Triamcinolone acetonide acetate crystal form B, preparation method of triamcinolone acetonide acetate crystal form B, medicinal composition containing crystal form B and application of crystal form B

A technology of triamcinolone acetonide acetate and its composition, which is applied in the field of new crystal form B of triamcinolone acetonide acetate and its preparation, can solve the problems of patients' pain, unqualified products, and easy caking, and achieve good reproducibility, Simple operation effect

Active Publication Date: 2017-03-22
SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In particular, the suspension injection is easy to agglomerate during storage, resulting in unqualified products, causing severe pain to patients during the injection process

Method used

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  • Triamcinolone acetonide acetate crystal form B, preparation method of triamcinolone acetonide acetate crystal form B, medicinal composition containing crystal form B and application of crystal form B
  • Triamcinolone acetonide acetate crystal form B, preparation method of triamcinolone acetonide acetate crystal form B, medicinal composition containing crystal form B and application of crystal form B
  • Triamcinolone acetonide acetate crystal form B, preparation method of triamcinolone acetonide acetate crystal form B, medicinal composition containing crystal form B and application of crystal form B

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] Mix 12 g of triamcinolone acetonide acetate in 500 mL of methanol, add a magnetic stirrer and stir at 200 rpm, and it can be completely dissolved at 50°C. Continue to stir and cool to 5°C to obtain a suspension, which is filtered and dried under reduced pressure at room temperature. The crystal form B was obtained as 11.4 g of white crystalline powder, and the yield was 95%.

[0039] The X-ray powder diffraction (XRPD) pattern of the crystal form B of triamcinolone acetonide acetate of embodiment 1 is shown in figure 1 ; Thermogravimetric analysis (TG) diagram see figure 2 ; Differential scanning calorimetry (DSC) diagram see image 3 ; Infrared spectrum (IR) figure see Figure 4 ; Commercially available triamcinolone acetonide acetate crystal form and the contrast figure of crystal form B of the present invention are as follows Figure 5 shown. Scanning electron microscope (SEM) picture see Figure 6 The crystal form B is suspended in water, and the scanning ele...

Embodiment 2

[0042] Mix 10 g of triamcinolone acetonide acetate in 500 mL of ethanol, add a magnetic stirring bar to stir at 200 rpm, and heat to 60° C. to dissolve completely. Continue to stir and cool to 5°C to obtain a suspension, which is filtered and dried under reduced pressure at room temperature. 9.4 g of white crystals were obtained as crystal form B, and the yield was 94%.

Embodiment 3

[0044] Mix 15 g of triamcinolone acetonide acetate in 500 mL of methyl ethyl ketone, add a magnetic stirring bar to stir at 200 rpm, and heat to 70° C. to dissolve completely. Continue to stir and cool to 5°C to obtain a suspension, which is filtered and dried under reduced pressure at room temperature. The crystal form B was obtained as 12.4 g of white crystalline powder, and the yield was 83%.

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Abstract

The invention discloses a triamcinolone acetonide acetate crystal form B, a preparation method of the triamcinolone acetonide acetate crystal form B, a medicinal composition containing the crystal form B and application of the crystal form B. A novel crystal form is comprehensively represented by means of XRD (X-Ray Powder Diffraction), IR (Infrared Radiation), DSC (Differential Scan Calorimetry), TGA (Thermo Gravimetric Analysis), SEM (Scanning Electron Microscope) and the like. Specific to the crystal form B, a powder diffraction pattern obtained by an X-ray powder diffraction method of Cu K alpha has diffraction peaks at the following 2 theta angles: 6.81 degrees+/-0.2 degree, 8.80 degrees+/-0.2 degree, 9.34 degrees+/-0.2 degree, 11.52 degrees+/-0.2 degree, 12.15 degrees+/-0.2 degree, 13.40 degrees+/-0.2 degree, 14.13 degrees+/-0.2 degree, 14.57 degrees+/-0.2 degree, 15.43 degrees+/-0.2 degree, 16.72 degrees+/-0.2 degree, 17.70 degrees+/-0.2 degree, 18.70 degrees+/-0.2 degree, and 19.08 degrees+/-0.2 degree. The new triamcinolone acetonide acetate crystal form, provided by the invention, has the advantages that the particles are small in size and uniform in distribution, agglomeration is difficult, preparation and storage of a mixed-suspended injection are facilitated, and the physical-chemical performance and patent medicine performance are superior.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical solid chemistry, and in particular relates to a new crystal form B of triamcinolone acetonide acetate and a preparation method thereof. Background technique [0002] Polymorphism refers to the phenomenon that solid substances form solid states with different physical and chemical properties in two or more different spatial arrangements. In the field of pharmaceutical research, polymorphism includes multi-component crystal forms such as organic solvates and hydrates. Drug polymorphism widely exists in the drug development process and is an inherent characteristic of small organic molecules. Polymorphism is not only controlled by internal factors such as the spatial structure and functional group properties of the molecule itself, intramolecular and intermolecular interactions, but also by drug synthesis process design, crystallization and purification conditions, preparation excipients sele...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07J71/00A61K31/58A61P17/00A61P37/08A61P29/00A61P19/02A61P11/06A61P11/02
CPCC07B2200/13C07J71/00
Inventor 梅雪锋王建荣朱冰清鲍俊杰
Owner SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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