patent application 201210137702.5 discloses two crystal forms of clindamycin phosphate: clindamycin phosphate n-butanol-water solvate crystal and clindamycin phosphate dimethyl sulfoxide-water solvate crystal, the crystal There is a molecule of solvent in the compound. Since n-butanol and dimethyl sulfoxide have certain toxicity, it will cause safety hazards in clinical use and is not suitable for clinical application.

Method used

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  • Clindamycin phosphate compound and preparation method and pharmaceutical composition thereof
  • Clindamycin phosphate compound and preparation method and pharmaceutical composition thereof
  • Clindamycin phosphate compound and preparation method and pharmaceutical composition thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0045] Embodiment 1: Preparation of Clindamycin Phosphate Compound

[0046] (1) Prepare 5L of a saturated solution of clindamycin phosphate solid at 45°C;

[0047] (2) Prepare 25L of mixed organic solvent of ethyl acetate, acetone and ether; the volume ratio of ethyl acetate, acetone and ether in the mixed organic solvent is 1:2:3;

[0048] (3) Cool the organic solvent to 0°C, and add a saturated aqueous solution of clindamycin phosphate to the organic solvent at a uniform speed under the condition of a stirring speed of 720 rpm, and continue stirring after the addition, and the stirring speed is 360 rpm Minutes; stop stirring after cooling down to 0°C; stand for crystal growth for 8 hours; filter after obtaining crystals, wash with absolute ethanol, and vacuum dry for 4 hours to obtain clindamycin phosphate compound; saturated aqueous solution of clindamycin phosphate The addition rate was 2.5 liters / hour.

[0049] Prepared clindamycin phosphate obtained by Cu-Kα ray measur...

Embodiment 2

[0050] Embodiment 2: Preparation of clindamycin phosphate compound

[0051] (1) Prepare 5L of a saturated solution of clindamycin phosphate solid at 58°C;

[0052] (2) Prepare 50L of mixed organic solvent of ethyl acetate, acetone and ether; the volume ratio of ethyl acetate, acetone and ether in the mixed organic solvent is 1:2:2;

[0053] (3) Cool the organic solvent to 5°C, and add a saturated aqueous solution of clindamycin phosphate to the organic solvent at a uniform speed under the condition of a stirring speed of 360 rpm. Minutes; stop stirring after cooling down to 0°C; let stand to grow crystals for 8 hours; filter after obtaining crystals, wash with absolute ethanol, and dry in vacuum for 4 hours to obtain clindamycin phosphate compound, saturated aqueous solution of clindamycin phosphate The rate of addition is 5 liters / hour.

[0054] Prepared clindamycin phosphate obtained by Cu-Kα ray measurement X-ray powder diffraction pattern as figure 1 As shown; the purit...

Embodiment 3

[0055] Embodiment 3: Preparation of Clindamycin Phosphate Compound

[0056] (1) Prepare 5L of a saturated solution of clindamycin phosphate solid at 50°C;

[0057] (2) Prepare 40L of mixed organic solvent of ethyl acetate, acetone and ether; the volume ratio of ethyl acetate, acetone and ether in the mixed organic solvent is 1:3:3;

[0058] (3) Cool the organic solvent to 2°C, and add a saturated aqueous solution of clindamycin phosphate to the organic solvent at a uniform speed under the condition of a stirring speed of 720 rpm, and continue stirring after the addition is completed, and the stirring speed is 360 rpm Minutes; stop stirring after cooling down to 1°C; stand still for 8 hours to grow crystals; filter after obtaining crystals, wash with absolute ethanol, and vacuum dry for 4 hours to obtain clindamycin phosphate compound; saturated aqueous solution of clindamycin phosphate The adding speed is: 5 liters / hour.

[0059] Prepared clindamycin phosphate obtained by Cu...

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Abstract

The invention relates to a pharmaceutical compound, and particularly relates to a pharmaceutical compound of clindamycin phosphate and a preparation method and a pharmaceutical composition thereof. The X-ray powder diffraction pattern of the clindamycin phosphate compound, measured by use of Cu-K alpha rays, is shown by the figure 1. The clindamycin phosphate compound provided by the invention has good stability, does not absorb moisture easily and is very suitable for being prepared into various powder-needle dosage forms so as to fundamentally solve the problem of stability drop after moisture absorption; and a stability test proves that the lyophilized powder needle, large-volume injection and small-volume injection prepared from the clindamycin phosphate compound have good stability and are very suitable for clinical application.

Description

technical field [0001] The present invention relates to a pharmaceutical compound, in particular to a pharmaceutical compound of clindamycin phosphate, its preparation method and its pharmaceutical composition. Background technique [0002] Clindamycin phosphate, the English name is Clindamycin phosphate, the chemical formula is 6-(1-methyl-4-propyl-2-pyrrolidine carbonyl amido)-1-1thio-methyl-7-chloro -6,7,8-trideoxy-L-threo-α-D-galactopyranoside-2-dihydrogen phosphate, the structural formula is: [0003] [0004] Clindamycin phosphate is a chemically semi-synthesized clindamycin derivative. It has no antibacterial activity in vitro, and when it enters the body, it is rapidly hydrolyzed into clindamycin to display its pharmacological activity. Therefore, the antibacterial spectrum, antibacterial activity and therapeutic effect are the same as Clindamycin is the same, but its ester solubility and permeability are better than clindamycin, and it can be administered orally...

Claims

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Application Information

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IPC IPC(8): C07H15/16C07H1/00A61K31/7056A61P31/04
Inventor 梁宏平
Owner 四川省惠达药业有限公司
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