New crystal form for sodium valproate and preparation method and usage thereof

Abstract

The invention provides a sodium valproate crystal form III. In a diffraction pattern of powder X-ray diffraction of a crystal, characteristic absorption peaks exist at diffraction angles (2 theta) of 5.40 DEG, 6.31+ / -0.1 DEG, 7.28 DEG, 76.86 DEG and 18.10 DEG. The invention also provides a preparation method of the crystal form and a medicinal composition containing the crystal form. The sodium valproate crystal from III has high solubility and controllability, is safe and stable and provides a new preparation choice for clinical application.

Description

technical field [0001] The invention provides a new crystal form of sodium valproate, which belongs to the field of medicine. 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 The prevention and treatment of personality and behavior disorder caused by epilepsy 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 can be administered by intravenous infusion to treat complex partial epile...

AI Technical Summary

Problems solved by technology

[0005] The lyophilized preparation of sodium valproate is a commonly used preparation for injection. The sodium valproate for injection that has been on the market consumes a lot of energy during the freeze-drying process, and the prepared sodium valproate powder injection has the following defects: appearance molding Not good, poor resolubility (usually fully dissolved within 120 seconds), high water content, poor stability, high endotoxin content

Among them, the resolubility is poor, that is, the drug dissolves slowly or incompletely, which can easily cause diseases such as vascular obstruction, insufficient blood supply, phlebitis, thrombus, local tissue necrosis, etc., and it is also easy to cause pain when the patient is injected. The medication cannot reach the drug concentration required for the treatment, and it is difficult to achieve the expected therapeutic effect. There is no clear limit value to control the solubility index of the product; the water content of the product is too high, and the weight loss on drying limit of commercially available products is no more than 3.0%. , the moisture in the freeze-dried product is too high, the product is more unstable during transportation and storage, and it will cause the final product to lose weight on drying. Strictly, the amount of endotoxin in 1 mg of sodium valproate is less than 0.3 EU, and the content of endotoxin is high, which greatly increases the risk of pyrogen reaction during clinical medication

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