Polymorphism of methocarbamol dipotassium phosphate and preparation method thereof

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 ...

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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

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