Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

Polymorphism of methocarbamol dipotassium phosphate and preparation method thereof

A technology of dipotassium phosphate dipotassium methocarbamol and dipotassium phosphate dimethocarbamol, which is applied in the field of polymorphs and their preparation, and can solve the problems of easily absorbing moisture and forming hard particles, unstable solids, and difficult precipitation of solids, etc. problems, to achieve the effects of convenient production, transportation and storage, improved stability, and uniform dispersion

Inactive Publication Date: 2013-06-05
NANKAI UNIV
View PDF4 Cites 1 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, because Methocarbamol itself is insoluble in water, and its water solubility is only 1:210, it has been adversely affected in clinical application.
[0003] Patent CN101863917A provides a method for structurally modifying Methocarbamol to synthesize Methocarbamol Phosphate. Although the solubility is improved, because Methocarbamol Dipotassium Phosphate is not sensitive to temperature, it is difficult to obtain it after cooling down during conventional refining. Precipitate solid, the precipitated solid is also unstable, easy to absorb moisture and form hard particles
There are still no reports on the stable polymorphic form of Methocarbamol Dipotassium Phosphate

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
  • Polymorphism of methocarbamol dipotassium phosphate and preparation method thereof
  • Polymorphism of methocarbamol dipotassium phosphate and preparation method thereof
  • Polymorphism of methocarbamol dipotassium phosphate and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] Dissolve 3.52g of dipotassium methocarbamol phosphate in 3mL of distilled water, heat in a water bath to 60°C to completely dissolve the solid, cool to room temperature and add absolute ethanol dropwise, filter after complete crystallization, and dry at 50°C for 8 hours to obtain the crystal form P, melting point: 155-157°C.

Embodiment 2

[0029] Dissolve 13.27g of dipotassium methocarbamol phosphate in 15mL of distilled water, heat in a water bath to 55°C to completely dissolve the solid, cool to room temperature and add methanol dropwise, filter after complete crystallization, and dry at 50°C for 8 hours to obtain crystal form P. Melting point: 155-156°C.

Embodiment 3

[0031] Dissolve 7.32g of dipotassium methocarbamol phosphate in 10mL of distilled water, heat in a water bath to 60°C to completely dissolve the solid, cool to room temperature and add isopropanol dropwise, filter after complete crystallization, and dry at 50°C for 8 hours to obtain the crystal form P, melting point: 156-157°C.

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
melting pointaaaaaaaaaa
melting pointaaaaaaaaaa
Login to View More

Abstract

The invention provides a polymorphism of methocarbamol dipotassium phosphate and a preparation method thereof, and relates to a polymorphism corresponding to 3-(o-methoxyphenoxy)-2-hydroxypropyl amino-acid ester dipotassium phosphate (methocarbamol dipotassium phosphate) and a preparation method thereof. A medicament containing the crystal form can be used for treating muscle sprain, lumbar muscle strain and ischialgia. The crystal form is specified by characterization results of an X-ray powder diffraction pattern (shown as Figure 1), nuclear magnetic resonance absorption spectra (shown as Figures 2-4), a thermogravimetry-differential thermal analysis curve (shown as Figure 5), an infrared spectrum absorption curve (shown as Figure 8) and liquid chromatography / mass spectrometry. The powder of the polymorphism is fine and uniform in dispersion; the stability is increased; the water solubility is 1:1; and the crystallization process is simple and convenient to implement production / transportation / storage, and conforms to the requirements for medicament preparation.

Description

technical field [0001] The present invention relates to 3-(o-methoxyphenoxy)-2-hydroxypropyl amino acid ester phosphate dipotassium salt (mesocarbamol phosphate dipotassium salt), a polymorph and its preparation method. The medicine containing the crystal form can be used for treating muscle sprain, lumbar muscle strain and sciatica. Background technique [0002] In Chinese patent CN101863917A (publication number), it is recorded that 3-(o-methoxyphenoxy)-2-hydroxypropyl amino acid ester (mesocarbamol) is an effective drug for treating symptoms such as abnormal muscle tension, spasm, and stiffness. Drugs are highly effective in the treatment of muscle sprains, lumbar muscle strain, sciatica, and lumbar disc herniation. However, because Methocarbamol itself is insoluble in water, and its water solubility is only 1:210, its clinical application has been adversely affected accordingly. [0003] Patent CN101863917A provides a method for structurally modifying Methocarbamol to ...

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 Applications(China)
IPC IPC(8): C07C271/12C07C269/08A61P21/00A61P25/02
Inventor 周煜乔园园
Owner NANKAI UNIV
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products