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Stable axitinib compound

A technology of axitinib and compounds, applied in the treatment of chronic renal cell carcinoma, axitinib crystal and its preparation field, can solve the problems of moisture absorption weight gain, high impurity content, difficult purification, etc., and achieve stable physical and chemical properties Effect

Inactive Publication Date: 2015-05-27
TIANJIN HANKANG PHARMA BIOTECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] Axitinib has great advantages in terms of effectiveness and safety, but in the actual production process, the applicant found that there are difficulties in purification, high impurity content and certain moisture absorption and weight gain in the preparation process of Axitinib And other issues

Method used

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  • Stable axitinib compound
  • Stable axitinib compound
  • Stable axitinib compound

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0060] In a 10L reaction kettle equipped with stirring, thermometer, and condenser, add 250g of axitinib, 488ml of isobutanol, 61ml of tetrahydrofuran, and 1951ml of water, start stirring, heat until dissolved, and naturally cool the filtrate to 20°C-35°C , and then left to keep warm for 3 hours, crystals were precipitated, filtered, and dried indoors to obtain 234.6 grams of axitinib white crystals, with a content of 99.95% and a single impurity of less than 0.06%.

[0061] Microparticles or microspheres are prepared by combining the compounds of the present invention with a pharmaceutically acceptable solid or liquid carrier, and optionally with pharmaceutically acceptable adjuvants and vehicles, using standard and conventional techniques. The composition is used for preparing oral preparations and injections. It is given by way of example only and in no way is it intended to limit the scope of the invention in any way.

Embodiment 2

[0063] Tablets containing axitinib

[0064] Prescription: Axitinib 100g, microcrystalline cellulose 10g, pregelatinized starch 15.4g, sodium starch glycolate 4.4g, lactose 150g, PEG-4000 20g, magnesium stearate 4g, polyvinyl chloride 29g Ketone K30, 30 grams of croscarmellose sodium, appropriate amount of distilled water, made into 1000 tablets.

[0065] Process:

[0066] Preparation of tablet core: mix the main ingredient and auxiliary materials evenly according to the determined prescription, granulate, ventilate and dry the granules below 40°C, sieve the granules with 16 meshes, add magnesium stearate and remaining starch, and press into tablets to obtain .

[0067] Isolation layer coating: add talcum powder to 5% polyvinylpyrrolidone (PVP) absolute ethanol solution, stir evenly, and prepare a 20% suspension as the isolation layer coating solution. Coating is carried out in a fluidized bed, and the process conditions are as follows: spray pressure 0.3MPa, liquid inlet sp...

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Abstract

The present invention belongs to the technical field of medicine, and particularly relates to an axitinib crystal and a preparation method thereof. The obtained axitinib crystal of the present invention has advantages of high purity and good stability, wherein the moisture absorption weight increase of the axitinib crystal is not significant even under the high humidity condition. The present invention further relates to applications of a composition using the axitinib crystal in treatment of advanced renal cell carcinoma.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to axitinib crystals and a preparation method thereof, and also relates to the application of the hydrate composition in treating chronic renal cell carcinoma. Background technique [0002] Renal cell carcinoma (RCC) is the most common kidney cancer. Worldwide, more than 210,000 people are diagnosed with RCC each year, resulting in nearly 100,000 deaths. In the past half century, the incidence of RCC has been increasing, and in the United States alone, since 1950, its incidence and fatality rates have increased by 126% and 36.5%, respectively. The natural history of RCC is unpredictable, and its clinical manifestations are complex. In addition to local symptoms (pain, hematuria, and renal mass), systemic (fever, anemia, liver disease, and neuromuscular disease) and endocrine symptoms (red blood cell disease) are more common. increase, hypertension, and hypercalcemia)....

Claims

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Application Information

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IPC IPC(8): C07D401/06A61K31/4439A61P35/00
CPCC07D401/06
Inventor 严洁李轩
Owner TIANJIN HANKANG PHARMA BIOTECH
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