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Gimeracil crystal form and preparation method thereof

A technology for gimeracil and crystal, which is applied in the field of gimeracil C-type crystal and its preparation, can solve the problems affecting drug efficacy and stability, melting point, solubility, dissolution, bioequivalence difference, etc., to meet the needs of the pharmaceutical industry , The effect of stable properties and high yield

Active Publication Date: 2013-12-25
NANJING CHIA TAI TIANQING PHARMA
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  • Description
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Problems solved by technology

Different crystal forms of the same drug may have significant differences in appearance, melting point, solubility, dissolution, bioequivalence, etc., which will affect the efficacy and stability of the drug

Method used

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  • Gimeracil crystal form and preparation method thereof
  • Gimeracil crystal form and preparation method thereof
  • Gimeracil crystal form and preparation method thereof

Examples

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preparation example Construction

[0023] The preparation of embodiment 1 Gimeracil type C crystals

[0024] 100g of commercially available gimeracil was heated and dissolved in 5L of a mixed solvent composed of ethanol, acetonitrile and water, and the volume percentage of ethanol: acetonitrile: water in the mixed solvent was 15%: 10%: 75%, stirred at 70°C to dissolve it , suction filtration while hot, cooling and crystallization of the filtrate for 16-24 hours, suction filtration, and drying to obtain 89 g of white powdery solid, with a yield of 89%, melting point: 277-278°C, and a purity of 99.92% as determined by HPLC.

[0025] Embodiment 2 Apparatus and test conditions used for identification of gimeracil C-type crystal crystal form

[0026] (i) Powder X-ray Diffraction:

[0027] Instrument: Bruker D8Advance X-ray diffractometer

[0028] Test condition: 40kv 40mA Slit: 1.0 / 1.0 / Ni / 0.2 Step size: 0.02°

[0029] Target type: Cu

[0030] (ii) Differential scanning thermal analysis:

[0031] Instrument: NET...

Embodiment 4

[0039] The preparation of embodiment 4 pharmaceutical composition

[0040] Put 0.58kg of gimeracilidine type C crystal prepared in Example 1, 2kg of tegafur, 1.96kg of oteracil potassium, 8.3kg of lactose, and 0.26kg of sodium lauryl sulfate into the granulator, and start stirring at 1000rpm Mix for 5 minutes, then slowly add 5 kg of 3% hydroxypropyl cellulose solution, and continue stirring for 1 minute after the addition is complete to obtain wet granules. The wet granules were dried at 80°C until the water content was 3% to obtain dry granules. The obtained dry granules are mixed with 0.065kg of magnesium stearate, and further made into capsules by conventional methods in the formulation field.

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Abstract

The invention relates to the technical field of pharmaceutical chemicals, in particular to a gimeracil C-type crystal form and a preparation method thereof. The X-ray powder diffraction reflective angle 2theta+ / -0.2 degrees of the gimeracil C-type crystal form has characteristic peaks at 13.96, 19.57, 23.56, 24.73, 25.14, 26.53, 30.11 and 31.14. The relative peak intensity correspondingly is 100.0, 12.0, 6.5, 32.1, 11.2, 24.0, 13.4 and 8.8. The preparation method comprises the steps of heating and dissolving gimeracil by adopting a mixed solvent of ethanol, acetonitrile and water, performing suction filtration while heating, and cooling filtrate slowly to crystallize.

Description

technical field [0001] The invention relates to the technical field of medicine and chemical engineering, in particular to a gimeracilidine C-type crystal and a preparation method thereof. Background technique [0002] In my country, the morbidity and mortality of gastric cancer rank among the top three among cancer patients. Gastric cancer accounts for a quarter of cancer deaths, and about half of the deaths from malignant tumors of the digestive system are caused by gastric cancer. [0003] S-1 is a fourth-generation fluorouracil derivative oral anticancer agent developed by Japan Dapeng Pharmaceutical Co., Ltd. It is widely used in advanced gastric cancer, head and neck cancer, rectal cancer, non-small cell lung cancer, metastatic breast cancer and treatment of tumors such as pancreatic cancer. It is mainly used in the treatment of gastric cancer. According to statistics, more than 80% of the cases of chemotherapy for advanced gastric cancer in Japan use S-1, and the eff...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D213/69A61K31/4412A61P35/00
Inventor 徐丹林帅柴雨柱杨治旻田舟山
Owner NANJING CHIA TAI TIANQING PHARMA
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