Methylprednisolone aceponate new crystal form and preparation method thereof

A technology of methylprednisolone acetonide and crystal, applied in directions such as pharmaceutical formulations, medical preparations containing active ingredients, steroids, etc., can solve problems such as no reports on the crystal form of methylprednisolone acetonide.

Inactive Publication Date: 2012-06-27
TIANJIN JINYAO GRP
View PDF2 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In addition, there is no other related crystal form report of methylprednisolone acetate

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Methylprednisolone aceponate new crystal form and preparation method thereof
  • Methylprednisolone aceponate new crystal form and preparation method thereof
  • Methylprednisolone aceponate new crystal form and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] Get 1kg of methylprednisolone acetate and completely dissolve it in 10L of tetrahydrofuran, then add a dissolution agent mixed with 5L of water and 5L of ethanol to the tetrahydrofuran in which methylprednisolone acetate has been dissolved, add it slowly while adding the dissolution agent While oscillating, until the turbidity that appeared when the eluent was just added disappears, evaporate under reduced pressure after the addition, and cool down, filter, and dry after crystals appear. The water content of the dried crystal was measured by the Karl Fischer method, and it was confirmed to be methylprednisolone acetate monohydrate. X-ray powder diffraction measurement, the measured characteristic peak positions are 2θ=8.6°, 12.2°, 13.6°, 15.3°, 19.3°, such as figure 2 shown.

Embodiment 2

[0027] Get 1kg of methylprednisolone acetate and dissolve it completely in 40L of acetonitrile, then add 4L of water and 20L of normal hexane as a dissolution agent to the acetonitrile in which methylprednisolone acetate has been dissolved, add slowly while adding the dissolution agent While oscillating, until the turbidity that appeared when the eluent was just added disappears, evaporate under reduced pressure after the addition, and cool down, filter, and dry after crystals appear. The water content of the dried crystal was measured by the Karl Fischer method, and it was confirmed to be methylprednisolone acetate monohydrate. X-ray powder diffraction measurement, the measured characteristic peak positions are 2θ=8.6°, 12.2°, 13.6°, 15.3°, 19.3°.

Embodiment 3

[0029] Add 0.2 g of methylprednisolone acetate into a mixed solution of 6 mL of tetrahydrofuran, 1 mL of water, and 2 mL of methanol, and stir until completely dissolved. The solution was transferred to a small beaker, sealed with parafilm, and a few small holes were punched on the film to facilitate solvent evaporation. After standing at room temperature for several days, crystallization was obtained. The water content of the dried crystal was measured by the Karl Fischer method, and it was confirmed to be methylprednisolone acetate monohydrate. X-ray powder diffraction measurement, the measured characteristic peak positions are 2θ=8.5°, 12.1°, 13.6°, 15.3°, 19.3°, such as image 3 shown.

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more

PUM

PropertyMeasurementUnit
boiling pointaaaaaaaaaa
wavelengthaaaaaaaaaa
Login to view more

Abstract

The invention relates to a methylprednisolone aceponate new crystal form and preparation method thereof. X-ray powder diffraction has characteristic peak at diffraction angle 2theta of 8.6 degrees, 12.2 degrees, 13.6 degrees, 15.3 degrees, 18.6 degrees and 19.3 degrees, and the method that methylprednisolone aceponate is fully dissolved into mixed solution of water and organic solvent, and then the organic solvent is evaporated can be adopted to prepare the new crystal form.

Description

Technical field: [0001] The invention relates to a steroid compound, in particular to a new crystal form of methylprednisolone acetate and a preparation method thereof. Background technique: [0002] The chemical structural formula of methylprednisolone acetate (Methylprednisolone aceponate, MPA, CAS: 86401-95-8) is as follows: [0003] [0004] Methylprednisolone acetate is developed by SchringAG of Germany as a derivative of methylprednisolone. It is a glucocorticoid with strong local anti-inflammatory activity and is used for the treatment of skin inflammation. At present, commercially available vinegar Promethylprednisolone skin preparations are produced by Schring AG in Germany, and the trade name is Advantan 0.1% Acetate methylprednisolone cream, which can be used to inhibit inflammation and allergic skin reactions, and also inhibit reactions associated with accelerated cell regeneration This leads to symptoms such as erythema, edema, skin thickening, subsidence of...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more

Application Information

Patent Timeline
no application Login to view more
Patent Type & Authority Patents(China)
IPC IPC(8): C07J5/00A61K31/573A61P29/00A61P17/00
Inventor 何运良李静
Owner TIANJIN JINYAO GRP
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Try Eureka
PatSnap group products