Novel crystal form of sodium valproate, and preparation method and application thereof

A technology of sodium valproate, crystal form, applied in the direction of anhydride/acid/halide active ingredients, nervous system diseases, organic chemistry, etc., can solve the problems of reducing sodium valproate hygroscopicity, poor resolubility, etc. Dissolution time, low water content, pain-reducing effect

Active Publication Date: 2012-07-04
SICHUAN CREDIT CHEMWERTH PHARMACEUTICAL CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In this invention, sodium valproate crystal form III has good solubility, which solves the problem of poor resolubility of existing sodium valproate powder injections, but this patent does not involve research on the hygroscopicity of sodium valproate
[0009] At present, there is no relevant report on reducing the hygroscopicity of sodium valproate by changing the crystal form of sodium valproate

Method used

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  • Novel crystal form of sodium valproate, and preparation method and application thereof
  • Novel crystal form of sodium valproate, and preparation method and application thereof
  • Novel crystal form of sodium valproate, and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Embodiment 1 The preparation method of sodium valproate crystal form I of the present invention

[0029] Weigh 3.00kg of sodium valproate into the reaction kettle, then weigh 20.00kg of acetone into it, heat up to 60-90°C, and start to reflux, measure 0.05L of water into it, and then reflux for 25 minutes, suction filter, The filtrate was naturally cooled to below 25°C at room temperature, crystallized for 2 to 4 hours, filtered with suction, and the filter cake was washed twice with 3.00 kg of acetone. After fully draining the solvent, the filter cake was dried to obtain sodium valproate crystal form I.

[0030] The P-XRD pattern of crystal form I is shown in figure 1 , see the DSC spectrum figure 2 .

[0031] Wherein, in the X-ray diffraction pattern, there are characteristic absorption peaks at (2θ)=5.54°, 6.64°, 20.90°, 24.38° and 26.13°±0.1° (also can be expressed as 5.54°±0.1°, 6.64°±0.1°, 20.90°±0.1°, 24.38°±0.1° and 26.13°±0.1°).

[0032] In the present inv...

Embodiment 2

[0033] Embodiment 2 The preparation method of pharmaceutical composition of the present invention

[0034] Under aseptic conditions, after the sodium valproate crystal form I was prepared by using Example 1, the crystal form I was put into a glass bottle and sealed to obtain the powder injection of sodium valproate crystal form I.

[0035] The beneficial effects of the present invention will be specifically described below through test examples.

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Abstract

The invention discloses a crystal form I of sodium valproate. In an X-ray powder diffraction pattern of the crystal, characteristic absorption peaks appear when a diffraction angle (2 theta) is equal to 5.54+/-0.1 degrees, 6.64+/-0.1 degrees, 20.90+/-0.1 degrees, 24.38+/-0.1 degrees and 26.13+/-0.1 degrees. The invention also discloses a preparation method and application of the crystal form I. According to the crystal form I of the sodium valproate, the moisture absorption is obviously reduced, low water content of the product is ensured, and the sodium valproate has stable quality in a storage period; when the moisture absorption is reduced, the dissolution time of the product is obviously shortened, the resolubility of the product is improved, the treatment effect and high safety of the sodium valproate in clinical treatment are ensured due to high resolubility, the pain during injection is relieved, the compliance of the patient in a treatment period is improved, and a good clinical effect is achieved.

Description

technical field [0001] The invention provides a new crystal form I of sodium valproate, which belongs to the field of medicines. Background technique [0002] Sodium valproate is a first-line broad-spectrum antiepileptic drug. The chemical structural formula is as follows: [0003] [0004] The chemical name of sodium valproate is 2-sodium valproate, molecular formula: C 8 h 15 NaO 2 , with a molecular weight of 166.2, is a white, odorless, crystalline water-soluble powder. It is a better antiepileptic drug and is suitable for various epilepsy (petit mal seizures, focal epilepsy, psychomotor seizures and mixed seizures) and Prevention and treatment of personality and behavioral disorders caused by epilepsy [Chinese Journal of Pharmaceutical Industry 1999, 30(9): 389-390], which can be prepared into oral preparations and injection preparations. At present, the specifications of oral preparations include tablet: 100mg, 200mg, syrup: 5ml: 200mg, 500mg. Sodium valproate...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C53/128A61K31/19A61P25/08
Inventor 傅霖李文婕陈刚陈功政万树伦
Owner SICHUAN CREDIT CHEMWERTH PHARMACEUTICAL CO LTD
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